Cannabis Prof. Suleiman Olimat. Cannabis القنب الهندي نبات الحشيش.
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Transcript of Cannabis Prof. Suleiman Olimat. Cannabis القنب الهندي نبات الحشيش.
Cannabis
Prof Suleiman Olimat
Cannabis
الهندي القنبالحشيش نبات
Cannabis is a genus of flowering plant that includes one or more species The plant is believed to have originated in the mountainous regions just north-west of the Himalayas in India though it could also have come from Northern Africa It is also known as hemp although this term usually refers to Cannabis cultivated for non-drug use
Cannabis sppThere are three species known Cannabis sativa C indica and C rudelarisThe leaves are the most recognisable and well-
known aspect of the cannabis plant Despite the great degree of variation found naturally in local populations of cannabis the leaves do not alter greatly in appearance between varieties
Hemp
What is Marijuana
Marijuana is the dried mix of flowers and leaves form the female Cannabis Sativa plant
Hashish is the resin or sap harvested from the plant
Hashish oil is the essential oil of the female Cannabis Sativa plant
Marijuana ndash History of Use
bull Cannabis ndash native to central Asia
bull Chinese ndash first to use employed for fabric medicines
bull India ndash country where first used for hallucinogenic properties
bull Africa ndash introduced through Arab traders used as medicine
bull Europe ndash became popular in 1800s
bull USA ndash 1900s -- use proscribed outlawed
bull End of 20th century ndash contentious debate regarding merits of legalization
HempvsMarijuana-1
bull The word hempis English for a number of varieties of the Cannabisplant particularly the varieties like industrial hemp that were bred over time for industrial uses such as fuel fiber paper seed food oil etc
HempvsMarijuana-2
bull The term marijuanais of Spanish derivation and was primarily used to describe varieties of Cannabisthat were more commonly bred over time for medicinal and recreational purposes like Cannabisindica and certain strains of Cannabissativa
HempvsMarijuana-3
bull Two cannabinoids are preponderant in Cannabis
bull THC CBDbull psychoactive ingredient antipsychoactive ingredient
Marijuana Hempbull (leaves and flowers of the female plant)
bull High in THC High in CBDbull Low in THCbull Low in CBD
Cannabis BiologyMajor Drug Component ndash delta-trans-tetrahydrocannabinol (THC)
- binds to specific receptors in brain
THC- produced in glands on leaves and flowers
-- female plants produce more glands
-- gland production stimulated by heat sunlight drought
-- sinsemilla (sin = without semilla = seeds) ndash particularly strong
Hashish ndash product - relatively pure resin
Glands THC
Chemical constituents of Cannabis
bull Cannabinoids (66)bull Nitrogenous compounds (27)bull Amino acids(18)bull Proteins enzymes (11)bull Sugars (34)bull Hydrocarbons (50)bull Simple alcohols (7)bull Simple aldehydes (12)bull Simple ketones (13)bull Simple acids (21)bull Fatty acids (22)bull Simple esterslactones (13)bull Steroids (11)bull Terpenes (20)bull Non-cannabinoid phenols (25)bull Flavoroids (21)bull Vitamins (1)bull Pigments (2)bull Elements (9) bull Total known compounds (483)
What is a cannabinoid
bullInitially compounds extracted by Cannabis spp producing characteristic psychoactivity
bullLater compounds with a characteristic terpenoid structure
bullCurrently most any compound that produces cannabinoid psychoactivity natural or synthetic
bullOccasionally just compounds that will interact with cannabinoid receptors
What are cannabinoidsbull Group of gt60 dibenzopyran chemicals found in
leaves and flowering tops of female cannabis plant (Cannabis sativa and Cannabis indica)
bull Some common cannabinoids are
In the plantIn your body (endogenous)
Synthetic
Δ9 ndash THC 2-arichidonyl glycerol (2 ndash AG)
CP 55940
Δ8 ndash THC anandamideHU ndash 210
cannabidiol and cannabinol
Natural cannabinoids
Representative cannabinoids
Classical cannabinoids Non-classical cannabinoid Aminoalkylindole
CB1 antagonists
Endogenous cannabinoids
Receptors suggest endogenous ligandsTwo main families identifiedBoth arachidonic acid derivativesPrecursors in membranes
ldquoMade on demandrdquoAmides (anandamide)
Esters (2-AG)
bull Significant differences
ndash Routes of synthesis ndash Mode of degradation
(FAAH vs MAGL)ndash Efficacy
Endocannabinoids
bull Anandamide (Sanskrit ananda inner bliss) is one endocannabinoid It is found in chocolate (though there is some controversy over whether the small quantity has any effect on the body) It is about as potent as THC
Structure of THC and synthetic analogs
Lipophilic side chain Most potent analog 100s
times more potent than THC
with 4 major cannabinoids in the plant
bull 2 isomers a trans-delta-9-THC and a delta-8-THC
bull A cannabidiol (the 2nd most abundant psychoactive ingredient after THC)
bull A cannabinol a decomposition product of THC that accumulates as cannabis samples age
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
THC
bull Variedly aromatic ring (C Ring)
O
O
H
11rsquo-di-methyl-pyrane ring (B ring)
Variedly unsaturated cyclohexyl ring (A ring)
Results of SAR
bull Psychoactive properties are (-) trans-enatioselective
bull Length lipophilicity C3 alkyl chain
bull Phenolic hydroxyl-group
bull C9 substitute
O
O
H
Modes of Absorption
bull The most common method of absorption is smoking Either in a loosely rolled cigarette called a joint or through a pipe or water pipe
Smoking and the Body
THC enters the body through the Lungs
The smoke is inhaled and held in the lungsAll affect how much THC will enter the plasmaTHC crosses the blood barrier through the capillaries in the lungs
After inhalation THC can reach the brain in about 14 seconds
After a 6 min smoking period peak blood levels reached at about 7 min (100 ngml plasma)
Most THC is absorbed from the blood within 30 min
Moves rapidly into the brain and across the bloodbrainplacental barrier Because fatty chains make it very lipid soluble
Half-life is about 19 hours Can store in fat cells
Established physiological effects are dose related
Lethal dose for THC use has now been studied and no human deaths have been reported due to intoxication from cannabis
Metabolites
bull Radioactively labeled delta-9-THC has been found to persist in the body as an active metabolite as long as 8 days after use
Primary metabolite has a half-life of 50 hours The complete elimination of the drug can take as long as 6 weeks
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
23 of metabolites are excreted in feces13 of metabolites are excreted in urine
Cannabis Pharmacology
Primary Cannabinoids from Cannabis are
bull Cannabinol (CBN) Cannabidiol (CBD) and Tetrahydrocannabinol (THC)
bull THC (-9-THC ) is the only one with significant psychoactive properties
bull CBN - 110 th activity of THC CBD - none
bull 2 isomers a trans-delta-9-THC and a delta-8-THC
bull A cannabidiol (the 2nd most abundant psychoactive ingredient after THC)
bull A cannabinol a decomposition product of THC that accumulates as cannabis samples age
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
Therapeutic
bull Antiemeticbull Reduction of intra-ocular tensionbull Analgesicbull Muscle relaxant bull Anti-convulsant bull Anti-inflammatory appetite ldquothe munchiesrdquo It is one of the most well-known effects of marijuana the
powerful surge in appetite many users feel after smoking or ingesting the drug colloquially known as the munchies
Marinol
THC in a sesame oil suspension
Cannabinoid ReceptorsBeforethe 1980s it was often speculated that
cannabinoids produced their effects through non specific interaction with cell membranes instead of interacting with specific receptors
The discovery of the first cannabinoid receptors in the 1980s helped to resolve this debate These receptors are common in animals and have been found in mammals birds fishes and reptiles
There are currently two known types of cannabinoid receptors CB1 and CB2
CB1 ReceptorsFound primarily in the brain (specifically basal ganglia limbic
system including the hippocampus and cerebellum)1048766Most dense in brain regions involved with thinking and memory
attention and control of movement1048766Also present in both male and female reproductive systems as
well as in the lungs liver and kidneys1048766Appear to be responsible for the euphoric and anticonvulsive
effects of Cannabis1048766Essentially absent in the medulla oblongata the part of the brain
that is responsible for respiratory and cardiovascular functions
Thus there is no risk of respiratory or cardiovascular failure as there is with many other drugs
CB2 Receptor
CB2 receptors are almost exclusively found in the immune system (T cells macrophages B cells) with the greatest density in the spleen
1048766CB2 receptors appear to be responsible for the anti-inflammatory and possible other therapeutic effects of Cannabis
1048766Also expressed on peripheral nerve terminals
Cannabis and Δ9- (THC) for weight loss
bull Obesity is one of the highest preventable causes of morbidity and mortality in the developed world It has been well known for a long time that exposure to cannabis produces an increase of appetite (a phenomenon referred to as the munchies) This phenomenon led to an exploration of the role of the endocannabinoid system in the regulation of obesity and associated metabolic syndrome This effort subsequently led to the development of a successful therapeutic approach for obesity that consisted of blocking the cannabinoid CB1 receptors using ligands such as Rimonabant in order to produce weight loss and improve metabolic profile
What is obesity
Obesity is characterized by an abnormal accumulation of body fat usually 20 percent or more over an individuals ideal body weight Obesity results when the size or number of fat cells in a persons body increases When a person gains weight these fat cells first increase in size and later in number When a person starts losing weight the cells decreas ein size but their number generally stays the same This is part of the reason that once you gain a significant amount of weight it is more difficult to lose it
The clinical definition of obesity is a body mass index(BMI)of 30 or higher BMI = Weight (in kg) Height (in meters) Squared
Rimonabant
bull Acompliareg(Sanofi-Aventis)
launched in Europe in 2006 for
oral treatment of obesity at 20 mg
once daily
Selective blocker of central
and peripheral CB1 receptors
It reduces food intake and improves lipid and glucose metabolism
Rimonabant
Despite being efficacious Rimonabant was associated with increased rates of depression and anxiety and therefore removed from the market
- Cannabis
- Slide 2
- Slide 3
- Cannabis spp
- Slide 5
- Slide 6
- Hemp
- What is Marijuana
- Marijuana ndash History of Use
- HempvsMarijuana-1
- HempvsMarijuana-2
- HempvsMarijuana-3
- Cannabis Biology
- Chemical constituents of Cannabis
- What is a cannabinoid
- What are cannabinoids
- Natural cannabinoids
- Slide 18
- Representative cannabinoids
- Slide 20
- Endocannabinoids
- Structure of THC and synthetic analogs
- Slide 23
- Slide 24
- THC
- Results of SAR
- Modes of Absorption
- Smoking and the Body
- Slide 29
- Slide 30
- Metabolites
- Slide 32
- Slide 33
- Cannabis Pharmacology
- Slide 35
- Therapeutic
- Marinol
- Cannabinoid Receptors
- CB1 Receptors
- CB2 Receptor
- Cannabis and Δ9- (THC) for weight loss
- What is obesity
- Slide 43
- Slide 44
- Rimonabant
- Slide 46
- Slide 47
- Slide 48
-
Cannabis
الهندي القنبالحشيش نبات
Cannabis is a genus of flowering plant that includes one or more species The plant is believed to have originated in the mountainous regions just north-west of the Himalayas in India though it could also have come from Northern Africa It is also known as hemp although this term usually refers to Cannabis cultivated for non-drug use
Cannabis sppThere are three species known Cannabis sativa C indica and C rudelarisThe leaves are the most recognisable and well-
known aspect of the cannabis plant Despite the great degree of variation found naturally in local populations of cannabis the leaves do not alter greatly in appearance between varieties
Hemp
What is Marijuana
Marijuana is the dried mix of flowers and leaves form the female Cannabis Sativa plant
Hashish is the resin or sap harvested from the plant
Hashish oil is the essential oil of the female Cannabis Sativa plant
Marijuana ndash History of Use
bull Cannabis ndash native to central Asia
bull Chinese ndash first to use employed for fabric medicines
bull India ndash country where first used for hallucinogenic properties
bull Africa ndash introduced through Arab traders used as medicine
bull Europe ndash became popular in 1800s
bull USA ndash 1900s -- use proscribed outlawed
bull End of 20th century ndash contentious debate regarding merits of legalization
HempvsMarijuana-1
bull The word hempis English for a number of varieties of the Cannabisplant particularly the varieties like industrial hemp that were bred over time for industrial uses such as fuel fiber paper seed food oil etc
HempvsMarijuana-2
bull The term marijuanais of Spanish derivation and was primarily used to describe varieties of Cannabisthat were more commonly bred over time for medicinal and recreational purposes like Cannabisindica and certain strains of Cannabissativa
HempvsMarijuana-3
bull Two cannabinoids are preponderant in Cannabis
bull THC CBDbull psychoactive ingredient antipsychoactive ingredient
Marijuana Hempbull (leaves and flowers of the female plant)
bull High in THC High in CBDbull Low in THCbull Low in CBD
Cannabis BiologyMajor Drug Component ndash delta-trans-tetrahydrocannabinol (THC)
- binds to specific receptors in brain
THC- produced in glands on leaves and flowers
-- female plants produce more glands
-- gland production stimulated by heat sunlight drought
-- sinsemilla (sin = without semilla = seeds) ndash particularly strong
Hashish ndash product - relatively pure resin
Glands THC
Chemical constituents of Cannabis
bull Cannabinoids (66)bull Nitrogenous compounds (27)bull Amino acids(18)bull Proteins enzymes (11)bull Sugars (34)bull Hydrocarbons (50)bull Simple alcohols (7)bull Simple aldehydes (12)bull Simple ketones (13)bull Simple acids (21)bull Fatty acids (22)bull Simple esterslactones (13)bull Steroids (11)bull Terpenes (20)bull Non-cannabinoid phenols (25)bull Flavoroids (21)bull Vitamins (1)bull Pigments (2)bull Elements (9) bull Total known compounds (483)
What is a cannabinoid
bullInitially compounds extracted by Cannabis spp producing characteristic psychoactivity
bullLater compounds with a characteristic terpenoid structure
bullCurrently most any compound that produces cannabinoid psychoactivity natural or synthetic
bullOccasionally just compounds that will interact with cannabinoid receptors
What are cannabinoidsbull Group of gt60 dibenzopyran chemicals found in
leaves and flowering tops of female cannabis plant (Cannabis sativa and Cannabis indica)
bull Some common cannabinoids are
In the plantIn your body (endogenous)
Synthetic
Δ9 ndash THC 2-arichidonyl glycerol (2 ndash AG)
CP 55940
Δ8 ndash THC anandamideHU ndash 210
cannabidiol and cannabinol
Natural cannabinoids
Representative cannabinoids
Classical cannabinoids Non-classical cannabinoid Aminoalkylindole
CB1 antagonists
Endogenous cannabinoids
Receptors suggest endogenous ligandsTwo main families identifiedBoth arachidonic acid derivativesPrecursors in membranes
ldquoMade on demandrdquoAmides (anandamide)
Esters (2-AG)
bull Significant differences
ndash Routes of synthesis ndash Mode of degradation
(FAAH vs MAGL)ndash Efficacy
Endocannabinoids
bull Anandamide (Sanskrit ananda inner bliss) is one endocannabinoid It is found in chocolate (though there is some controversy over whether the small quantity has any effect on the body) It is about as potent as THC
Structure of THC and synthetic analogs
Lipophilic side chain Most potent analog 100s
times more potent than THC
with 4 major cannabinoids in the plant
bull 2 isomers a trans-delta-9-THC and a delta-8-THC
bull A cannabidiol (the 2nd most abundant psychoactive ingredient after THC)
bull A cannabinol a decomposition product of THC that accumulates as cannabis samples age
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
THC
bull Variedly aromatic ring (C Ring)
O
O
H
11rsquo-di-methyl-pyrane ring (B ring)
Variedly unsaturated cyclohexyl ring (A ring)
Results of SAR
bull Psychoactive properties are (-) trans-enatioselective
bull Length lipophilicity C3 alkyl chain
bull Phenolic hydroxyl-group
bull C9 substitute
O
O
H
Modes of Absorption
bull The most common method of absorption is smoking Either in a loosely rolled cigarette called a joint or through a pipe or water pipe
Smoking and the Body
THC enters the body through the Lungs
The smoke is inhaled and held in the lungsAll affect how much THC will enter the plasmaTHC crosses the blood barrier through the capillaries in the lungs
After inhalation THC can reach the brain in about 14 seconds
After a 6 min smoking period peak blood levels reached at about 7 min (100 ngml plasma)
Most THC is absorbed from the blood within 30 min
Moves rapidly into the brain and across the bloodbrainplacental barrier Because fatty chains make it very lipid soluble
Half-life is about 19 hours Can store in fat cells
Established physiological effects are dose related
Lethal dose for THC use has now been studied and no human deaths have been reported due to intoxication from cannabis
Metabolites
bull Radioactively labeled delta-9-THC has been found to persist in the body as an active metabolite as long as 8 days after use
Primary metabolite has a half-life of 50 hours The complete elimination of the drug can take as long as 6 weeks
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
23 of metabolites are excreted in feces13 of metabolites are excreted in urine
Cannabis Pharmacology
Primary Cannabinoids from Cannabis are
bull Cannabinol (CBN) Cannabidiol (CBD) and Tetrahydrocannabinol (THC)
bull THC (-9-THC ) is the only one with significant psychoactive properties
bull CBN - 110 th activity of THC CBD - none
bull 2 isomers a trans-delta-9-THC and a delta-8-THC
bull A cannabidiol (the 2nd most abundant psychoactive ingredient after THC)
bull A cannabinol a decomposition product of THC that accumulates as cannabis samples age
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
Therapeutic
bull Antiemeticbull Reduction of intra-ocular tensionbull Analgesicbull Muscle relaxant bull Anti-convulsant bull Anti-inflammatory appetite ldquothe munchiesrdquo It is one of the most well-known effects of marijuana the
powerful surge in appetite many users feel after smoking or ingesting the drug colloquially known as the munchies
Marinol
THC in a sesame oil suspension
Cannabinoid ReceptorsBeforethe 1980s it was often speculated that
cannabinoids produced their effects through non specific interaction with cell membranes instead of interacting with specific receptors
The discovery of the first cannabinoid receptors in the 1980s helped to resolve this debate These receptors are common in animals and have been found in mammals birds fishes and reptiles
There are currently two known types of cannabinoid receptors CB1 and CB2
CB1 ReceptorsFound primarily in the brain (specifically basal ganglia limbic
system including the hippocampus and cerebellum)1048766Most dense in brain regions involved with thinking and memory
attention and control of movement1048766Also present in both male and female reproductive systems as
well as in the lungs liver and kidneys1048766Appear to be responsible for the euphoric and anticonvulsive
effects of Cannabis1048766Essentially absent in the medulla oblongata the part of the brain
that is responsible for respiratory and cardiovascular functions
Thus there is no risk of respiratory or cardiovascular failure as there is with many other drugs
CB2 Receptor
CB2 receptors are almost exclusively found in the immune system (T cells macrophages B cells) with the greatest density in the spleen
1048766CB2 receptors appear to be responsible for the anti-inflammatory and possible other therapeutic effects of Cannabis
1048766Also expressed on peripheral nerve terminals
Cannabis and Δ9- (THC) for weight loss
bull Obesity is one of the highest preventable causes of morbidity and mortality in the developed world It has been well known for a long time that exposure to cannabis produces an increase of appetite (a phenomenon referred to as the munchies) This phenomenon led to an exploration of the role of the endocannabinoid system in the regulation of obesity and associated metabolic syndrome This effort subsequently led to the development of a successful therapeutic approach for obesity that consisted of blocking the cannabinoid CB1 receptors using ligands such as Rimonabant in order to produce weight loss and improve metabolic profile
What is obesity
Obesity is characterized by an abnormal accumulation of body fat usually 20 percent or more over an individuals ideal body weight Obesity results when the size or number of fat cells in a persons body increases When a person gains weight these fat cells first increase in size and later in number When a person starts losing weight the cells decreas ein size but their number generally stays the same This is part of the reason that once you gain a significant amount of weight it is more difficult to lose it
The clinical definition of obesity is a body mass index(BMI)of 30 or higher BMI = Weight (in kg) Height (in meters) Squared
Rimonabant
bull Acompliareg(Sanofi-Aventis)
launched in Europe in 2006 for
oral treatment of obesity at 20 mg
once daily
Selective blocker of central
and peripheral CB1 receptors
It reduces food intake and improves lipid and glucose metabolism
Rimonabant
Despite being efficacious Rimonabant was associated with increased rates of depression and anxiety and therefore removed from the market
- Cannabis
- Slide 2
- Slide 3
- Cannabis spp
- Slide 5
- Slide 6
- Hemp
- What is Marijuana
- Marijuana ndash History of Use
- HempvsMarijuana-1
- HempvsMarijuana-2
- HempvsMarijuana-3
- Cannabis Biology
- Chemical constituents of Cannabis
- What is a cannabinoid
- What are cannabinoids
- Natural cannabinoids
- Slide 18
- Representative cannabinoids
- Slide 20
- Endocannabinoids
- Structure of THC and synthetic analogs
- Slide 23
- Slide 24
- THC
- Results of SAR
- Modes of Absorption
- Smoking and the Body
- Slide 29
- Slide 30
- Metabolites
- Slide 32
- Slide 33
- Cannabis Pharmacology
- Slide 35
- Therapeutic
- Marinol
- Cannabinoid Receptors
- CB1 Receptors
- CB2 Receptor
- Cannabis and Δ9- (THC) for weight loss
- What is obesity
- Slide 43
- Slide 44
- Rimonabant
- Slide 46
- Slide 47
- Slide 48
-
Cannabis is a genus of flowering plant that includes one or more species The plant is believed to have originated in the mountainous regions just north-west of the Himalayas in India though it could also have come from Northern Africa It is also known as hemp although this term usually refers to Cannabis cultivated for non-drug use
Cannabis sppThere are three species known Cannabis sativa C indica and C rudelarisThe leaves are the most recognisable and well-
known aspect of the cannabis plant Despite the great degree of variation found naturally in local populations of cannabis the leaves do not alter greatly in appearance between varieties
Hemp
What is Marijuana
Marijuana is the dried mix of flowers and leaves form the female Cannabis Sativa plant
Hashish is the resin or sap harvested from the plant
Hashish oil is the essential oil of the female Cannabis Sativa plant
Marijuana ndash History of Use
bull Cannabis ndash native to central Asia
bull Chinese ndash first to use employed for fabric medicines
bull India ndash country where first used for hallucinogenic properties
bull Africa ndash introduced through Arab traders used as medicine
bull Europe ndash became popular in 1800s
bull USA ndash 1900s -- use proscribed outlawed
bull End of 20th century ndash contentious debate regarding merits of legalization
HempvsMarijuana-1
bull The word hempis English for a number of varieties of the Cannabisplant particularly the varieties like industrial hemp that were bred over time for industrial uses such as fuel fiber paper seed food oil etc
HempvsMarijuana-2
bull The term marijuanais of Spanish derivation and was primarily used to describe varieties of Cannabisthat were more commonly bred over time for medicinal and recreational purposes like Cannabisindica and certain strains of Cannabissativa
HempvsMarijuana-3
bull Two cannabinoids are preponderant in Cannabis
bull THC CBDbull psychoactive ingredient antipsychoactive ingredient
Marijuana Hempbull (leaves and flowers of the female plant)
bull High in THC High in CBDbull Low in THCbull Low in CBD
Cannabis BiologyMajor Drug Component ndash delta-trans-tetrahydrocannabinol (THC)
- binds to specific receptors in brain
THC- produced in glands on leaves and flowers
-- female plants produce more glands
-- gland production stimulated by heat sunlight drought
-- sinsemilla (sin = without semilla = seeds) ndash particularly strong
Hashish ndash product - relatively pure resin
Glands THC
Chemical constituents of Cannabis
bull Cannabinoids (66)bull Nitrogenous compounds (27)bull Amino acids(18)bull Proteins enzymes (11)bull Sugars (34)bull Hydrocarbons (50)bull Simple alcohols (7)bull Simple aldehydes (12)bull Simple ketones (13)bull Simple acids (21)bull Fatty acids (22)bull Simple esterslactones (13)bull Steroids (11)bull Terpenes (20)bull Non-cannabinoid phenols (25)bull Flavoroids (21)bull Vitamins (1)bull Pigments (2)bull Elements (9) bull Total known compounds (483)
What is a cannabinoid
bullInitially compounds extracted by Cannabis spp producing characteristic psychoactivity
bullLater compounds with a characteristic terpenoid structure
bullCurrently most any compound that produces cannabinoid psychoactivity natural or synthetic
bullOccasionally just compounds that will interact with cannabinoid receptors
What are cannabinoidsbull Group of gt60 dibenzopyran chemicals found in
leaves and flowering tops of female cannabis plant (Cannabis sativa and Cannabis indica)
bull Some common cannabinoids are
In the plantIn your body (endogenous)
Synthetic
Δ9 ndash THC 2-arichidonyl glycerol (2 ndash AG)
CP 55940
Δ8 ndash THC anandamideHU ndash 210
cannabidiol and cannabinol
Natural cannabinoids
Representative cannabinoids
Classical cannabinoids Non-classical cannabinoid Aminoalkylindole
CB1 antagonists
Endogenous cannabinoids
Receptors suggest endogenous ligandsTwo main families identifiedBoth arachidonic acid derivativesPrecursors in membranes
ldquoMade on demandrdquoAmides (anandamide)
Esters (2-AG)
bull Significant differences
ndash Routes of synthesis ndash Mode of degradation
(FAAH vs MAGL)ndash Efficacy
Endocannabinoids
bull Anandamide (Sanskrit ananda inner bliss) is one endocannabinoid It is found in chocolate (though there is some controversy over whether the small quantity has any effect on the body) It is about as potent as THC
Structure of THC and synthetic analogs
Lipophilic side chain Most potent analog 100s
times more potent than THC
with 4 major cannabinoids in the plant
bull 2 isomers a trans-delta-9-THC and a delta-8-THC
bull A cannabidiol (the 2nd most abundant psychoactive ingredient after THC)
bull A cannabinol a decomposition product of THC that accumulates as cannabis samples age
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
THC
bull Variedly aromatic ring (C Ring)
O
O
H
11rsquo-di-methyl-pyrane ring (B ring)
Variedly unsaturated cyclohexyl ring (A ring)
Results of SAR
bull Psychoactive properties are (-) trans-enatioselective
bull Length lipophilicity C3 alkyl chain
bull Phenolic hydroxyl-group
bull C9 substitute
O
O
H
Modes of Absorption
bull The most common method of absorption is smoking Either in a loosely rolled cigarette called a joint or through a pipe or water pipe
Smoking and the Body
THC enters the body through the Lungs
The smoke is inhaled and held in the lungsAll affect how much THC will enter the plasmaTHC crosses the blood barrier through the capillaries in the lungs
After inhalation THC can reach the brain in about 14 seconds
After a 6 min smoking period peak blood levels reached at about 7 min (100 ngml plasma)
Most THC is absorbed from the blood within 30 min
Moves rapidly into the brain and across the bloodbrainplacental barrier Because fatty chains make it very lipid soluble
Half-life is about 19 hours Can store in fat cells
Established physiological effects are dose related
Lethal dose for THC use has now been studied and no human deaths have been reported due to intoxication from cannabis
Metabolites
bull Radioactively labeled delta-9-THC has been found to persist in the body as an active metabolite as long as 8 days after use
Primary metabolite has a half-life of 50 hours The complete elimination of the drug can take as long as 6 weeks
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
23 of metabolites are excreted in feces13 of metabolites are excreted in urine
Cannabis Pharmacology
Primary Cannabinoids from Cannabis are
bull Cannabinol (CBN) Cannabidiol (CBD) and Tetrahydrocannabinol (THC)
bull THC (-9-THC ) is the only one with significant psychoactive properties
bull CBN - 110 th activity of THC CBD - none
bull 2 isomers a trans-delta-9-THC and a delta-8-THC
bull A cannabidiol (the 2nd most abundant psychoactive ingredient after THC)
bull A cannabinol a decomposition product of THC that accumulates as cannabis samples age
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
Therapeutic
bull Antiemeticbull Reduction of intra-ocular tensionbull Analgesicbull Muscle relaxant bull Anti-convulsant bull Anti-inflammatory appetite ldquothe munchiesrdquo It is one of the most well-known effects of marijuana the
powerful surge in appetite many users feel after smoking or ingesting the drug colloquially known as the munchies
Marinol
THC in a sesame oil suspension
Cannabinoid ReceptorsBeforethe 1980s it was often speculated that
cannabinoids produced their effects through non specific interaction with cell membranes instead of interacting with specific receptors
The discovery of the first cannabinoid receptors in the 1980s helped to resolve this debate These receptors are common in animals and have been found in mammals birds fishes and reptiles
There are currently two known types of cannabinoid receptors CB1 and CB2
CB1 ReceptorsFound primarily in the brain (specifically basal ganglia limbic
system including the hippocampus and cerebellum)1048766Most dense in brain regions involved with thinking and memory
attention and control of movement1048766Also present in both male and female reproductive systems as
well as in the lungs liver and kidneys1048766Appear to be responsible for the euphoric and anticonvulsive
effects of Cannabis1048766Essentially absent in the medulla oblongata the part of the brain
that is responsible for respiratory and cardiovascular functions
Thus there is no risk of respiratory or cardiovascular failure as there is with many other drugs
CB2 Receptor
CB2 receptors are almost exclusively found in the immune system (T cells macrophages B cells) with the greatest density in the spleen
1048766CB2 receptors appear to be responsible for the anti-inflammatory and possible other therapeutic effects of Cannabis
1048766Also expressed on peripheral nerve terminals
Cannabis and Δ9- (THC) for weight loss
bull Obesity is one of the highest preventable causes of morbidity and mortality in the developed world It has been well known for a long time that exposure to cannabis produces an increase of appetite (a phenomenon referred to as the munchies) This phenomenon led to an exploration of the role of the endocannabinoid system in the regulation of obesity and associated metabolic syndrome This effort subsequently led to the development of a successful therapeutic approach for obesity that consisted of blocking the cannabinoid CB1 receptors using ligands such as Rimonabant in order to produce weight loss and improve metabolic profile
What is obesity
Obesity is characterized by an abnormal accumulation of body fat usually 20 percent or more over an individuals ideal body weight Obesity results when the size or number of fat cells in a persons body increases When a person gains weight these fat cells first increase in size and later in number When a person starts losing weight the cells decreas ein size but their number generally stays the same This is part of the reason that once you gain a significant amount of weight it is more difficult to lose it
The clinical definition of obesity is a body mass index(BMI)of 30 or higher BMI = Weight (in kg) Height (in meters) Squared
Rimonabant
bull Acompliareg(Sanofi-Aventis)
launched in Europe in 2006 for
oral treatment of obesity at 20 mg
once daily
Selective blocker of central
and peripheral CB1 receptors
It reduces food intake and improves lipid and glucose metabolism
Rimonabant
Despite being efficacious Rimonabant was associated with increased rates of depression and anxiety and therefore removed from the market
- Cannabis
- Slide 2
- Slide 3
- Cannabis spp
- Slide 5
- Slide 6
- Hemp
- What is Marijuana
- Marijuana ndash History of Use
- HempvsMarijuana-1
- HempvsMarijuana-2
- HempvsMarijuana-3
- Cannabis Biology
- Chemical constituents of Cannabis
- What is a cannabinoid
- What are cannabinoids
- Natural cannabinoids
- Slide 18
- Representative cannabinoids
- Slide 20
- Endocannabinoids
- Structure of THC and synthetic analogs
- Slide 23
- Slide 24
- THC
- Results of SAR
- Modes of Absorption
- Smoking and the Body
- Slide 29
- Slide 30
- Metabolites
- Slide 32
- Slide 33
- Cannabis Pharmacology
- Slide 35
- Therapeutic
- Marinol
- Cannabinoid Receptors
- CB1 Receptors
- CB2 Receptor
- Cannabis and Δ9- (THC) for weight loss
- What is obesity
- Slide 43
- Slide 44
- Rimonabant
- Slide 46
- Slide 47
- Slide 48
-
Cannabis sppThere are three species known Cannabis sativa C indica and C rudelarisThe leaves are the most recognisable and well-
known aspect of the cannabis plant Despite the great degree of variation found naturally in local populations of cannabis the leaves do not alter greatly in appearance between varieties
Hemp
What is Marijuana
Marijuana is the dried mix of flowers and leaves form the female Cannabis Sativa plant
Hashish is the resin or sap harvested from the plant
Hashish oil is the essential oil of the female Cannabis Sativa plant
Marijuana ndash History of Use
bull Cannabis ndash native to central Asia
bull Chinese ndash first to use employed for fabric medicines
bull India ndash country where first used for hallucinogenic properties
bull Africa ndash introduced through Arab traders used as medicine
bull Europe ndash became popular in 1800s
bull USA ndash 1900s -- use proscribed outlawed
bull End of 20th century ndash contentious debate regarding merits of legalization
HempvsMarijuana-1
bull The word hempis English for a number of varieties of the Cannabisplant particularly the varieties like industrial hemp that were bred over time for industrial uses such as fuel fiber paper seed food oil etc
HempvsMarijuana-2
bull The term marijuanais of Spanish derivation and was primarily used to describe varieties of Cannabisthat were more commonly bred over time for medicinal and recreational purposes like Cannabisindica and certain strains of Cannabissativa
HempvsMarijuana-3
bull Two cannabinoids are preponderant in Cannabis
bull THC CBDbull psychoactive ingredient antipsychoactive ingredient
Marijuana Hempbull (leaves and flowers of the female plant)
bull High in THC High in CBDbull Low in THCbull Low in CBD
Cannabis BiologyMajor Drug Component ndash delta-trans-tetrahydrocannabinol (THC)
- binds to specific receptors in brain
THC- produced in glands on leaves and flowers
-- female plants produce more glands
-- gland production stimulated by heat sunlight drought
-- sinsemilla (sin = without semilla = seeds) ndash particularly strong
Hashish ndash product - relatively pure resin
Glands THC
Chemical constituents of Cannabis
bull Cannabinoids (66)bull Nitrogenous compounds (27)bull Amino acids(18)bull Proteins enzymes (11)bull Sugars (34)bull Hydrocarbons (50)bull Simple alcohols (7)bull Simple aldehydes (12)bull Simple ketones (13)bull Simple acids (21)bull Fatty acids (22)bull Simple esterslactones (13)bull Steroids (11)bull Terpenes (20)bull Non-cannabinoid phenols (25)bull Flavoroids (21)bull Vitamins (1)bull Pigments (2)bull Elements (9) bull Total known compounds (483)
What is a cannabinoid
bullInitially compounds extracted by Cannabis spp producing characteristic psychoactivity
bullLater compounds with a characteristic terpenoid structure
bullCurrently most any compound that produces cannabinoid psychoactivity natural or synthetic
bullOccasionally just compounds that will interact with cannabinoid receptors
What are cannabinoidsbull Group of gt60 dibenzopyran chemicals found in
leaves and flowering tops of female cannabis plant (Cannabis sativa and Cannabis indica)
bull Some common cannabinoids are
In the plantIn your body (endogenous)
Synthetic
Δ9 ndash THC 2-arichidonyl glycerol (2 ndash AG)
CP 55940
Δ8 ndash THC anandamideHU ndash 210
cannabidiol and cannabinol
Natural cannabinoids
Representative cannabinoids
Classical cannabinoids Non-classical cannabinoid Aminoalkylindole
CB1 antagonists
Endogenous cannabinoids
Receptors suggest endogenous ligandsTwo main families identifiedBoth arachidonic acid derivativesPrecursors in membranes
ldquoMade on demandrdquoAmides (anandamide)
Esters (2-AG)
bull Significant differences
ndash Routes of synthesis ndash Mode of degradation
(FAAH vs MAGL)ndash Efficacy
Endocannabinoids
bull Anandamide (Sanskrit ananda inner bliss) is one endocannabinoid It is found in chocolate (though there is some controversy over whether the small quantity has any effect on the body) It is about as potent as THC
Structure of THC and synthetic analogs
Lipophilic side chain Most potent analog 100s
times more potent than THC
with 4 major cannabinoids in the plant
bull 2 isomers a trans-delta-9-THC and a delta-8-THC
bull A cannabidiol (the 2nd most abundant psychoactive ingredient after THC)
bull A cannabinol a decomposition product of THC that accumulates as cannabis samples age
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
THC
bull Variedly aromatic ring (C Ring)
O
O
H
11rsquo-di-methyl-pyrane ring (B ring)
Variedly unsaturated cyclohexyl ring (A ring)
Results of SAR
bull Psychoactive properties are (-) trans-enatioselective
bull Length lipophilicity C3 alkyl chain
bull Phenolic hydroxyl-group
bull C9 substitute
O
O
H
Modes of Absorption
bull The most common method of absorption is smoking Either in a loosely rolled cigarette called a joint or through a pipe or water pipe
Smoking and the Body
THC enters the body through the Lungs
The smoke is inhaled and held in the lungsAll affect how much THC will enter the plasmaTHC crosses the blood barrier through the capillaries in the lungs
After inhalation THC can reach the brain in about 14 seconds
After a 6 min smoking period peak blood levels reached at about 7 min (100 ngml plasma)
Most THC is absorbed from the blood within 30 min
Moves rapidly into the brain and across the bloodbrainplacental barrier Because fatty chains make it very lipid soluble
Half-life is about 19 hours Can store in fat cells
Established physiological effects are dose related
Lethal dose for THC use has now been studied and no human deaths have been reported due to intoxication from cannabis
Metabolites
bull Radioactively labeled delta-9-THC has been found to persist in the body as an active metabolite as long as 8 days after use
Primary metabolite has a half-life of 50 hours The complete elimination of the drug can take as long as 6 weeks
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
23 of metabolites are excreted in feces13 of metabolites are excreted in urine
Cannabis Pharmacology
Primary Cannabinoids from Cannabis are
bull Cannabinol (CBN) Cannabidiol (CBD) and Tetrahydrocannabinol (THC)
bull THC (-9-THC ) is the only one with significant psychoactive properties
bull CBN - 110 th activity of THC CBD - none
bull 2 isomers a trans-delta-9-THC and a delta-8-THC
bull A cannabidiol (the 2nd most abundant psychoactive ingredient after THC)
bull A cannabinol a decomposition product of THC that accumulates as cannabis samples age
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
Therapeutic
bull Antiemeticbull Reduction of intra-ocular tensionbull Analgesicbull Muscle relaxant bull Anti-convulsant bull Anti-inflammatory appetite ldquothe munchiesrdquo It is one of the most well-known effects of marijuana the
powerful surge in appetite many users feel after smoking or ingesting the drug colloquially known as the munchies
Marinol
THC in a sesame oil suspension
Cannabinoid ReceptorsBeforethe 1980s it was often speculated that
cannabinoids produced their effects through non specific interaction with cell membranes instead of interacting with specific receptors
The discovery of the first cannabinoid receptors in the 1980s helped to resolve this debate These receptors are common in animals and have been found in mammals birds fishes and reptiles
There are currently two known types of cannabinoid receptors CB1 and CB2
CB1 ReceptorsFound primarily in the brain (specifically basal ganglia limbic
system including the hippocampus and cerebellum)1048766Most dense in brain regions involved with thinking and memory
attention and control of movement1048766Also present in both male and female reproductive systems as
well as in the lungs liver and kidneys1048766Appear to be responsible for the euphoric and anticonvulsive
effects of Cannabis1048766Essentially absent in the medulla oblongata the part of the brain
that is responsible for respiratory and cardiovascular functions
Thus there is no risk of respiratory or cardiovascular failure as there is with many other drugs
CB2 Receptor
CB2 receptors are almost exclusively found in the immune system (T cells macrophages B cells) with the greatest density in the spleen
1048766CB2 receptors appear to be responsible for the anti-inflammatory and possible other therapeutic effects of Cannabis
1048766Also expressed on peripheral nerve terminals
Cannabis and Δ9- (THC) for weight loss
bull Obesity is one of the highest preventable causes of morbidity and mortality in the developed world It has been well known for a long time that exposure to cannabis produces an increase of appetite (a phenomenon referred to as the munchies) This phenomenon led to an exploration of the role of the endocannabinoid system in the regulation of obesity and associated metabolic syndrome This effort subsequently led to the development of a successful therapeutic approach for obesity that consisted of blocking the cannabinoid CB1 receptors using ligands such as Rimonabant in order to produce weight loss and improve metabolic profile
What is obesity
Obesity is characterized by an abnormal accumulation of body fat usually 20 percent or more over an individuals ideal body weight Obesity results when the size or number of fat cells in a persons body increases When a person gains weight these fat cells first increase in size and later in number When a person starts losing weight the cells decreas ein size but their number generally stays the same This is part of the reason that once you gain a significant amount of weight it is more difficult to lose it
The clinical definition of obesity is a body mass index(BMI)of 30 or higher BMI = Weight (in kg) Height (in meters) Squared
Rimonabant
bull Acompliareg(Sanofi-Aventis)
launched in Europe in 2006 for
oral treatment of obesity at 20 mg
once daily
Selective blocker of central
and peripheral CB1 receptors
It reduces food intake and improves lipid and glucose metabolism
Rimonabant
Despite being efficacious Rimonabant was associated with increased rates of depression and anxiety and therefore removed from the market
- Cannabis
- Slide 2
- Slide 3
- Cannabis spp
- Slide 5
- Slide 6
- Hemp
- What is Marijuana
- Marijuana ndash History of Use
- HempvsMarijuana-1
- HempvsMarijuana-2
- HempvsMarijuana-3
- Cannabis Biology
- Chemical constituents of Cannabis
- What is a cannabinoid
- What are cannabinoids
- Natural cannabinoids
- Slide 18
- Representative cannabinoids
- Slide 20
- Endocannabinoids
- Structure of THC and synthetic analogs
- Slide 23
- Slide 24
- THC
- Results of SAR
- Modes of Absorption
- Smoking and the Body
- Slide 29
- Slide 30
- Metabolites
- Slide 32
- Slide 33
- Cannabis Pharmacology
- Slide 35
- Therapeutic
- Marinol
- Cannabinoid Receptors
- CB1 Receptors
- CB2 Receptor
- Cannabis and Δ9- (THC) for weight loss
- What is obesity
- Slide 43
- Slide 44
- Rimonabant
- Slide 46
- Slide 47
- Slide 48
-
Hemp
What is Marijuana
Marijuana is the dried mix of flowers and leaves form the female Cannabis Sativa plant
Hashish is the resin or sap harvested from the plant
Hashish oil is the essential oil of the female Cannabis Sativa plant
Marijuana ndash History of Use
bull Cannabis ndash native to central Asia
bull Chinese ndash first to use employed for fabric medicines
bull India ndash country where first used for hallucinogenic properties
bull Africa ndash introduced through Arab traders used as medicine
bull Europe ndash became popular in 1800s
bull USA ndash 1900s -- use proscribed outlawed
bull End of 20th century ndash contentious debate regarding merits of legalization
HempvsMarijuana-1
bull The word hempis English for a number of varieties of the Cannabisplant particularly the varieties like industrial hemp that were bred over time for industrial uses such as fuel fiber paper seed food oil etc
HempvsMarijuana-2
bull The term marijuanais of Spanish derivation and was primarily used to describe varieties of Cannabisthat were more commonly bred over time for medicinal and recreational purposes like Cannabisindica and certain strains of Cannabissativa
HempvsMarijuana-3
bull Two cannabinoids are preponderant in Cannabis
bull THC CBDbull psychoactive ingredient antipsychoactive ingredient
Marijuana Hempbull (leaves and flowers of the female plant)
bull High in THC High in CBDbull Low in THCbull Low in CBD
Cannabis BiologyMajor Drug Component ndash delta-trans-tetrahydrocannabinol (THC)
- binds to specific receptors in brain
THC- produced in glands on leaves and flowers
-- female plants produce more glands
-- gland production stimulated by heat sunlight drought
-- sinsemilla (sin = without semilla = seeds) ndash particularly strong
Hashish ndash product - relatively pure resin
Glands THC
Chemical constituents of Cannabis
bull Cannabinoids (66)bull Nitrogenous compounds (27)bull Amino acids(18)bull Proteins enzymes (11)bull Sugars (34)bull Hydrocarbons (50)bull Simple alcohols (7)bull Simple aldehydes (12)bull Simple ketones (13)bull Simple acids (21)bull Fatty acids (22)bull Simple esterslactones (13)bull Steroids (11)bull Terpenes (20)bull Non-cannabinoid phenols (25)bull Flavoroids (21)bull Vitamins (1)bull Pigments (2)bull Elements (9) bull Total known compounds (483)
What is a cannabinoid
bullInitially compounds extracted by Cannabis spp producing characteristic psychoactivity
bullLater compounds with a characteristic terpenoid structure
bullCurrently most any compound that produces cannabinoid psychoactivity natural or synthetic
bullOccasionally just compounds that will interact with cannabinoid receptors
What are cannabinoidsbull Group of gt60 dibenzopyran chemicals found in
leaves and flowering tops of female cannabis plant (Cannabis sativa and Cannabis indica)
bull Some common cannabinoids are
In the plantIn your body (endogenous)
Synthetic
Δ9 ndash THC 2-arichidonyl glycerol (2 ndash AG)
CP 55940
Δ8 ndash THC anandamideHU ndash 210
cannabidiol and cannabinol
Natural cannabinoids
Representative cannabinoids
Classical cannabinoids Non-classical cannabinoid Aminoalkylindole
CB1 antagonists
Endogenous cannabinoids
Receptors suggest endogenous ligandsTwo main families identifiedBoth arachidonic acid derivativesPrecursors in membranes
ldquoMade on demandrdquoAmides (anandamide)
Esters (2-AG)
bull Significant differences
ndash Routes of synthesis ndash Mode of degradation
(FAAH vs MAGL)ndash Efficacy
Endocannabinoids
bull Anandamide (Sanskrit ananda inner bliss) is one endocannabinoid It is found in chocolate (though there is some controversy over whether the small quantity has any effect on the body) It is about as potent as THC
Structure of THC and synthetic analogs
Lipophilic side chain Most potent analog 100s
times more potent than THC
with 4 major cannabinoids in the plant
bull 2 isomers a trans-delta-9-THC and a delta-8-THC
bull A cannabidiol (the 2nd most abundant psychoactive ingredient after THC)
bull A cannabinol a decomposition product of THC that accumulates as cannabis samples age
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
THC
bull Variedly aromatic ring (C Ring)
O
O
H
11rsquo-di-methyl-pyrane ring (B ring)
Variedly unsaturated cyclohexyl ring (A ring)
Results of SAR
bull Psychoactive properties are (-) trans-enatioselective
bull Length lipophilicity C3 alkyl chain
bull Phenolic hydroxyl-group
bull C9 substitute
O
O
H
Modes of Absorption
bull The most common method of absorption is smoking Either in a loosely rolled cigarette called a joint or through a pipe or water pipe
Smoking and the Body
THC enters the body through the Lungs
The smoke is inhaled and held in the lungsAll affect how much THC will enter the plasmaTHC crosses the blood barrier through the capillaries in the lungs
After inhalation THC can reach the brain in about 14 seconds
After a 6 min smoking period peak blood levels reached at about 7 min (100 ngml plasma)
Most THC is absorbed from the blood within 30 min
Moves rapidly into the brain and across the bloodbrainplacental barrier Because fatty chains make it very lipid soluble
Half-life is about 19 hours Can store in fat cells
Established physiological effects are dose related
Lethal dose for THC use has now been studied and no human deaths have been reported due to intoxication from cannabis
Metabolites
bull Radioactively labeled delta-9-THC has been found to persist in the body as an active metabolite as long as 8 days after use
Primary metabolite has a half-life of 50 hours The complete elimination of the drug can take as long as 6 weeks
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
23 of metabolites are excreted in feces13 of metabolites are excreted in urine
Cannabis Pharmacology
Primary Cannabinoids from Cannabis are
bull Cannabinol (CBN) Cannabidiol (CBD) and Tetrahydrocannabinol (THC)
bull THC (-9-THC ) is the only one with significant psychoactive properties
bull CBN - 110 th activity of THC CBD - none
bull 2 isomers a trans-delta-9-THC and a delta-8-THC
bull A cannabidiol (the 2nd most abundant psychoactive ingredient after THC)
bull A cannabinol a decomposition product of THC that accumulates as cannabis samples age
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
Therapeutic
bull Antiemeticbull Reduction of intra-ocular tensionbull Analgesicbull Muscle relaxant bull Anti-convulsant bull Anti-inflammatory appetite ldquothe munchiesrdquo It is one of the most well-known effects of marijuana the
powerful surge in appetite many users feel after smoking or ingesting the drug colloquially known as the munchies
Marinol
THC in a sesame oil suspension
Cannabinoid ReceptorsBeforethe 1980s it was often speculated that
cannabinoids produced their effects through non specific interaction with cell membranes instead of interacting with specific receptors
The discovery of the first cannabinoid receptors in the 1980s helped to resolve this debate These receptors are common in animals and have been found in mammals birds fishes and reptiles
There are currently two known types of cannabinoid receptors CB1 and CB2
CB1 ReceptorsFound primarily in the brain (specifically basal ganglia limbic
system including the hippocampus and cerebellum)1048766Most dense in brain regions involved with thinking and memory
attention and control of movement1048766Also present in both male and female reproductive systems as
well as in the lungs liver and kidneys1048766Appear to be responsible for the euphoric and anticonvulsive
effects of Cannabis1048766Essentially absent in the medulla oblongata the part of the brain
that is responsible for respiratory and cardiovascular functions
Thus there is no risk of respiratory or cardiovascular failure as there is with many other drugs
CB2 Receptor
CB2 receptors are almost exclusively found in the immune system (T cells macrophages B cells) with the greatest density in the spleen
1048766CB2 receptors appear to be responsible for the anti-inflammatory and possible other therapeutic effects of Cannabis
1048766Also expressed on peripheral nerve terminals
Cannabis and Δ9- (THC) for weight loss
bull Obesity is one of the highest preventable causes of morbidity and mortality in the developed world It has been well known for a long time that exposure to cannabis produces an increase of appetite (a phenomenon referred to as the munchies) This phenomenon led to an exploration of the role of the endocannabinoid system in the regulation of obesity and associated metabolic syndrome This effort subsequently led to the development of a successful therapeutic approach for obesity that consisted of blocking the cannabinoid CB1 receptors using ligands such as Rimonabant in order to produce weight loss and improve metabolic profile
What is obesity
Obesity is characterized by an abnormal accumulation of body fat usually 20 percent or more over an individuals ideal body weight Obesity results when the size or number of fat cells in a persons body increases When a person gains weight these fat cells first increase in size and later in number When a person starts losing weight the cells decreas ein size but their number generally stays the same This is part of the reason that once you gain a significant amount of weight it is more difficult to lose it
The clinical definition of obesity is a body mass index(BMI)of 30 or higher BMI = Weight (in kg) Height (in meters) Squared
Rimonabant
bull Acompliareg(Sanofi-Aventis)
launched in Europe in 2006 for
oral treatment of obesity at 20 mg
once daily
Selective blocker of central
and peripheral CB1 receptors
It reduces food intake and improves lipid and glucose metabolism
Rimonabant
Despite being efficacious Rimonabant was associated with increased rates of depression and anxiety and therefore removed from the market
- Cannabis
- Slide 2
- Slide 3
- Cannabis spp
- Slide 5
- Slide 6
- Hemp
- What is Marijuana
- Marijuana ndash History of Use
- HempvsMarijuana-1
- HempvsMarijuana-2
- HempvsMarijuana-3
- Cannabis Biology
- Chemical constituents of Cannabis
- What is a cannabinoid
- What are cannabinoids
- Natural cannabinoids
- Slide 18
- Representative cannabinoids
- Slide 20
- Endocannabinoids
- Structure of THC and synthetic analogs
- Slide 23
- Slide 24
- THC
- Results of SAR
- Modes of Absorption
- Smoking and the Body
- Slide 29
- Slide 30
- Metabolites
- Slide 32
- Slide 33
- Cannabis Pharmacology
- Slide 35
- Therapeutic
- Marinol
- Cannabinoid Receptors
- CB1 Receptors
- CB2 Receptor
- Cannabis and Δ9- (THC) for weight loss
- What is obesity
- Slide 43
- Slide 44
- Rimonabant
- Slide 46
- Slide 47
- Slide 48
-
What is Marijuana
Marijuana is the dried mix of flowers and leaves form the female Cannabis Sativa plant
Hashish is the resin or sap harvested from the plant
Hashish oil is the essential oil of the female Cannabis Sativa plant
Marijuana ndash History of Use
bull Cannabis ndash native to central Asia
bull Chinese ndash first to use employed for fabric medicines
bull India ndash country where first used for hallucinogenic properties
bull Africa ndash introduced through Arab traders used as medicine
bull Europe ndash became popular in 1800s
bull USA ndash 1900s -- use proscribed outlawed
bull End of 20th century ndash contentious debate regarding merits of legalization
HempvsMarijuana-1
bull The word hempis English for a number of varieties of the Cannabisplant particularly the varieties like industrial hemp that were bred over time for industrial uses such as fuel fiber paper seed food oil etc
HempvsMarijuana-2
bull The term marijuanais of Spanish derivation and was primarily used to describe varieties of Cannabisthat were more commonly bred over time for medicinal and recreational purposes like Cannabisindica and certain strains of Cannabissativa
HempvsMarijuana-3
bull Two cannabinoids are preponderant in Cannabis
bull THC CBDbull psychoactive ingredient antipsychoactive ingredient
Marijuana Hempbull (leaves and flowers of the female plant)
bull High in THC High in CBDbull Low in THCbull Low in CBD
Cannabis BiologyMajor Drug Component ndash delta-trans-tetrahydrocannabinol (THC)
- binds to specific receptors in brain
THC- produced in glands on leaves and flowers
-- female plants produce more glands
-- gland production stimulated by heat sunlight drought
-- sinsemilla (sin = without semilla = seeds) ndash particularly strong
Hashish ndash product - relatively pure resin
Glands THC
Chemical constituents of Cannabis
bull Cannabinoids (66)bull Nitrogenous compounds (27)bull Amino acids(18)bull Proteins enzymes (11)bull Sugars (34)bull Hydrocarbons (50)bull Simple alcohols (7)bull Simple aldehydes (12)bull Simple ketones (13)bull Simple acids (21)bull Fatty acids (22)bull Simple esterslactones (13)bull Steroids (11)bull Terpenes (20)bull Non-cannabinoid phenols (25)bull Flavoroids (21)bull Vitamins (1)bull Pigments (2)bull Elements (9) bull Total known compounds (483)
What is a cannabinoid
bullInitially compounds extracted by Cannabis spp producing characteristic psychoactivity
bullLater compounds with a characteristic terpenoid structure
bullCurrently most any compound that produces cannabinoid psychoactivity natural or synthetic
bullOccasionally just compounds that will interact with cannabinoid receptors
What are cannabinoidsbull Group of gt60 dibenzopyran chemicals found in
leaves and flowering tops of female cannabis plant (Cannabis sativa and Cannabis indica)
bull Some common cannabinoids are
In the plantIn your body (endogenous)
Synthetic
Δ9 ndash THC 2-arichidonyl glycerol (2 ndash AG)
CP 55940
Δ8 ndash THC anandamideHU ndash 210
cannabidiol and cannabinol
Natural cannabinoids
Representative cannabinoids
Classical cannabinoids Non-classical cannabinoid Aminoalkylindole
CB1 antagonists
Endogenous cannabinoids
Receptors suggest endogenous ligandsTwo main families identifiedBoth arachidonic acid derivativesPrecursors in membranes
ldquoMade on demandrdquoAmides (anandamide)
Esters (2-AG)
bull Significant differences
ndash Routes of synthesis ndash Mode of degradation
(FAAH vs MAGL)ndash Efficacy
Endocannabinoids
bull Anandamide (Sanskrit ananda inner bliss) is one endocannabinoid It is found in chocolate (though there is some controversy over whether the small quantity has any effect on the body) It is about as potent as THC
Structure of THC and synthetic analogs
Lipophilic side chain Most potent analog 100s
times more potent than THC
with 4 major cannabinoids in the plant
bull 2 isomers a trans-delta-9-THC and a delta-8-THC
bull A cannabidiol (the 2nd most abundant psychoactive ingredient after THC)
bull A cannabinol a decomposition product of THC that accumulates as cannabis samples age
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
THC
bull Variedly aromatic ring (C Ring)
O
O
H
11rsquo-di-methyl-pyrane ring (B ring)
Variedly unsaturated cyclohexyl ring (A ring)
Results of SAR
bull Psychoactive properties are (-) trans-enatioselective
bull Length lipophilicity C3 alkyl chain
bull Phenolic hydroxyl-group
bull C9 substitute
O
O
H
Modes of Absorption
bull The most common method of absorption is smoking Either in a loosely rolled cigarette called a joint or through a pipe or water pipe
Smoking and the Body
THC enters the body through the Lungs
The smoke is inhaled and held in the lungsAll affect how much THC will enter the plasmaTHC crosses the blood barrier through the capillaries in the lungs
After inhalation THC can reach the brain in about 14 seconds
After a 6 min smoking period peak blood levels reached at about 7 min (100 ngml plasma)
Most THC is absorbed from the blood within 30 min
Moves rapidly into the brain and across the bloodbrainplacental barrier Because fatty chains make it very lipid soluble
Half-life is about 19 hours Can store in fat cells
Established physiological effects are dose related
Lethal dose for THC use has now been studied and no human deaths have been reported due to intoxication from cannabis
Metabolites
bull Radioactively labeled delta-9-THC has been found to persist in the body as an active metabolite as long as 8 days after use
Primary metabolite has a half-life of 50 hours The complete elimination of the drug can take as long as 6 weeks
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
23 of metabolites are excreted in feces13 of metabolites are excreted in urine
Cannabis Pharmacology
Primary Cannabinoids from Cannabis are
bull Cannabinol (CBN) Cannabidiol (CBD) and Tetrahydrocannabinol (THC)
bull THC (-9-THC ) is the only one with significant psychoactive properties
bull CBN - 110 th activity of THC CBD - none
bull 2 isomers a trans-delta-9-THC and a delta-8-THC
bull A cannabidiol (the 2nd most abundant psychoactive ingredient after THC)
bull A cannabinol a decomposition product of THC that accumulates as cannabis samples age
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
Therapeutic
bull Antiemeticbull Reduction of intra-ocular tensionbull Analgesicbull Muscle relaxant bull Anti-convulsant bull Anti-inflammatory appetite ldquothe munchiesrdquo It is one of the most well-known effects of marijuana the
powerful surge in appetite many users feel after smoking or ingesting the drug colloquially known as the munchies
Marinol
THC in a sesame oil suspension
Cannabinoid ReceptorsBeforethe 1980s it was often speculated that
cannabinoids produced their effects through non specific interaction with cell membranes instead of interacting with specific receptors
The discovery of the first cannabinoid receptors in the 1980s helped to resolve this debate These receptors are common in animals and have been found in mammals birds fishes and reptiles
There are currently two known types of cannabinoid receptors CB1 and CB2
CB1 ReceptorsFound primarily in the brain (specifically basal ganglia limbic
system including the hippocampus and cerebellum)1048766Most dense in brain regions involved with thinking and memory
attention and control of movement1048766Also present in both male and female reproductive systems as
well as in the lungs liver and kidneys1048766Appear to be responsible for the euphoric and anticonvulsive
effects of Cannabis1048766Essentially absent in the medulla oblongata the part of the brain
that is responsible for respiratory and cardiovascular functions
Thus there is no risk of respiratory or cardiovascular failure as there is with many other drugs
CB2 Receptor
CB2 receptors are almost exclusively found in the immune system (T cells macrophages B cells) with the greatest density in the spleen
1048766CB2 receptors appear to be responsible for the anti-inflammatory and possible other therapeutic effects of Cannabis
1048766Also expressed on peripheral nerve terminals
Cannabis and Δ9- (THC) for weight loss
bull Obesity is one of the highest preventable causes of morbidity and mortality in the developed world It has been well known for a long time that exposure to cannabis produces an increase of appetite (a phenomenon referred to as the munchies) This phenomenon led to an exploration of the role of the endocannabinoid system in the regulation of obesity and associated metabolic syndrome This effort subsequently led to the development of a successful therapeutic approach for obesity that consisted of blocking the cannabinoid CB1 receptors using ligands such as Rimonabant in order to produce weight loss and improve metabolic profile
What is obesity
Obesity is characterized by an abnormal accumulation of body fat usually 20 percent or more over an individuals ideal body weight Obesity results when the size or number of fat cells in a persons body increases When a person gains weight these fat cells first increase in size and later in number When a person starts losing weight the cells decreas ein size but their number generally stays the same This is part of the reason that once you gain a significant amount of weight it is more difficult to lose it
The clinical definition of obesity is a body mass index(BMI)of 30 or higher BMI = Weight (in kg) Height (in meters) Squared
Rimonabant
bull Acompliareg(Sanofi-Aventis)
launched in Europe in 2006 for
oral treatment of obesity at 20 mg
once daily
Selective blocker of central
and peripheral CB1 receptors
It reduces food intake and improves lipid and glucose metabolism
Rimonabant
Despite being efficacious Rimonabant was associated with increased rates of depression and anxiety and therefore removed from the market
- Cannabis
- Slide 2
- Slide 3
- Cannabis spp
- Slide 5
- Slide 6
- Hemp
- What is Marijuana
- Marijuana ndash History of Use
- HempvsMarijuana-1
- HempvsMarijuana-2
- HempvsMarijuana-3
- Cannabis Biology
- Chemical constituents of Cannabis
- What is a cannabinoid
- What are cannabinoids
- Natural cannabinoids
- Slide 18
- Representative cannabinoids
- Slide 20
- Endocannabinoids
- Structure of THC and synthetic analogs
- Slide 23
- Slide 24
- THC
- Results of SAR
- Modes of Absorption
- Smoking and the Body
- Slide 29
- Slide 30
- Metabolites
- Slide 32
- Slide 33
- Cannabis Pharmacology
- Slide 35
- Therapeutic
- Marinol
- Cannabinoid Receptors
- CB1 Receptors
- CB2 Receptor
- Cannabis and Δ9- (THC) for weight loss
- What is obesity
- Slide 43
- Slide 44
- Rimonabant
- Slide 46
- Slide 47
- Slide 48
-
Marijuana ndash History of Use
bull Cannabis ndash native to central Asia
bull Chinese ndash first to use employed for fabric medicines
bull India ndash country where first used for hallucinogenic properties
bull Africa ndash introduced through Arab traders used as medicine
bull Europe ndash became popular in 1800s
bull USA ndash 1900s -- use proscribed outlawed
bull End of 20th century ndash contentious debate regarding merits of legalization
HempvsMarijuana-1
bull The word hempis English for a number of varieties of the Cannabisplant particularly the varieties like industrial hemp that were bred over time for industrial uses such as fuel fiber paper seed food oil etc
HempvsMarijuana-2
bull The term marijuanais of Spanish derivation and was primarily used to describe varieties of Cannabisthat were more commonly bred over time for medicinal and recreational purposes like Cannabisindica and certain strains of Cannabissativa
HempvsMarijuana-3
bull Two cannabinoids are preponderant in Cannabis
bull THC CBDbull psychoactive ingredient antipsychoactive ingredient
Marijuana Hempbull (leaves and flowers of the female plant)
bull High in THC High in CBDbull Low in THCbull Low in CBD
Cannabis BiologyMajor Drug Component ndash delta-trans-tetrahydrocannabinol (THC)
- binds to specific receptors in brain
THC- produced in glands on leaves and flowers
-- female plants produce more glands
-- gland production stimulated by heat sunlight drought
-- sinsemilla (sin = without semilla = seeds) ndash particularly strong
Hashish ndash product - relatively pure resin
Glands THC
Chemical constituents of Cannabis
bull Cannabinoids (66)bull Nitrogenous compounds (27)bull Amino acids(18)bull Proteins enzymes (11)bull Sugars (34)bull Hydrocarbons (50)bull Simple alcohols (7)bull Simple aldehydes (12)bull Simple ketones (13)bull Simple acids (21)bull Fatty acids (22)bull Simple esterslactones (13)bull Steroids (11)bull Terpenes (20)bull Non-cannabinoid phenols (25)bull Flavoroids (21)bull Vitamins (1)bull Pigments (2)bull Elements (9) bull Total known compounds (483)
What is a cannabinoid
bullInitially compounds extracted by Cannabis spp producing characteristic psychoactivity
bullLater compounds with a characteristic terpenoid structure
bullCurrently most any compound that produces cannabinoid psychoactivity natural or synthetic
bullOccasionally just compounds that will interact with cannabinoid receptors
What are cannabinoidsbull Group of gt60 dibenzopyran chemicals found in
leaves and flowering tops of female cannabis plant (Cannabis sativa and Cannabis indica)
bull Some common cannabinoids are
In the plantIn your body (endogenous)
Synthetic
Δ9 ndash THC 2-arichidonyl glycerol (2 ndash AG)
CP 55940
Δ8 ndash THC anandamideHU ndash 210
cannabidiol and cannabinol
Natural cannabinoids
Representative cannabinoids
Classical cannabinoids Non-classical cannabinoid Aminoalkylindole
CB1 antagonists
Endogenous cannabinoids
Receptors suggest endogenous ligandsTwo main families identifiedBoth arachidonic acid derivativesPrecursors in membranes
ldquoMade on demandrdquoAmides (anandamide)
Esters (2-AG)
bull Significant differences
ndash Routes of synthesis ndash Mode of degradation
(FAAH vs MAGL)ndash Efficacy
Endocannabinoids
bull Anandamide (Sanskrit ananda inner bliss) is one endocannabinoid It is found in chocolate (though there is some controversy over whether the small quantity has any effect on the body) It is about as potent as THC
Structure of THC and synthetic analogs
Lipophilic side chain Most potent analog 100s
times more potent than THC
with 4 major cannabinoids in the plant
bull 2 isomers a trans-delta-9-THC and a delta-8-THC
bull A cannabidiol (the 2nd most abundant psychoactive ingredient after THC)
bull A cannabinol a decomposition product of THC that accumulates as cannabis samples age
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
THC
bull Variedly aromatic ring (C Ring)
O
O
H
11rsquo-di-methyl-pyrane ring (B ring)
Variedly unsaturated cyclohexyl ring (A ring)
Results of SAR
bull Psychoactive properties are (-) trans-enatioselective
bull Length lipophilicity C3 alkyl chain
bull Phenolic hydroxyl-group
bull C9 substitute
O
O
H
Modes of Absorption
bull The most common method of absorption is smoking Either in a loosely rolled cigarette called a joint or through a pipe or water pipe
Smoking and the Body
THC enters the body through the Lungs
The smoke is inhaled and held in the lungsAll affect how much THC will enter the plasmaTHC crosses the blood barrier through the capillaries in the lungs
After inhalation THC can reach the brain in about 14 seconds
After a 6 min smoking period peak blood levels reached at about 7 min (100 ngml plasma)
Most THC is absorbed from the blood within 30 min
Moves rapidly into the brain and across the bloodbrainplacental barrier Because fatty chains make it very lipid soluble
Half-life is about 19 hours Can store in fat cells
Established physiological effects are dose related
Lethal dose for THC use has now been studied and no human deaths have been reported due to intoxication from cannabis
Metabolites
bull Radioactively labeled delta-9-THC has been found to persist in the body as an active metabolite as long as 8 days after use
Primary metabolite has a half-life of 50 hours The complete elimination of the drug can take as long as 6 weeks
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
23 of metabolites are excreted in feces13 of metabolites are excreted in urine
Cannabis Pharmacology
Primary Cannabinoids from Cannabis are
bull Cannabinol (CBN) Cannabidiol (CBD) and Tetrahydrocannabinol (THC)
bull THC (-9-THC ) is the only one with significant psychoactive properties
bull CBN - 110 th activity of THC CBD - none
bull 2 isomers a trans-delta-9-THC and a delta-8-THC
bull A cannabidiol (the 2nd most abundant psychoactive ingredient after THC)
bull A cannabinol a decomposition product of THC that accumulates as cannabis samples age
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
Therapeutic
bull Antiemeticbull Reduction of intra-ocular tensionbull Analgesicbull Muscle relaxant bull Anti-convulsant bull Anti-inflammatory appetite ldquothe munchiesrdquo It is one of the most well-known effects of marijuana the
powerful surge in appetite many users feel after smoking or ingesting the drug colloquially known as the munchies
Marinol
THC in a sesame oil suspension
Cannabinoid ReceptorsBeforethe 1980s it was often speculated that
cannabinoids produced their effects through non specific interaction with cell membranes instead of interacting with specific receptors
The discovery of the first cannabinoid receptors in the 1980s helped to resolve this debate These receptors are common in animals and have been found in mammals birds fishes and reptiles
There are currently two known types of cannabinoid receptors CB1 and CB2
CB1 ReceptorsFound primarily in the brain (specifically basal ganglia limbic
system including the hippocampus and cerebellum)1048766Most dense in brain regions involved with thinking and memory
attention and control of movement1048766Also present in both male and female reproductive systems as
well as in the lungs liver and kidneys1048766Appear to be responsible for the euphoric and anticonvulsive
effects of Cannabis1048766Essentially absent in the medulla oblongata the part of the brain
that is responsible for respiratory and cardiovascular functions
Thus there is no risk of respiratory or cardiovascular failure as there is with many other drugs
CB2 Receptor
CB2 receptors are almost exclusively found in the immune system (T cells macrophages B cells) with the greatest density in the spleen
1048766CB2 receptors appear to be responsible for the anti-inflammatory and possible other therapeutic effects of Cannabis
1048766Also expressed on peripheral nerve terminals
Cannabis and Δ9- (THC) for weight loss
bull Obesity is one of the highest preventable causes of morbidity and mortality in the developed world It has been well known for a long time that exposure to cannabis produces an increase of appetite (a phenomenon referred to as the munchies) This phenomenon led to an exploration of the role of the endocannabinoid system in the regulation of obesity and associated metabolic syndrome This effort subsequently led to the development of a successful therapeutic approach for obesity that consisted of blocking the cannabinoid CB1 receptors using ligands such as Rimonabant in order to produce weight loss and improve metabolic profile
What is obesity
Obesity is characterized by an abnormal accumulation of body fat usually 20 percent or more over an individuals ideal body weight Obesity results when the size or number of fat cells in a persons body increases When a person gains weight these fat cells first increase in size and later in number When a person starts losing weight the cells decreas ein size but their number generally stays the same This is part of the reason that once you gain a significant amount of weight it is more difficult to lose it
The clinical definition of obesity is a body mass index(BMI)of 30 or higher BMI = Weight (in kg) Height (in meters) Squared
Rimonabant
bull Acompliareg(Sanofi-Aventis)
launched in Europe in 2006 for
oral treatment of obesity at 20 mg
once daily
Selective blocker of central
and peripheral CB1 receptors
It reduces food intake and improves lipid and glucose metabolism
Rimonabant
Despite being efficacious Rimonabant was associated with increased rates of depression and anxiety and therefore removed from the market
- Cannabis
- Slide 2
- Slide 3
- Cannabis spp
- Slide 5
- Slide 6
- Hemp
- What is Marijuana
- Marijuana ndash History of Use
- HempvsMarijuana-1
- HempvsMarijuana-2
- HempvsMarijuana-3
- Cannabis Biology
- Chemical constituents of Cannabis
- What is a cannabinoid
- What are cannabinoids
- Natural cannabinoids
- Slide 18
- Representative cannabinoids
- Slide 20
- Endocannabinoids
- Structure of THC and synthetic analogs
- Slide 23
- Slide 24
- THC
- Results of SAR
- Modes of Absorption
- Smoking and the Body
- Slide 29
- Slide 30
- Metabolites
- Slide 32
- Slide 33
- Cannabis Pharmacology
- Slide 35
- Therapeutic
- Marinol
- Cannabinoid Receptors
- CB1 Receptors
- CB2 Receptor
- Cannabis and Δ9- (THC) for weight loss
- What is obesity
- Slide 43
- Slide 44
- Rimonabant
- Slide 46
- Slide 47
- Slide 48
-
HempvsMarijuana-1
bull The word hempis English for a number of varieties of the Cannabisplant particularly the varieties like industrial hemp that were bred over time for industrial uses such as fuel fiber paper seed food oil etc
HempvsMarijuana-2
bull The term marijuanais of Spanish derivation and was primarily used to describe varieties of Cannabisthat were more commonly bred over time for medicinal and recreational purposes like Cannabisindica and certain strains of Cannabissativa
HempvsMarijuana-3
bull Two cannabinoids are preponderant in Cannabis
bull THC CBDbull psychoactive ingredient antipsychoactive ingredient
Marijuana Hempbull (leaves and flowers of the female plant)
bull High in THC High in CBDbull Low in THCbull Low in CBD
Cannabis BiologyMajor Drug Component ndash delta-trans-tetrahydrocannabinol (THC)
- binds to specific receptors in brain
THC- produced in glands on leaves and flowers
-- female plants produce more glands
-- gland production stimulated by heat sunlight drought
-- sinsemilla (sin = without semilla = seeds) ndash particularly strong
Hashish ndash product - relatively pure resin
Glands THC
Chemical constituents of Cannabis
bull Cannabinoids (66)bull Nitrogenous compounds (27)bull Amino acids(18)bull Proteins enzymes (11)bull Sugars (34)bull Hydrocarbons (50)bull Simple alcohols (7)bull Simple aldehydes (12)bull Simple ketones (13)bull Simple acids (21)bull Fatty acids (22)bull Simple esterslactones (13)bull Steroids (11)bull Terpenes (20)bull Non-cannabinoid phenols (25)bull Flavoroids (21)bull Vitamins (1)bull Pigments (2)bull Elements (9) bull Total known compounds (483)
What is a cannabinoid
bullInitially compounds extracted by Cannabis spp producing characteristic psychoactivity
bullLater compounds with a characteristic terpenoid structure
bullCurrently most any compound that produces cannabinoid psychoactivity natural or synthetic
bullOccasionally just compounds that will interact with cannabinoid receptors
What are cannabinoidsbull Group of gt60 dibenzopyran chemicals found in
leaves and flowering tops of female cannabis plant (Cannabis sativa and Cannabis indica)
bull Some common cannabinoids are
In the plantIn your body (endogenous)
Synthetic
Δ9 ndash THC 2-arichidonyl glycerol (2 ndash AG)
CP 55940
Δ8 ndash THC anandamideHU ndash 210
cannabidiol and cannabinol
Natural cannabinoids
Representative cannabinoids
Classical cannabinoids Non-classical cannabinoid Aminoalkylindole
CB1 antagonists
Endogenous cannabinoids
Receptors suggest endogenous ligandsTwo main families identifiedBoth arachidonic acid derivativesPrecursors in membranes
ldquoMade on demandrdquoAmides (anandamide)
Esters (2-AG)
bull Significant differences
ndash Routes of synthesis ndash Mode of degradation
(FAAH vs MAGL)ndash Efficacy
Endocannabinoids
bull Anandamide (Sanskrit ananda inner bliss) is one endocannabinoid It is found in chocolate (though there is some controversy over whether the small quantity has any effect on the body) It is about as potent as THC
Structure of THC and synthetic analogs
Lipophilic side chain Most potent analog 100s
times more potent than THC
with 4 major cannabinoids in the plant
bull 2 isomers a trans-delta-9-THC and a delta-8-THC
bull A cannabidiol (the 2nd most abundant psychoactive ingredient after THC)
bull A cannabinol a decomposition product of THC that accumulates as cannabis samples age
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
THC
bull Variedly aromatic ring (C Ring)
O
O
H
11rsquo-di-methyl-pyrane ring (B ring)
Variedly unsaturated cyclohexyl ring (A ring)
Results of SAR
bull Psychoactive properties are (-) trans-enatioselective
bull Length lipophilicity C3 alkyl chain
bull Phenolic hydroxyl-group
bull C9 substitute
O
O
H
Modes of Absorption
bull The most common method of absorption is smoking Either in a loosely rolled cigarette called a joint or through a pipe or water pipe
Smoking and the Body
THC enters the body through the Lungs
The smoke is inhaled and held in the lungsAll affect how much THC will enter the plasmaTHC crosses the blood barrier through the capillaries in the lungs
After inhalation THC can reach the brain in about 14 seconds
After a 6 min smoking period peak blood levels reached at about 7 min (100 ngml plasma)
Most THC is absorbed from the blood within 30 min
Moves rapidly into the brain and across the bloodbrainplacental barrier Because fatty chains make it very lipid soluble
Half-life is about 19 hours Can store in fat cells
Established physiological effects are dose related
Lethal dose for THC use has now been studied and no human deaths have been reported due to intoxication from cannabis
Metabolites
bull Radioactively labeled delta-9-THC has been found to persist in the body as an active metabolite as long as 8 days after use
Primary metabolite has a half-life of 50 hours The complete elimination of the drug can take as long as 6 weeks
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
23 of metabolites are excreted in feces13 of metabolites are excreted in urine
Cannabis Pharmacology
Primary Cannabinoids from Cannabis are
bull Cannabinol (CBN) Cannabidiol (CBD) and Tetrahydrocannabinol (THC)
bull THC (-9-THC ) is the only one with significant psychoactive properties
bull CBN - 110 th activity of THC CBD - none
bull 2 isomers a trans-delta-9-THC and a delta-8-THC
bull A cannabidiol (the 2nd most abundant psychoactive ingredient after THC)
bull A cannabinol a decomposition product of THC that accumulates as cannabis samples age
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
Therapeutic
bull Antiemeticbull Reduction of intra-ocular tensionbull Analgesicbull Muscle relaxant bull Anti-convulsant bull Anti-inflammatory appetite ldquothe munchiesrdquo It is one of the most well-known effects of marijuana the
powerful surge in appetite many users feel after smoking or ingesting the drug colloquially known as the munchies
Marinol
THC in a sesame oil suspension
Cannabinoid ReceptorsBeforethe 1980s it was often speculated that
cannabinoids produced their effects through non specific interaction with cell membranes instead of interacting with specific receptors
The discovery of the first cannabinoid receptors in the 1980s helped to resolve this debate These receptors are common in animals and have been found in mammals birds fishes and reptiles
There are currently two known types of cannabinoid receptors CB1 and CB2
CB1 ReceptorsFound primarily in the brain (specifically basal ganglia limbic
system including the hippocampus and cerebellum)1048766Most dense in brain regions involved with thinking and memory
attention and control of movement1048766Also present in both male and female reproductive systems as
well as in the lungs liver and kidneys1048766Appear to be responsible for the euphoric and anticonvulsive
effects of Cannabis1048766Essentially absent in the medulla oblongata the part of the brain
that is responsible for respiratory and cardiovascular functions
Thus there is no risk of respiratory or cardiovascular failure as there is with many other drugs
CB2 Receptor
CB2 receptors are almost exclusively found in the immune system (T cells macrophages B cells) with the greatest density in the spleen
1048766CB2 receptors appear to be responsible for the anti-inflammatory and possible other therapeutic effects of Cannabis
1048766Also expressed on peripheral nerve terminals
Cannabis and Δ9- (THC) for weight loss
bull Obesity is one of the highest preventable causes of morbidity and mortality in the developed world It has been well known for a long time that exposure to cannabis produces an increase of appetite (a phenomenon referred to as the munchies) This phenomenon led to an exploration of the role of the endocannabinoid system in the regulation of obesity and associated metabolic syndrome This effort subsequently led to the development of a successful therapeutic approach for obesity that consisted of blocking the cannabinoid CB1 receptors using ligands such as Rimonabant in order to produce weight loss and improve metabolic profile
What is obesity
Obesity is characterized by an abnormal accumulation of body fat usually 20 percent or more over an individuals ideal body weight Obesity results when the size or number of fat cells in a persons body increases When a person gains weight these fat cells first increase in size and later in number When a person starts losing weight the cells decreas ein size but their number generally stays the same This is part of the reason that once you gain a significant amount of weight it is more difficult to lose it
The clinical definition of obesity is a body mass index(BMI)of 30 or higher BMI = Weight (in kg) Height (in meters) Squared
Rimonabant
bull Acompliareg(Sanofi-Aventis)
launched in Europe in 2006 for
oral treatment of obesity at 20 mg
once daily
Selective blocker of central
and peripheral CB1 receptors
It reduces food intake and improves lipid and glucose metabolism
Rimonabant
Despite being efficacious Rimonabant was associated with increased rates of depression and anxiety and therefore removed from the market
- Cannabis
- Slide 2
- Slide 3
- Cannabis spp
- Slide 5
- Slide 6
- Hemp
- What is Marijuana
- Marijuana ndash History of Use
- HempvsMarijuana-1
- HempvsMarijuana-2
- HempvsMarijuana-3
- Cannabis Biology
- Chemical constituents of Cannabis
- What is a cannabinoid
- What are cannabinoids
- Natural cannabinoids
- Slide 18
- Representative cannabinoids
- Slide 20
- Endocannabinoids
- Structure of THC and synthetic analogs
- Slide 23
- Slide 24
- THC
- Results of SAR
- Modes of Absorption
- Smoking and the Body
- Slide 29
- Slide 30
- Metabolites
- Slide 32
- Slide 33
- Cannabis Pharmacology
- Slide 35
- Therapeutic
- Marinol
- Cannabinoid Receptors
- CB1 Receptors
- CB2 Receptor
- Cannabis and Δ9- (THC) for weight loss
- What is obesity
- Slide 43
- Slide 44
- Rimonabant
- Slide 46
- Slide 47
- Slide 48
-
HempvsMarijuana-2
bull The term marijuanais of Spanish derivation and was primarily used to describe varieties of Cannabisthat were more commonly bred over time for medicinal and recreational purposes like Cannabisindica and certain strains of Cannabissativa
HempvsMarijuana-3
bull Two cannabinoids are preponderant in Cannabis
bull THC CBDbull psychoactive ingredient antipsychoactive ingredient
Marijuana Hempbull (leaves and flowers of the female plant)
bull High in THC High in CBDbull Low in THCbull Low in CBD
Cannabis BiologyMajor Drug Component ndash delta-trans-tetrahydrocannabinol (THC)
- binds to specific receptors in brain
THC- produced in glands on leaves and flowers
-- female plants produce more glands
-- gland production stimulated by heat sunlight drought
-- sinsemilla (sin = without semilla = seeds) ndash particularly strong
Hashish ndash product - relatively pure resin
Glands THC
Chemical constituents of Cannabis
bull Cannabinoids (66)bull Nitrogenous compounds (27)bull Amino acids(18)bull Proteins enzymes (11)bull Sugars (34)bull Hydrocarbons (50)bull Simple alcohols (7)bull Simple aldehydes (12)bull Simple ketones (13)bull Simple acids (21)bull Fatty acids (22)bull Simple esterslactones (13)bull Steroids (11)bull Terpenes (20)bull Non-cannabinoid phenols (25)bull Flavoroids (21)bull Vitamins (1)bull Pigments (2)bull Elements (9) bull Total known compounds (483)
What is a cannabinoid
bullInitially compounds extracted by Cannabis spp producing characteristic psychoactivity
bullLater compounds with a characteristic terpenoid structure
bullCurrently most any compound that produces cannabinoid psychoactivity natural or synthetic
bullOccasionally just compounds that will interact with cannabinoid receptors
What are cannabinoidsbull Group of gt60 dibenzopyran chemicals found in
leaves and flowering tops of female cannabis plant (Cannabis sativa and Cannabis indica)
bull Some common cannabinoids are
In the plantIn your body (endogenous)
Synthetic
Δ9 ndash THC 2-arichidonyl glycerol (2 ndash AG)
CP 55940
Δ8 ndash THC anandamideHU ndash 210
cannabidiol and cannabinol
Natural cannabinoids
Representative cannabinoids
Classical cannabinoids Non-classical cannabinoid Aminoalkylindole
CB1 antagonists
Endogenous cannabinoids
Receptors suggest endogenous ligandsTwo main families identifiedBoth arachidonic acid derivativesPrecursors in membranes
ldquoMade on demandrdquoAmides (anandamide)
Esters (2-AG)
bull Significant differences
ndash Routes of synthesis ndash Mode of degradation
(FAAH vs MAGL)ndash Efficacy
Endocannabinoids
bull Anandamide (Sanskrit ananda inner bliss) is one endocannabinoid It is found in chocolate (though there is some controversy over whether the small quantity has any effect on the body) It is about as potent as THC
Structure of THC and synthetic analogs
Lipophilic side chain Most potent analog 100s
times more potent than THC
with 4 major cannabinoids in the plant
bull 2 isomers a trans-delta-9-THC and a delta-8-THC
bull A cannabidiol (the 2nd most abundant psychoactive ingredient after THC)
bull A cannabinol a decomposition product of THC that accumulates as cannabis samples age
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
THC
bull Variedly aromatic ring (C Ring)
O
O
H
11rsquo-di-methyl-pyrane ring (B ring)
Variedly unsaturated cyclohexyl ring (A ring)
Results of SAR
bull Psychoactive properties are (-) trans-enatioselective
bull Length lipophilicity C3 alkyl chain
bull Phenolic hydroxyl-group
bull C9 substitute
O
O
H
Modes of Absorption
bull The most common method of absorption is smoking Either in a loosely rolled cigarette called a joint or through a pipe or water pipe
Smoking and the Body
THC enters the body through the Lungs
The smoke is inhaled and held in the lungsAll affect how much THC will enter the plasmaTHC crosses the blood barrier through the capillaries in the lungs
After inhalation THC can reach the brain in about 14 seconds
After a 6 min smoking period peak blood levels reached at about 7 min (100 ngml plasma)
Most THC is absorbed from the blood within 30 min
Moves rapidly into the brain and across the bloodbrainplacental barrier Because fatty chains make it very lipid soluble
Half-life is about 19 hours Can store in fat cells
Established physiological effects are dose related
Lethal dose for THC use has now been studied and no human deaths have been reported due to intoxication from cannabis
Metabolites
bull Radioactively labeled delta-9-THC has been found to persist in the body as an active metabolite as long as 8 days after use
Primary metabolite has a half-life of 50 hours The complete elimination of the drug can take as long as 6 weeks
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
23 of metabolites are excreted in feces13 of metabolites are excreted in urine
Cannabis Pharmacology
Primary Cannabinoids from Cannabis are
bull Cannabinol (CBN) Cannabidiol (CBD) and Tetrahydrocannabinol (THC)
bull THC (-9-THC ) is the only one with significant psychoactive properties
bull CBN - 110 th activity of THC CBD - none
bull 2 isomers a trans-delta-9-THC and a delta-8-THC
bull A cannabidiol (the 2nd most abundant psychoactive ingredient after THC)
bull A cannabinol a decomposition product of THC that accumulates as cannabis samples age
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
Therapeutic
bull Antiemeticbull Reduction of intra-ocular tensionbull Analgesicbull Muscle relaxant bull Anti-convulsant bull Anti-inflammatory appetite ldquothe munchiesrdquo It is one of the most well-known effects of marijuana the
powerful surge in appetite many users feel after smoking or ingesting the drug colloquially known as the munchies
Marinol
THC in a sesame oil suspension
Cannabinoid ReceptorsBeforethe 1980s it was often speculated that
cannabinoids produced their effects through non specific interaction with cell membranes instead of interacting with specific receptors
The discovery of the first cannabinoid receptors in the 1980s helped to resolve this debate These receptors are common in animals and have been found in mammals birds fishes and reptiles
There are currently two known types of cannabinoid receptors CB1 and CB2
CB1 ReceptorsFound primarily in the brain (specifically basal ganglia limbic
system including the hippocampus and cerebellum)1048766Most dense in brain regions involved with thinking and memory
attention and control of movement1048766Also present in both male and female reproductive systems as
well as in the lungs liver and kidneys1048766Appear to be responsible for the euphoric and anticonvulsive
effects of Cannabis1048766Essentially absent in the medulla oblongata the part of the brain
that is responsible for respiratory and cardiovascular functions
Thus there is no risk of respiratory or cardiovascular failure as there is with many other drugs
CB2 Receptor
CB2 receptors are almost exclusively found in the immune system (T cells macrophages B cells) with the greatest density in the spleen
1048766CB2 receptors appear to be responsible for the anti-inflammatory and possible other therapeutic effects of Cannabis
1048766Also expressed on peripheral nerve terminals
Cannabis and Δ9- (THC) for weight loss
bull Obesity is one of the highest preventable causes of morbidity and mortality in the developed world It has been well known for a long time that exposure to cannabis produces an increase of appetite (a phenomenon referred to as the munchies) This phenomenon led to an exploration of the role of the endocannabinoid system in the regulation of obesity and associated metabolic syndrome This effort subsequently led to the development of a successful therapeutic approach for obesity that consisted of blocking the cannabinoid CB1 receptors using ligands such as Rimonabant in order to produce weight loss and improve metabolic profile
What is obesity
Obesity is characterized by an abnormal accumulation of body fat usually 20 percent or more over an individuals ideal body weight Obesity results when the size or number of fat cells in a persons body increases When a person gains weight these fat cells first increase in size and later in number When a person starts losing weight the cells decreas ein size but their number generally stays the same This is part of the reason that once you gain a significant amount of weight it is more difficult to lose it
The clinical definition of obesity is a body mass index(BMI)of 30 or higher BMI = Weight (in kg) Height (in meters) Squared
Rimonabant
bull Acompliareg(Sanofi-Aventis)
launched in Europe in 2006 for
oral treatment of obesity at 20 mg
once daily
Selective blocker of central
and peripheral CB1 receptors
It reduces food intake and improves lipid and glucose metabolism
Rimonabant
Despite being efficacious Rimonabant was associated with increased rates of depression and anxiety and therefore removed from the market
- Cannabis
- Slide 2
- Slide 3
- Cannabis spp
- Slide 5
- Slide 6
- Hemp
- What is Marijuana
- Marijuana ndash History of Use
- HempvsMarijuana-1
- HempvsMarijuana-2
- HempvsMarijuana-3
- Cannabis Biology
- Chemical constituents of Cannabis
- What is a cannabinoid
- What are cannabinoids
- Natural cannabinoids
- Slide 18
- Representative cannabinoids
- Slide 20
- Endocannabinoids
- Structure of THC and synthetic analogs
- Slide 23
- Slide 24
- THC
- Results of SAR
- Modes of Absorption
- Smoking and the Body
- Slide 29
- Slide 30
- Metabolites
- Slide 32
- Slide 33
- Cannabis Pharmacology
- Slide 35
- Therapeutic
- Marinol
- Cannabinoid Receptors
- CB1 Receptors
- CB2 Receptor
- Cannabis and Δ9- (THC) for weight loss
- What is obesity
- Slide 43
- Slide 44
- Rimonabant
- Slide 46
- Slide 47
- Slide 48
-
HempvsMarijuana-3
bull Two cannabinoids are preponderant in Cannabis
bull THC CBDbull psychoactive ingredient antipsychoactive ingredient
Marijuana Hempbull (leaves and flowers of the female plant)
bull High in THC High in CBDbull Low in THCbull Low in CBD
Cannabis BiologyMajor Drug Component ndash delta-trans-tetrahydrocannabinol (THC)
- binds to specific receptors in brain
THC- produced in glands on leaves and flowers
-- female plants produce more glands
-- gland production stimulated by heat sunlight drought
-- sinsemilla (sin = without semilla = seeds) ndash particularly strong
Hashish ndash product - relatively pure resin
Glands THC
Chemical constituents of Cannabis
bull Cannabinoids (66)bull Nitrogenous compounds (27)bull Amino acids(18)bull Proteins enzymes (11)bull Sugars (34)bull Hydrocarbons (50)bull Simple alcohols (7)bull Simple aldehydes (12)bull Simple ketones (13)bull Simple acids (21)bull Fatty acids (22)bull Simple esterslactones (13)bull Steroids (11)bull Terpenes (20)bull Non-cannabinoid phenols (25)bull Flavoroids (21)bull Vitamins (1)bull Pigments (2)bull Elements (9) bull Total known compounds (483)
What is a cannabinoid
bullInitially compounds extracted by Cannabis spp producing characteristic psychoactivity
bullLater compounds with a characteristic terpenoid structure
bullCurrently most any compound that produces cannabinoid psychoactivity natural or synthetic
bullOccasionally just compounds that will interact with cannabinoid receptors
What are cannabinoidsbull Group of gt60 dibenzopyran chemicals found in
leaves and flowering tops of female cannabis plant (Cannabis sativa and Cannabis indica)
bull Some common cannabinoids are
In the plantIn your body (endogenous)
Synthetic
Δ9 ndash THC 2-arichidonyl glycerol (2 ndash AG)
CP 55940
Δ8 ndash THC anandamideHU ndash 210
cannabidiol and cannabinol
Natural cannabinoids
Representative cannabinoids
Classical cannabinoids Non-classical cannabinoid Aminoalkylindole
CB1 antagonists
Endogenous cannabinoids
Receptors suggest endogenous ligandsTwo main families identifiedBoth arachidonic acid derivativesPrecursors in membranes
ldquoMade on demandrdquoAmides (anandamide)
Esters (2-AG)
bull Significant differences
ndash Routes of synthesis ndash Mode of degradation
(FAAH vs MAGL)ndash Efficacy
Endocannabinoids
bull Anandamide (Sanskrit ananda inner bliss) is one endocannabinoid It is found in chocolate (though there is some controversy over whether the small quantity has any effect on the body) It is about as potent as THC
Structure of THC and synthetic analogs
Lipophilic side chain Most potent analog 100s
times more potent than THC
with 4 major cannabinoids in the plant
bull 2 isomers a trans-delta-9-THC and a delta-8-THC
bull A cannabidiol (the 2nd most abundant psychoactive ingredient after THC)
bull A cannabinol a decomposition product of THC that accumulates as cannabis samples age
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
THC
bull Variedly aromatic ring (C Ring)
O
O
H
11rsquo-di-methyl-pyrane ring (B ring)
Variedly unsaturated cyclohexyl ring (A ring)
Results of SAR
bull Psychoactive properties are (-) trans-enatioselective
bull Length lipophilicity C3 alkyl chain
bull Phenolic hydroxyl-group
bull C9 substitute
O
O
H
Modes of Absorption
bull The most common method of absorption is smoking Either in a loosely rolled cigarette called a joint or through a pipe or water pipe
Smoking and the Body
THC enters the body through the Lungs
The smoke is inhaled and held in the lungsAll affect how much THC will enter the plasmaTHC crosses the blood barrier through the capillaries in the lungs
After inhalation THC can reach the brain in about 14 seconds
After a 6 min smoking period peak blood levels reached at about 7 min (100 ngml plasma)
Most THC is absorbed from the blood within 30 min
Moves rapidly into the brain and across the bloodbrainplacental barrier Because fatty chains make it very lipid soluble
Half-life is about 19 hours Can store in fat cells
Established physiological effects are dose related
Lethal dose for THC use has now been studied and no human deaths have been reported due to intoxication from cannabis
Metabolites
bull Radioactively labeled delta-9-THC has been found to persist in the body as an active metabolite as long as 8 days after use
Primary metabolite has a half-life of 50 hours The complete elimination of the drug can take as long as 6 weeks
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
23 of metabolites are excreted in feces13 of metabolites are excreted in urine
Cannabis Pharmacology
Primary Cannabinoids from Cannabis are
bull Cannabinol (CBN) Cannabidiol (CBD) and Tetrahydrocannabinol (THC)
bull THC (-9-THC ) is the only one with significant psychoactive properties
bull CBN - 110 th activity of THC CBD - none
bull 2 isomers a trans-delta-9-THC and a delta-8-THC
bull A cannabidiol (the 2nd most abundant psychoactive ingredient after THC)
bull A cannabinol a decomposition product of THC that accumulates as cannabis samples age
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
Therapeutic
bull Antiemeticbull Reduction of intra-ocular tensionbull Analgesicbull Muscle relaxant bull Anti-convulsant bull Anti-inflammatory appetite ldquothe munchiesrdquo It is one of the most well-known effects of marijuana the
powerful surge in appetite many users feel after smoking or ingesting the drug colloquially known as the munchies
Marinol
THC in a sesame oil suspension
Cannabinoid ReceptorsBeforethe 1980s it was often speculated that
cannabinoids produced their effects through non specific interaction with cell membranes instead of interacting with specific receptors
The discovery of the first cannabinoid receptors in the 1980s helped to resolve this debate These receptors are common in animals and have been found in mammals birds fishes and reptiles
There are currently two known types of cannabinoid receptors CB1 and CB2
CB1 ReceptorsFound primarily in the brain (specifically basal ganglia limbic
system including the hippocampus and cerebellum)1048766Most dense in brain regions involved with thinking and memory
attention and control of movement1048766Also present in both male and female reproductive systems as
well as in the lungs liver and kidneys1048766Appear to be responsible for the euphoric and anticonvulsive
effects of Cannabis1048766Essentially absent in the medulla oblongata the part of the brain
that is responsible for respiratory and cardiovascular functions
Thus there is no risk of respiratory or cardiovascular failure as there is with many other drugs
CB2 Receptor
CB2 receptors are almost exclusively found in the immune system (T cells macrophages B cells) with the greatest density in the spleen
1048766CB2 receptors appear to be responsible for the anti-inflammatory and possible other therapeutic effects of Cannabis
1048766Also expressed on peripheral nerve terminals
Cannabis and Δ9- (THC) for weight loss
bull Obesity is one of the highest preventable causes of morbidity and mortality in the developed world It has been well known for a long time that exposure to cannabis produces an increase of appetite (a phenomenon referred to as the munchies) This phenomenon led to an exploration of the role of the endocannabinoid system in the regulation of obesity and associated metabolic syndrome This effort subsequently led to the development of a successful therapeutic approach for obesity that consisted of blocking the cannabinoid CB1 receptors using ligands such as Rimonabant in order to produce weight loss and improve metabolic profile
What is obesity
Obesity is characterized by an abnormal accumulation of body fat usually 20 percent or more over an individuals ideal body weight Obesity results when the size or number of fat cells in a persons body increases When a person gains weight these fat cells first increase in size and later in number When a person starts losing weight the cells decreas ein size but their number generally stays the same This is part of the reason that once you gain a significant amount of weight it is more difficult to lose it
The clinical definition of obesity is a body mass index(BMI)of 30 or higher BMI = Weight (in kg) Height (in meters) Squared
Rimonabant
bull Acompliareg(Sanofi-Aventis)
launched in Europe in 2006 for
oral treatment of obesity at 20 mg
once daily
Selective blocker of central
and peripheral CB1 receptors
It reduces food intake and improves lipid and glucose metabolism
Rimonabant
Despite being efficacious Rimonabant was associated with increased rates of depression and anxiety and therefore removed from the market
- Cannabis
- Slide 2
- Slide 3
- Cannabis spp
- Slide 5
- Slide 6
- Hemp
- What is Marijuana
- Marijuana ndash History of Use
- HempvsMarijuana-1
- HempvsMarijuana-2
- HempvsMarijuana-3
- Cannabis Biology
- Chemical constituents of Cannabis
- What is a cannabinoid
- What are cannabinoids
- Natural cannabinoids
- Slide 18
- Representative cannabinoids
- Slide 20
- Endocannabinoids
- Structure of THC and synthetic analogs
- Slide 23
- Slide 24
- THC
- Results of SAR
- Modes of Absorption
- Smoking and the Body
- Slide 29
- Slide 30
- Metabolites
- Slide 32
- Slide 33
- Cannabis Pharmacology
- Slide 35
- Therapeutic
- Marinol
- Cannabinoid Receptors
- CB1 Receptors
- CB2 Receptor
- Cannabis and Δ9- (THC) for weight loss
- What is obesity
- Slide 43
- Slide 44
- Rimonabant
- Slide 46
- Slide 47
- Slide 48
-
Cannabis BiologyMajor Drug Component ndash delta-trans-tetrahydrocannabinol (THC)
- binds to specific receptors in brain
THC- produced in glands on leaves and flowers
-- female plants produce more glands
-- gland production stimulated by heat sunlight drought
-- sinsemilla (sin = without semilla = seeds) ndash particularly strong
Hashish ndash product - relatively pure resin
Glands THC
Chemical constituents of Cannabis
bull Cannabinoids (66)bull Nitrogenous compounds (27)bull Amino acids(18)bull Proteins enzymes (11)bull Sugars (34)bull Hydrocarbons (50)bull Simple alcohols (7)bull Simple aldehydes (12)bull Simple ketones (13)bull Simple acids (21)bull Fatty acids (22)bull Simple esterslactones (13)bull Steroids (11)bull Terpenes (20)bull Non-cannabinoid phenols (25)bull Flavoroids (21)bull Vitamins (1)bull Pigments (2)bull Elements (9) bull Total known compounds (483)
What is a cannabinoid
bullInitially compounds extracted by Cannabis spp producing characteristic psychoactivity
bullLater compounds with a characteristic terpenoid structure
bullCurrently most any compound that produces cannabinoid psychoactivity natural or synthetic
bullOccasionally just compounds that will interact with cannabinoid receptors
What are cannabinoidsbull Group of gt60 dibenzopyran chemicals found in
leaves and flowering tops of female cannabis plant (Cannabis sativa and Cannabis indica)
bull Some common cannabinoids are
In the plantIn your body (endogenous)
Synthetic
Δ9 ndash THC 2-arichidonyl glycerol (2 ndash AG)
CP 55940
Δ8 ndash THC anandamideHU ndash 210
cannabidiol and cannabinol
Natural cannabinoids
Representative cannabinoids
Classical cannabinoids Non-classical cannabinoid Aminoalkylindole
CB1 antagonists
Endogenous cannabinoids
Receptors suggest endogenous ligandsTwo main families identifiedBoth arachidonic acid derivativesPrecursors in membranes
ldquoMade on demandrdquoAmides (anandamide)
Esters (2-AG)
bull Significant differences
ndash Routes of synthesis ndash Mode of degradation
(FAAH vs MAGL)ndash Efficacy
Endocannabinoids
bull Anandamide (Sanskrit ananda inner bliss) is one endocannabinoid It is found in chocolate (though there is some controversy over whether the small quantity has any effect on the body) It is about as potent as THC
Structure of THC and synthetic analogs
Lipophilic side chain Most potent analog 100s
times more potent than THC
with 4 major cannabinoids in the plant
bull 2 isomers a trans-delta-9-THC and a delta-8-THC
bull A cannabidiol (the 2nd most abundant psychoactive ingredient after THC)
bull A cannabinol a decomposition product of THC that accumulates as cannabis samples age
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
THC
bull Variedly aromatic ring (C Ring)
O
O
H
11rsquo-di-methyl-pyrane ring (B ring)
Variedly unsaturated cyclohexyl ring (A ring)
Results of SAR
bull Psychoactive properties are (-) trans-enatioselective
bull Length lipophilicity C3 alkyl chain
bull Phenolic hydroxyl-group
bull C9 substitute
O
O
H
Modes of Absorption
bull The most common method of absorption is smoking Either in a loosely rolled cigarette called a joint or through a pipe or water pipe
Smoking and the Body
THC enters the body through the Lungs
The smoke is inhaled and held in the lungsAll affect how much THC will enter the plasmaTHC crosses the blood barrier through the capillaries in the lungs
After inhalation THC can reach the brain in about 14 seconds
After a 6 min smoking period peak blood levels reached at about 7 min (100 ngml plasma)
Most THC is absorbed from the blood within 30 min
Moves rapidly into the brain and across the bloodbrainplacental barrier Because fatty chains make it very lipid soluble
Half-life is about 19 hours Can store in fat cells
Established physiological effects are dose related
Lethal dose for THC use has now been studied and no human deaths have been reported due to intoxication from cannabis
Metabolites
bull Radioactively labeled delta-9-THC has been found to persist in the body as an active metabolite as long as 8 days after use
Primary metabolite has a half-life of 50 hours The complete elimination of the drug can take as long as 6 weeks
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
23 of metabolites are excreted in feces13 of metabolites are excreted in urine
Cannabis Pharmacology
Primary Cannabinoids from Cannabis are
bull Cannabinol (CBN) Cannabidiol (CBD) and Tetrahydrocannabinol (THC)
bull THC (-9-THC ) is the only one with significant psychoactive properties
bull CBN - 110 th activity of THC CBD - none
bull 2 isomers a trans-delta-9-THC and a delta-8-THC
bull A cannabidiol (the 2nd most abundant psychoactive ingredient after THC)
bull A cannabinol a decomposition product of THC that accumulates as cannabis samples age
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
Therapeutic
bull Antiemeticbull Reduction of intra-ocular tensionbull Analgesicbull Muscle relaxant bull Anti-convulsant bull Anti-inflammatory appetite ldquothe munchiesrdquo It is one of the most well-known effects of marijuana the
powerful surge in appetite many users feel after smoking or ingesting the drug colloquially known as the munchies
Marinol
THC in a sesame oil suspension
Cannabinoid ReceptorsBeforethe 1980s it was often speculated that
cannabinoids produced their effects through non specific interaction with cell membranes instead of interacting with specific receptors
The discovery of the first cannabinoid receptors in the 1980s helped to resolve this debate These receptors are common in animals and have been found in mammals birds fishes and reptiles
There are currently two known types of cannabinoid receptors CB1 and CB2
CB1 ReceptorsFound primarily in the brain (specifically basal ganglia limbic
system including the hippocampus and cerebellum)1048766Most dense in brain regions involved with thinking and memory
attention and control of movement1048766Also present in both male and female reproductive systems as
well as in the lungs liver and kidneys1048766Appear to be responsible for the euphoric and anticonvulsive
effects of Cannabis1048766Essentially absent in the medulla oblongata the part of the brain
that is responsible for respiratory and cardiovascular functions
Thus there is no risk of respiratory or cardiovascular failure as there is with many other drugs
CB2 Receptor
CB2 receptors are almost exclusively found in the immune system (T cells macrophages B cells) with the greatest density in the spleen
1048766CB2 receptors appear to be responsible for the anti-inflammatory and possible other therapeutic effects of Cannabis
1048766Also expressed on peripheral nerve terminals
Cannabis and Δ9- (THC) for weight loss
bull Obesity is one of the highest preventable causes of morbidity and mortality in the developed world It has been well known for a long time that exposure to cannabis produces an increase of appetite (a phenomenon referred to as the munchies) This phenomenon led to an exploration of the role of the endocannabinoid system in the regulation of obesity and associated metabolic syndrome This effort subsequently led to the development of a successful therapeutic approach for obesity that consisted of blocking the cannabinoid CB1 receptors using ligands such as Rimonabant in order to produce weight loss and improve metabolic profile
What is obesity
Obesity is characterized by an abnormal accumulation of body fat usually 20 percent or more over an individuals ideal body weight Obesity results when the size or number of fat cells in a persons body increases When a person gains weight these fat cells first increase in size and later in number When a person starts losing weight the cells decreas ein size but their number generally stays the same This is part of the reason that once you gain a significant amount of weight it is more difficult to lose it
The clinical definition of obesity is a body mass index(BMI)of 30 or higher BMI = Weight (in kg) Height (in meters) Squared
Rimonabant
bull Acompliareg(Sanofi-Aventis)
launched in Europe in 2006 for
oral treatment of obesity at 20 mg
once daily
Selective blocker of central
and peripheral CB1 receptors
It reduces food intake and improves lipid and glucose metabolism
Rimonabant
Despite being efficacious Rimonabant was associated with increased rates of depression and anxiety and therefore removed from the market
- Cannabis
- Slide 2
- Slide 3
- Cannabis spp
- Slide 5
- Slide 6
- Hemp
- What is Marijuana
- Marijuana ndash History of Use
- HempvsMarijuana-1
- HempvsMarijuana-2
- HempvsMarijuana-3
- Cannabis Biology
- Chemical constituents of Cannabis
- What is a cannabinoid
- What are cannabinoids
- Natural cannabinoids
- Slide 18
- Representative cannabinoids
- Slide 20
- Endocannabinoids
- Structure of THC and synthetic analogs
- Slide 23
- Slide 24
- THC
- Results of SAR
- Modes of Absorption
- Smoking and the Body
- Slide 29
- Slide 30
- Metabolites
- Slide 32
- Slide 33
- Cannabis Pharmacology
- Slide 35
- Therapeutic
- Marinol
- Cannabinoid Receptors
- CB1 Receptors
- CB2 Receptor
- Cannabis and Δ9- (THC) for weight loss
- What is obesity
- Slide 43
- Slide 44
- Rimonabant
- Slide 46
- Slide 47
- Slide 48
-
Chemical constituents of Cannabis
bull Cannabinoids (66)bull Nitrogenous compounds (27)bull Amino acids(18)bull Proteins enzymes (11)bull Sugars (34)bull Hydrocarbons (50)bull Simple alcohols (7)bull Simple aldehydes (12)bull Simple ketones (13)bull Simple acids (21)bull Fatty acids (22)bull Simple esterslactones (13)bull Steroids (11)bull Terpenes (20)bull Non-cannabinoid phenols (25)bull Flavoroids (21)bull Vitamins (1)bull Pigments (2)bull Elements (9) bull Total known compounds (483)
What is a cannabinoid
bullInitially compounds extracted by Cannabis spp producing characteristic psychoactivity
bullLater compounds with a characteristic terpenoid structure
bullCurrently most any compound that produces cannabinoid psychoactivity natural or synthetic
bullOccasionally just compounds that will interact with cannabinoid receptors
What are cannabinoidsbull Group of gt60 dibenzopyran chemicals found in
leaves and flowering tops of female cannabis plant (Cannabis sativa and Cannabis indica)
bull Some common cannabinoids are
In the plantIn your body (endogenous)
Synthetic
Δ9 ndash THC 2-arichidonyl glycerol (2 ndash AG)
CP 55940
Δ8 ndash THC anandamideHU ndash 210
cannabidiol and cannabinol
Natural cannabinoids
Representative cannabinoids
Classical cannabinoids Non-classical cannabinoid Aminoalkylindole
CB1 antagonists
Endogenous cannabinoids
Receptors suggest endogenous ligandsTwo main families identifiedBoth arachidonic acid derivativesPrecursors in membranes
ldquoMade on demandrdquoAmides (anandamide)
Esters (2-AG)
bull Significant differences
ndash Routes of synthesis ndash Mode of degradation
(FAAH vs MAGL)ndash Efficacy
Endocannabinoids
bull Anandamide (Sanskrit ananda inner bliss) is one endocannabinoid It is found in chocolate (though there is some controversy over whether the small quantity has any effect on the body) It is about as potent as THC
Structure of THC and synthetic analogs
Lipophilic side chain Most potent analog 100s
times more potent than THC
with 4 major cannabinoids in the plant
bull 2 isomers a trans-delta-9-THC and a delta-8-THC
bull A cannabidiol (the 2nd most abundant psychoactive ingredient after THC)
bull A cannabinol a decomposition product of THC that accumulates as cannabis samples age
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
THC
bull Variedly aromatic ring (C Ring)
O
O
H
11rsquo-di-methyl-pyrane ring (B ring)
Variedly unsaturated cyclohexyl ring (A ring)
Results of SAR
bull Psychoactive properties are (-) trans-enatioselective
bull Length lipophilicity C3 alkyl chain
bull Phenolic hydroxyl-group
bull C9 substitute
O
O
H
Modes of Absorption
bull The most common method of absorption is smoking Either in a loosely rolled cigarette called a joint or through a pipe or water pipe
Smoking and the Body
THC enters the body through the Lungs
The smoke is inhaled and held in the lungsAll affect how much THC will enter the plasmaTHC crosses the blood barrier through the capillaries in the lungs
After inhalation THC can reach the brain in about 14 seconds
After a 6 min smoking period peak blood levels reached at about 7 min (100 ngml plasma)
Most THC is absorbed from the blood within 30 min
Moves rapidly into the brain and across the bloodbrainplacental barrier Because fatty chains make it very lipid soluble
Half-life is about 19 hours Can store in fat cells
Established physiological effects are dose related
Lethal dose for THC use has now been studied and no human deaths have been reported due to intoxication from cannabis
Metabolites
bull Radioactively labeled delta-9-THC has been found to persist in the body as an active metabolite as long as 8 days after use
Primary metabolite has a half-life of 50 hours The complete elimination of the drug can take as long as 6 weeks
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
23 of metabolites are excreted in feces13 of metabolites are excreted in urine
Cannabis Pharmacology
Primary Cannabinoids from Cannabis are
bull Cannabinol (CBN) Cannabidiol (CBD) and Tetrahydrocannabinol (THC)
bull THC (-9-THC ) is the only one with significant psychoactive properties
bull CBN - 110 th activity of THC CBD - none
bull 2 isomers a trans-delta-9-THC and a delta-8-THC
bull A cannabidiol (the 2nd most abundant psychoactive ingredient after THC)
bull A cannabinol a decomposition product of THC that accumulates as cannabis samples age
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
Therapeutic
bull Antiemeticbull Reduction of intra-ocular tensionbull Analgesicbull Muscle relaxant bull Anti-convulsant bull Anti-inflammatory appetite ldquothe munchiesrdquo It is one of the most well-known effects of marijuana the
powerful surge in appetite many users feel after smoking or ingesting the drug colloquially known as the munchies
Marinol
THC in a sesame oil suspension
Cannabinoid ReceptorsBeforethe 1980s it was often speculated that
cannabinoids produced their effects through non specific interaction with cell membranes instead of interacting with specific receptors
The discovery of the first cannabinoid receptors in the 1980s helped to resolve this debate These receptors are common in animals and have been found in mammals birds fishes and reptiles
There are currently two known types of cannabinoid receptors CB1 and CB2
CB1 ReceptorsFound primarily in the brain (specifically basal ganglia limbic
system including the hippocampus and cerebellum)1048766Most dense in brain regions involved with thinking and memory
attention and control of movement1048766Also present in both male and female reproductive systems as
well as in the lungs liver and kidneys1048766Appear to be responsible for the euphoric and anticonvulsive
effects of Cannabis1048766Essentially absent in the medulla oblongata the part of the brain
that is responsible for respiratory and cardiovascular functions
Thus there is no risk of respiratory or cardiovascular failure as there is with many other drugs
CB2 Receptor
CB2 receptors are almost exclusively found in the immune system (T cells macrophages B cells) with the greatest density in the spleen
1048766CB2 receptors appear to be responsible for the anti-inflammatory and possible other therapeutic effects of Cannabis
1048766Also expressed on peripheral nerve terminals
Cannabis and Δ9- (THC) for weight loss
bull Obesity is one of the highest preventable causes of morbidity and mortality in the developed world It has been well known for a long time that exposure to cannabis produces an increase of appetite (a phenomenon referred to as the munchies) This phenomenon led to an exploration of the role of the endocannabinoid system in the regulation of obesity and associated metabolic syndrome This effort subsequently led to the development of a successful therapeutic approach for obesity that consisted of blocking the cannabinoid CB1 receptors using ligands such as Rimonabant in order to produce weight loss and improve metabolic profile
What is obesity
Obesity is characterized by an abnormal accumulation of body fat usually 20 percent or more over an individuals ideal body weight Obesity results when the size or number of fat cells in a persons body increases When a person gains weight these fat cells first increase in size and later in number When a person starts losing weight the cells decreas ein size but their number generally stays the same This is part of the reason that once you gain a significant amount of weight it is more difficult to lose it
The clinical definition of obesity is a body mass index(BMI)of 30 or higher BMI = Weight (in kg) Height (in meters) Squared
Rimonabant
bull Acompliareg(Sanofi-Aventis)
launched in Europe in 2006 for
oral treatment of obesity at 20 mg
once daily
Selective blocker of central
and peripheral CB1 receptors
It reduces food intake and improves lipid and glucose metabolism
Rimonabant
Despite being efficacious Rimonabant was associated with increased rates of depression and anxiety and therefore removed from the market
- Cannabis
- Slide 2
- Slide 3
- Cannabis spp
- Slide 5
- Slide 6
- Hemp
- What is Marijuana
- Marijuana ndash History of Use
- HempvsMarijuana-1
- HempvsMarijuana-2
- HempvsMarijuana-3
- Cannabis Biology
- Chemical constituents of Cannabis
- What is a cannabinoid
- What are cannabinoids
- Natural cannabinoids
- Slide 18
- Representative cannabinoids
- Slide 20
- Endocannabinoids
- Structure of THC and synthetic analogs
- Slide 23
- Slide 24
- THC
- Results of SAR
- Modes of Absorption
- Smoking and the Body
- Slide 29
- Slide 30
- Metabolites
- Slide 32
- Slide 33
- Cannabis Pharmacology
- Slide 35
- Therapeutic
- Marinol
- Cannabinoid Receptors
- CB1 Receptors
- CB2 Receptor
- Cannabis and Δ9- (THC) for weight loss
- What is obesity
- Slide 43
- Slide 44
- Rimonabant
- Slide 46
- Slide 47
- Slide 48
-
What is a cannabinoid
bullInitially compounds extracted by Cannabis spp producing characteristic psychoactivity
bullLater compounds with a characteristic terpenoid structure
bullCurrently most any compound that produces cannabinoid psychoactivity natural or synthetic
bullOccasionally just compounds that will interact with cannabinoid receptors
What are cannabinoidsbull Group of gt60 dibenzopyran chemicals found in
leaves and flowering tops of female cannabis plant (Cannabis sativa and Cannabis indica)
bull Some common cannabinoids are
In the plantIn your body (endogenous)
Synthetic
Δ9 ndash THC 2-arichidonyl glycerol (2 ndash AG)
CP 55940
Δ8 ndash THC anandamideHU ndash 210
cannabidiol and cannabinol
Natural cannabinoids
Representative cannabinoids
Classical cannabinoids Non-classical cannabinoid Aminoalkylindole
CB1 antagonists
Endogenous cannabinoids
Receptors suggest endogenous ligandsTwo main families identifiedBoth arachidonic acid derivativesPrecursors in membranes
ldquoMade on demandrdquoAmides (anandamide)
Esters (2-AG)
bull Significant differences
ndash Routes of synthesis ndash Mode of degradation
(FAAH vs MAGL)ndash Efficacy
Endocannabinoids
bull Anandamide (Sanskrit ananda inner bliss) is one endocannabinoid It is found in chocolate (though there is some controversy over whether the small quantity has any effect on the body) It is about as potent as THC
Structure of THC and synthetic analogs
Lipophilic side chain Most potent analog 100s
times more potent than THC
with 4 major cannabinoids in the plant
bull 2 isomers a trans-delta-9-THC and a delta-8-THC
bull A cannabidiol (the 2nd most abundant psychoactive ingredient after THC)
bull A cannabinol a decomposition product of THC that accumulates as cannabis samples age
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
THC
bull Variedly aromatic ring (C Ring)
O
O
H
11rsquo-di-methyl-pyrane ring (B ring)
Variedly unsaturated cyclohexyl ring (A ring)
Results of SAR
bull Psychoactive properties are (-) trans-enatioselective
bull Length lipophilicity C3 alkyl chain
bull Phenolic hydroxyl-group
bull C9 substitute
O
O
H
Modes of Absorption
bull The most common method of absorption is smoking Either in a loosely rolled cigarette called a joint or through a pipe or water pipe
Smoking and the Body
THC enters the body through the Lungs
The smoke is inhaled and held in the lungsAll affect how much THC will enter the plasmaTHC crosses the blood barrier through the capillaries in the lungs
After inhalation THC can reach the brain in about 14 seconds
After a 6 min smoking period peak blood levels reached at about 7 min (100 ngml plasma)
Most THC is absorbed from the blood within 30 min
Moves rapidly into the brain and across the bloodbrainplacental barrier Because fatty chains make it very lipid soluble
Half-life is about 19 hours Can store in fat cells
Established physiological effects are dose related
Lethal dose for THC use has now been studied and no human deaths have been reported due to intoxication from cannabis
Metabolites
bull Radioactively labeled delta-9-THC has been found to persist in the body as an active metabolite as long as 8 days after use
Primary metabolite has a half-life of 50 hours The complete elimination of the drug can take as long as 6 weeks
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
23 of metabolites are excreted in feces13 of metabolites are excreted in urine
Cannabis Pharmacology
Primary Cannabinoids from Cannabis are
bull Cannabinol (CBN) Cannabidiol (CBD) and Tetrahydrocannabinol (THC)
bull THC (-9-THC ) is the only one with significant psychoactive properties
bull CBN - 110 th activity of THC CBD - none
bull 2 isomers a trans-delta-9-THC and a delta-8-THC
bull A cannabidiol (the 2nd most abundant psychoactive ingredient after THC)
bull A cannabinol a decomposition product of THC that accumulates as cannabis samples age
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
Therapeutic
bull Antiemeticbull Reduction of intra-ocular tensionbull Analgesicbull Muscle relaxant bull Anti-convulsant bull Anti-inflammatory appetite ldquothe munchiesrdquo It is one of the most well-known effects of marijuana the
powerful surge in appetite many users feel after smoking or ingesting the drug colloquially known as the munchies
Marinol
THC in a sesame oil suspension
Cannabinoid ReceptorsBeforethe 1980s it was often speculated that
cannabinoids produced their effects through non specific interaction with cell membranes instead of interacting with specific receptors
The discovery of the first cannabinoid receptors in the 1980s helped to resolve this debate These receptors are common in animals and have been found in mammals birds fishes and reptiles
There are currently two known types of cannabinoid receptors CB1 and CB2
CB1 ReceptorsFound primarily in the brain (specifically basal ganglia limbic
system including the hippocampus and cerebellum)1048766Most dense in brain regions involved with thinking and memory
attention and control of movement1048766Also present in both male and female reproductive systems as
well as in the lungs liver and kidneys1048766Appear to be responsible for the euphoric and anticonvulsive
effects of Cannabis1048766Essentially absent in the medulla oblongata the part of the brain
that is responsible for respiratory and cardiovascular functions
Thus there is no risk of respiratory or cardiovascular failure as there is with many other drugs
CB2 Receptor
CB2 receptors are almost exclusively found in the immune system (T cells macrophages B cells) with the greatest density in the spleen
1048766CB2 receptors appear to be responsible for the anti-inflammatory and possible other therapeutic effects of Cannabis
1048766Also expressed on peripheral nerve terminals
Cannabis and Δ9- (THC) for weight loss
bull Obesity is one of the highest preventable causes of morbidity and mortality in the developed world It has been well known for a long time that exposure to cannabis produces an increase of appetite (a phenomenon referred to as the munchies) This phenomenon led to an exploration of the role of the endocannabinoid system in the regulation of obesity and associated metabolic syndrome This effort subsequently led to the development of a successful therapeutic approach for obesity that consisted of blocking the cannabinoid CB1 receptors using ligands such as Rimonabant in order to produce weight loss and improve metabolic profile
What is obesity
Obesity is characterized by an abnormal accumulation of body fat usually 20 percent or more over an individuals ideal body weight Obesity results when the size or number of fat cells in a persons body increases When a person gains weight these fat cells first increase in size and later in number When a person starts losing weight the cells decreas ein size but their number generally stays the same This is part of the reason that once you gain a significant amount of weight it is more difficult to lose it
The clinical definition of obesity is a body mass index(BMI)of 30 or higher BMI = Weight (in kg) Height (in meters) Squared
Rimonabant
bull Acompliareg(Sanofi-Aventis)
launched in Europe in 2006 for
oral treatment of obesity at 20 mg
once daily
Selective blocker of central
and peripheral CB1 receptors
It reduces food intake and improves lipid and glucose metabolism
Rimonabant
Despite being efficacious Rimonabant was associated with increased rates of depression and anxiety and therefore removed from the market
- Cannabis
- Slide 2
- Slide 3
- Cannabis spp
- Slide 5
- Slide 6
- Hemp
- What is Marijuana
- Marijuana ndash History of Use
- HempvsMarijuana-1
- HempvsMarijuana-2
- HempvsMarijuana-3
- Cannabis Biology
- Chemical constituents of Cannabis
- What is a cannabinoid
- What are cannabinoids
- Natural cannabinoids
- Slide 18
- Representative cannabinoids
- Slide 20
- Endocannabinoids
- Structure of THC and synthetic analogs
- Slide 23
- Slide 24
- THC
- Results of SAR
- Modes of Absorption
- Smoking and the Body
- Slide 29
- Slide 30
- Metabolites
- Slide 32
- Slide 33
- Cannabis Pharmacology
- Slide 35
- Therapeutic
- Marinol
- Cannabinoid Receptors
- CB1 Receptors
- CB2 Receptor
- Cannabis and Δ9- (THC) for weight loss
- What is obesity
- Slide 43
- Slide 44
- Rimonabant
- Slide 46
- Slide 47
- Slide 48
-
What are cannabinoidsbull Group of gt60 dibenzopyran chemicals found in
leaves and flowering tops of female cannabis plant (Cannabis sativa and Cannabis indica)
bull Some common cannabinoids are
In the plantIn your body (endogenous)
Synthetic
Δ9 ndash THC 2-arichidonyl glycerol (2 ndash AG)
CP 55940
Δ8 ndash THC anandamideHU ndash 210
cannabidiol and cannabinol
Natural cannabinoids
Representative cannabinoids
Classical cannabinoids Non-classical cannabinoid Aminoalkylindole
CB1 antagonists
Endogenous cannabinoids
Receptors suggest endogenous ligandsTwo main families identifiedBoth arachidonic acid derivativesPrecursors in membranes
ldquoMade on demandrdquoAmides (anandamide)
Esters (2-AG)
bull Significant differences
ndash Routes of synthesis ndash Mode of degradation
(FAAH vs MAGL)ndash Efficacy
Endocannabinoids
bull Anandamide (Sanskrit ananda inner bliss) is one endocannabinoid It is found in chocolate (though there is some controversy over whether the small quantity has any effect on the body) It is about as potent as THC
Structure of THC and synthetic analogs
Lipophilic side chain Most potent analog 100s
times more potent than THC
with 4 major cannabinoids in the plant
bull 2 isomers a trans-delta-9-THC and a delta-8-THC
bull A cannabidiol (the 2nd most abundant psychoactive ingredient after THC)
bull A cannabinol a decomposition product of THC that accumulates as cannabis samples age
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
THC
bull Variedly aromatic ring (C Ring)
O
O
H
11rsquo-di-methyl-pyrane ring (B ring)
Variedly unsaturated cyclohexyl ring (A ring)
Results of SAR
bull Psychoactive properties are (-) trans-enatioselective
bull Length lipophilicity C3 alkyl chain
bull Phenolic hydroxyl-group
bull C9 substitute
O
O
H
Modes of Absorption
bull The most common method of absorption is smoking Either in a loosely rolled cigarette called a joint or through a pipe or water pipe
Smoking and the Body
THC enters the body through the Lungs
The smoke is inhaled and held in the lungsAll affect how much THC will enter the plasmaTHC crosses the blood barrier through the capillaries in the lungs
After inhalation THC can reach the brain in about 14 seconds
After a 6 min smoking period peak blood levels reached at about 7 min (100 ngml plasma)
Most THC is absorbed from the blood within 30 min
Moves rapidly into the brain and across the bloodbrainplacental barrier Because fatty chains make it very lipid soluble
Half-life is about 19 hours Can store in fat cells
Established physiological effects are dose related
Lethal dose for THC use has now been studied and no human deaths have been reported due to intoxication from cannabis
Metabolites
bull Radioactively labeled delta-9-THC has been found to persist in the body as an active metabolite as long as 8 days after use
Primary metabolite has a half-life of 50 hours The complete elimination of the drug can take as long as 6 weeks
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
23 of metabolites are excreted in feces13 of metabolites are excreted in urine
Cannabis Pharmacology
Primary Cannabinoids from Cannabis are
bull Cannabinol (CBN) Cannabidiol (CBD) and Tetrahydrocannabinol (THC)
bull THC (-9-THC ) is the only one with significant psychoactive properties
bull CBN - 110 th activity of THC CBD - none
bull 2 isomers a trans-delta-9-THC and a delta-8-THC
bull A cannabidiol (the 2nd most abundant psychoactive ingredient after THC)
bull A cannabinol a decomposition product of THC that accumulates as cannabis samples age
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
Therapeutic
bull Antiemeticbull Reduction of intra-ocular tensionbull Analgesicbull Muscle relaxant bull Anti-convulsant bull Anti-inflammatory appetite ldquothe munchiesrdquo It is one of the most well-known effects of marijuana the
powerful surge in appetite many users feel after smoking or ingesting the drug colloquially known as the munchies
Marinol
THC in a sesame oil suspension
Cannabinoid ReceptorsBeforethe 1980s it was often speculated that
cannabinoids produced their effects through non specific interaction with cell membranes instead of interacting with specific receptors
The discovery of the first cannabinoid receptors in the 1980s helped to resolve this debate These receptors are common in animals and have been found in mammals birds fishes and reptiles
There are currently two known types of cannabinoid receptors CB1 and CB2
CB1 ReceptorsFound primarily in the brain (specifically basal ganglia limbic
system including the hippocampus and cerebellum)1048766Most dense in brain regions involved with thinking and memory
attention and control of movement1048766Also present in both male and female reproductive systems as
well as in the lungs liver and kidneys1048766Appear to be responsible for the euphoric and anticonvulsive
effects of Cannabis1048766Essentially absent in the medulla oblongata the part of the brain
that is responsible for respiratory and cardiovascular functions
Thus there is no risk of respiratory or cardiovascular failure as there is with many other drugs
CB2 Receptor
CB2 receptors are almost exclusively found in the immune system (T cells macrophages B cells) with the greatest density in the spleen
1048766CB2 receptors appear to be responsible for the anti-inflammatory and possible other therapeutic effects of Cannabis
1048766Also expressed on peripheral nerve terminals
Cannabis and Δ9- (THC) for weight loss
bull Obesity is one of the highest preventable causes of morbidity and mortality in the developed world It has been well known for a long time that exposure to cannabis produces an increase of appetite (a phenomenon referred to as the munchies) This phenomenon led to an exploration of the role of the endocannabinoid system in the regulation of obesity and associated metabolic syndrome This effort subsequently led to the development of a successful therapeutic approach for obesity that consisted of blocking the cannabinoid CB1 receptors using ligands such as Rimonabant in order to produce weight loss and improve metabolic profile
What is obesity
Obesity is characterized by an abnormal accumulation of body fat usually 20 percent or more over an individuals ideal body weight Obesity results when the size or number of fat cells in a persons body increases When a person gains weight these fat cells first increase in size and later in number When a person starts losing weight the cells decreas ein size but their number generally stays the same This is part of the reason that once you gain a significant amount of weight it is more difficult to lose it
The clinical definition of obesity is a body mass index(BMI)of 30 or higher BMI = Weight (in kg) Height (in meters) Squared
Rimonabant
bull Acompliareg(Sanofi-Aventis)
launched in Europe in 2006 for
oral treatment of obesity at 20 mg
once daily
Selective blocker of central
and peripheral CB1 receptors
It reduces food intake and improves lipid and glucose metabolism
Rimonabant
Despite being efficacious Rimonabant was associated with increased rates of depression and anxiety and therefore removed from the market
- Cannabis
- Slide 2
- Slide 3
- Cannabis spp
- Slide 5
- Slide 6
- Hemp
- What is Marijuana
- Marijuana ndash History of Use
- HempvsMarijuana-1
- HempvsMarijuana-2
- HempvsMarijuana-3
- Cannabis Biology
- Chemical constituents of Cannabis
- What is a cannabinoid
- What are cannabinoids
- Natural cannabinoids
- Slide 18
- Representative cannabinoids
- Slide 20
- Endocannabinoids
- Structure of THC and synthetic analogs
- Slide 23
- Slide 24
- THC
- Results of SAR
- Modes of Absorption
- Smoking and the Body
- Slide 29
- Slide 30
- Metabolites
- Slide 32
- Slide 33
- Cannabis Pharmacology
- Slide 35
- Therapeutic
- Marinol
- Cannabinoid Receptors
- CB1 Receptors
- CB2 Receptor
- Cannabis and Δ9- (THC) for weight loss
- What is obesity
- Slide 43
- Slide 44
- Rimonabant
- Slide 46
- Slide 47
- Slide 48
-
Natural cannabinoids
Representative cannabinoids
Classical cannabinoids Non-classical cannabinoid Aminoalkylindole
CB1 antagonists
Endogenous cannabinoids
Receptors suggest endogenous ligandsTwo main families identifiedBoth arachidonic acid derivativesPrecursors in membranes
ldquoMade on demandrdquoAmides (anandamide)
Esters (2-AG)
bull Significant differences
ndash Routes of synthesis ndash Mode of degradation
(FAAH vs MAGL)ndash Efficacy
Endocannabinoids
bull Anandamide (Sanskrit ananda inner bliss) is one endocannabinoid It is found in chocolate (though there is some controversy over whether the small quantity has any effect on the body) It is about as potent as THC
Structure of THC and synthetic analogs
Lipophilic side chain Most potent analog 100s
times more potent than THC
with 4 major cannabinoids in the plant
bull 2 isomers a trans-delta-9-THC and a delta-8-THC
bull A cannabidiol (the 2nd most abundant psychoactive ingredient after THC)
bull A cannabinol a decomposition product of THC that accumulates as cannabis samples age
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
THC
bull Variedly aromatic ring (C Ring)
O
O
H
11rsquo-di-methyl-pyrane ring (B ring)
Variedly unsaturated cyclohexyl ring (A ring)
Results of SAR
bull Psychoactive properties are (-) trans-enatioselective
bull Length lipophilicity C3 alkyl chain
bull Phenolic hydroxyl-group
bull C9 substitute
O
O
H
Modes of Absorption
bull The most common method of absorption is smoking Either in a loosely rolled cigarette called a joint or through a pipe or water pipe
Smoking and the Body
THC enters the body through the Lungs
The smoke is inhaled and held in the lungsAll affect how much THC will enter the plasmaTHC crosses the blood barrier through the capillaries in the lungs
After inhalation THC can reach the brain in about 14 seconds
After a 6 min smoking period peak blood levels reached at about 7 min (100 ngml plasma)
Most THC is absorbed from the blood within 30 min
Moves rapidly into the brain and across the bloodbrainplacental barrier Because fatty chains make it very lipid soluble
Half-life is about 19 hours Can store in fat cells
Established physiological effects are dose related
Lethal dose for THC use has now been studied and no human deaths have been reported due to intoxication from cannabis
Metabolites
bull Radioactively labeled delta-9-THC has been found to persist in the body as an active metabolite as long as 8 days after use
Primary metabolite has a half-life of 50 hours The complete elimination of the drug can take as long as 6 weeks
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
23 of metabolites are excreted in feces13 of metabolites are excreted in urine
Cannabis Pharmacology
Primary Cannabinoids from Cannabis are
bull Cannabinol (CBN) Cannabidiol (CBD) and Tetrahydrocannabinol (THC)
bull THC (-9-THC ) is the only one with significant psychoactive properties
bull CBN - 110 th activity of THC CBD - none
bull 2 isomers a trans-delta-9-THC and a delta-8-THC
bull A cannabidiol (the 2nd most abundant psychoactive ingredient after THC)
bull A cannabinol a decomposition product of THC that accumulates as cannabis samples age
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
Therapeutic
bull Antiemeticbull Reduction of intra-ocular tensionbull Analgesicbull Muscle relaxant bull Anti-convulsant bull Anti-inflammatory appetite ldquothe munchiesrdquo It is one of the most well-known effects of marijuana the
powerful surge in appetite many users feel after smoking or ingesting the drug colloquially known as the munchies
Marinol
THC in a sesame oil suspension
Cannabinoid ReceptorsBeforethe 1980s it was often speculated that
cannabinoids produced their effects through non specific interaction with cell membranes instead of interacting with specific receptors
The discovery of the first cannabinoid receptors in the 1980s helped to resolve this debate These receptors are common in animals and have been found in mammals birds fishes and reptiles
There are currently two known types of cannabinoid receptors CB1 and CB2
CB1 ReceptorsFound primarily in the brain (specifically basal ganglia limbic
system including the hippocampus and cerebellum)1048766Most dense in brain regions involved with thinking and memory
attention and control of movement1048766Also present in both male and female reproductive systems as
well as in the lungs liver and kidneys1048766Appear to be responsible for the euphoric and anticonvulsive
effects of Cannabis1048766Essentially absent in the medulla oblongata the part of the brain
that is responsible for respiratory and cardiovascular functions
Thus there is no risk of respiratory or cardiovascular failure as there is with many other drugs
CB2 Receptor
CB2 receptors are almost exclusively found in the immune system (T cells macrophages B cells) with the greatest density in the spleen
1048766CB2 receptors appear to be responsible for the anti-inflammatory and possible other therapeutic effects of Cannabis
1048766Also expressed on peripheral nerve terminals
Cannabis and Δ9- (THC) for weight loss
bull Obesity is one of the highest preventable causes of morbidity and mortality in the developed world It has been well known for a long time that exposure to cannabis produces an increase of appetite (a phenomenon referred to as the munchies) This phenomenon led to an exploration of the role of the endocannabinoid system in the regulation of obesity and associated metabolic syndrome This effort subsequently led to the development of a successful therapeutic approach for obesity that consisted of blocking the cannabinoid CB1 receptors using ligands such as Rimonabant in order to produce weight loss and improve metabolic profile
What is obesity
Obesity is characterized by an abnormal accumulation of body fat usually 20 percent or more over an individuals ideal body weight Obesity results when the size or number of fat cells in a persons body increases When a person gains weight these fat cells first increase in size and later in number When a person starts losing weight the cells decreas ein size but their number generally stays the same This is part of the reason that once you gain a significant amount of weight it is more difficult to lose it
The clinical definition of obesity is a body mass index(BMI)of 30 or higher BMI = Weight (in kg) Height (in meters) Squared
Rimonabant
bull Acompliareg(Sanofi-Aventis)
launched in Europe in 2006 for
oral treatment of obesity at 20 mg
once daily
Selective blocker of central
and peripheral CB1 receptors
It reduces food intake and improves lipid and glucose metabolism
Rimonabant
Despite being efficacious Rimonabant was associated with increased rates of depression and anxiety and therefore removed from the market
- Cannabis
- Slide 2
- Slide 3
- Cannabis spp
- Slide 5
- Slide 6
- Hemp
- What is Marijuana
- Marijuana ndash History of Use
- HempvsMarijuana-1
- HempvsMarijuana-2
- HempvsMarijuana-3
- Cannabis Biology
- Chemical constituents of Cannabis
- What is a cannabinoid
- What are cannabinoids
- Natural cannabinoids
- Slide 18
- Representative cannabinoids
- Slide 20
- Endocannabinoids
- Structure of THC and synthetic analogs
- Slide 23
- Slide 24
- THC
- Results of SAR
- Modes of Absorption
- Smoking and the Body
- Slide 29
- Slide 30
- Metabolites
- Slide 32
- Slide 33
- Cannabis Pharmacology
- Slide 35
- Therapeutic
- Marinol
- Cannabinoid Receptors
- CB1 Receptors
- CB2 Receptor
- Cannabis and Δ9- (THC) for weight loss
- What is obesity
- Slide 43
- Slide 44
- Rimonabant
- Slide 46
- Slide 47
- Slide 48
-
Representative cannabinoids
Classical cannabinoids Non-classical cannabinoid Aminoalkylindole
CB1 antagonists
Endogenous cannabinoids
Receptors suggest endogenous ligandsTwo main families identifiedBoth arachidonic acid derivativesPrecursors in membranes
ldquoMade on demandrdquoAmides (anandamide)
Esters (2-AG)
bull Significant differences
ndash Routes of synthesis ndash Mode of degradation
(FAAH vs MAGL)ndash Efficacy
Endocannabinoids
bull Anandamide (Sanskrit ananda inner bliss) is one endocannabinoid It is found in chocolate (though there is some controversy over whether the small quantity has any effect on the body) It is about as potent as THC
Structure of THC and synthetic analogs
Lipophilic side chain Most potent analog 100s
times more potent than THC
with 4 major cannabinoids in the plant
bull 2 isomers a trans-delta-9-THC and a delta-8-THC
bull A cannabidiol (the 2nd most abundant psychoactive ingredient after THC)
bull A cannabinol a decomposition product of THC that accumulates as cannabis samples age
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
THC
bull Variedly aromatic ring (C Ring)
O
O
H
11rsquo-di-methyl-pyrane ring (B ring)
Variedly unsaturated cyclohexyl ring (A ring)
Results of SAR
bull Psychoactive properties are (-) trans-enatioselective
bull Length lipophilicity C3 alkyl chain
bull Phenolic hydroxyl-group
bull C9 substitute
O
O
H
Modes of Absorption
bull The most common method of absorption is smoking Either in a loosely rolled cigarette called a joint or through a pipe or water pipe
Smoking and the Body
THC enters the body through the Lungs
The smoke is inhaled and held in the lungsAll affect how much THC will enter the plasmaTHC crosses the blood barrier through the capillaries in the lungs
After inhalation THC can reach the brain in about 14 seconds
After a 6 min smoking period peak blood levels reached at about 7 min (100 ngml plasma)
Most THC is absorbed from the blood within 30 min
Moves rapidly into the brain and across the bloodbrainplacental barrier Because fatty chains make it very lipid soluble
Half-life is about 19 hours Can store in fat cells
Established physiological effects are dose related
Lethal dose for THC use has now been studied and no human deaths have been reported due to intoxication from cannabis
Metabolites
bull Radioactively labeled delta-9-THC has been found to persist in the body as an active metabolite as long as 8 days after use
Primary metabolite has a half-life of 50 hours The complete elimination of the drug can take as long as 6 weeks
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
23 of metabolites are excreted in feces13 of metabolites are excreted in urine
Cannabis Pharmacology
Primary Cannabinoids from Cannabis are
bull Cannabinol (CBN) Cannabidiol (CBD) and Tetrahydrocannabinol (THC)
bull THC (-9-THC ) is the only one with significant psychoactive properties
bull CBN - 110 th activity of THC CBD - none
bull 2 isomers a trans-delta-9-THC and a delta-8-THC
bull A cannabidiol (the 2nd most abundant psychoactive ingredient after THC)
bull A cannabinol a decomposition product of THC that accumulates as cannabis samples age
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
Therapeutic
bull Antiemeticbull Reduction of intra-ocular tensionbull Analgesicbull Muscle relaxant bull Anti-convulsant bull Anti-inflammatory appetite ldquothe munchiesrdquo It is one of the most well-known effects of marijuana the
powerful surge in appetite many users feel after smoking or ingesting the drug colloquially known as the munchies
Marinol
THC in a sesame oil suspension
Cannabinoid ReceptorsBeforethe 1980s it was often speculated that
cannabinoids produced their effects through non specific interaction with cell membranes instead of interacting with specific receptors
The discovery of the first cannabinoid receptors in the 1980s helped to resolve this debate These receptors are common in animals and have been found in mammals birds fishes and reptiles
There are currently two known types of cannabinoid receptors CB1 and CB2
CB1 ReceptorsFound primarily in the brain (specifically basal ganglia limbic
system including the hippocampus and cerebellum)1048766Most dense in brain regions involved with thinking and memory
attention and control of movement1048766Also present in both male and female reproductive systems as
well as in the lungs liver and kidneys1048766Appear to be responsible for the euphoric and anticonvulsive
effects of Cannabis1048766Essentially absent in the medulla oblongata the part of the brain
that is responsible for respiratory and cardiovascular functions
Thus there is no risk of respiratory or cardiovascular failure as there is with many other drugs
CB2 Receptor
CB2 receptors are almost exclusively found in the immune system (T cells macrophages B cells) with the greatest density in the spleen
1048766CB2 receptors appear to be responsible for the anti-inflammatory and possible other therapeutic effects of Cannabis
1048766Also expressed on peripheral nerve terminals
Cannabis and Δ9- (THC) for weight loss
bull Obesity is one of the highest preventable causes of morbidity and mortality in the developed world It has been well known for a long time that exposure to cannabis produces an increase of appetite (a phenomenon referred to as the munchies) This phenomenon led to an exploration of the role of the endocannabinoid system in the regulation of obesity and associated metabolic syndrome This effort subsequently led to the development of a successful therapeutic approach for obesity that consisted of blocking the cannabinoid CB1 receptors using ligands such as Rimonabant in order to produce weight loss and improve metabolic profile
What is obesity
Obesity is characterized by an abnormal accumulation of body fat usually 20 percent or more over an individuals ideal body weight Obesity results when the size or number of fat cells in a persons body increases When a person gains weight these fat cells first increase in size and later in number When a person starts losing weight the cells decreas ein size but their number generally stays the same This is part of the reason that once you gain a significant amount of weight it is more difficult to lose it
The clinical definition of obesity is a body mass index(BMI)of 30 or higher BMI = Weight (in kg) Height (in meters) Squared
Rimonabant
bull Acompliareg(Sanofi-Aventis)
launched in Europe in 2006 for
oral treatment of obesity at 20 mg
once daily
Selective blocker of central
and peripheral CB1 receptors
It reduces food intake and improves lipid and glucose metabolism
Rimonabant
Despite being efficacious Rimonabant was associated with increased rates of depression and anxiety and therefore removed from the market
- Cannabis
- Slide 2
- Slide 3
- Cannabis spp
- Slide 5
- Slide 6
- Hemp
- What is Marijuana
- Marijuana ndash History of Use
- HempvsMarijuana-1
- HempvsMarijuana-2
- HempvsMarijuana-3
- Cannabis Biology
- Chemical constituents of Cannabis
- What is a cannabinoid
- What are cannabinoids
- Natural cannabinoids
- Slide 18
- Representative cannabinoids
- Slide 20
- Endocannabinoids
- Structure of THC and synthetic analogs
- Slide 23
- Slide 24
- THC
- Results of SAR
- Modes of Absorption
- Smoking and the Body
- Slide 29
- Slide 30
- Metabolites
- Slide 32
- Slide 33
- Cannabis Pharmacology
- Slide 35
- Therapeutic
- Marinol
- Cannabinoid Receptors
- CB1 Receptors
- CB2 Receptor
- Cannabis and Δ9- (THC) for weight loss
- What is obesity
- Slide 43
- Slide 44
- Rimonabant
- Slide 46
- Slide 47
- Slide 48
-
Endogenous cannabinoids
Receptors suggest endogenous ligandsTwo main families identifiedBoth arachidonic acid derivativesPrecursors in membranes
ldquoMade on demandrdquoAmides (anandamide)
Esters (2-AG)
bull Significant differences
ndash Routes of synthesis ndash Mode of degradation
(FAAH vs MAGL)ndash Efficacy
Endocannabinoids
bull Anandamide (Sanskrit ananda inner bliss) is one endocannabinoid It is found in chocolate (though there is some controversy over whether the small quantity has any effect on the body) It is about as potent as THC
Structure of THC and synthetic analogs
Lipophilic side chain Most potent analog 100s
times more potent than THC
with 4 major cannabinoids in the plant
bull 2 isomers a trans-delta-9-THC and a delta-8-THC
bull A cannabidiol (the 2nd most abundant psychoactive ingredient after THC)
bull A cannabinol a decomposition product of THC that accumulates as cannabis samples age
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
THC
bull Variedly aromatic ring (C Ring)
O
O
H
11rsquo-di-methyl-pyrane ring (B ring)
Variedly unsaturated cyclohexyl ring (A ring)
Results of SAR
bull Psychoactive properties are (-) trans-enatioselective
bull Length lipophilicity C3 alkyl chain
bull Phenolic hydroxyl-group
bull C9 substitute
O
O
H
Modes of Absorption
bull The most common method of absorption is smoking Either in a loosely rolled cigarette called a joint or through a pipe or water pipe
Smoking and the Body
THC enters the body through the Lungs
The smoke is inhaled and held in the lungsAll affect how much THC will enter the plasmaTHC crosses the blood barrier through the capillaries in the lungs
After inhalation THC can reach the brain in about 14 seconds
After a 6 min smoking period peak blood levels reached at about 7 min (100 ngml plasma)
Most THC is absorbed from the blood within 30 min
Moves rapidly into the brain and across the bloodbrainplacental barrier Because fatty chains make it very lipid soluble
Half-life is about 19 hours Can store in fat cells
Established physiological effects are dose related
Lethal dose for THC use has now been studied and no human deaths have been reported due to intoxication from cannabis
Metabolites
bull Radioactively labeled delta-9-THC has been found to persist in the body as an active metabolite as long as 8 days after use
Primary metabolite has a half-life of 50 hours The complete elimination of the drug can take as long as 6 weeks
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
23 of metabolites are excreted in feces13 of metabolites are excreted in urine
Cannabis Pharmacology
Primary Cannabinoids from Cannabis are
bull Cannabinol (CBN) Cannabidiol (CBD) and Tetrahydrocannabinol (THC)
bull THC (-9-THC ) is the only one with significant psychoactive properties
bull CBN - 110 th activity of THC CBD - none
bull 2 isomers a trans-delta-9-THC and a delta-8-THC
bull A cannabidiol (the 2nd most abundant psychoactive ingredient after THC)
bull A cannabinol a decomposition product of THC that accumulates as cannabis samples age
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
Therapeutic
bull Antiemeticbull Reduction of intra-ocular tensionbull Analgesicbull Muscle relaxant bull Anti-convulsant bull Anti-inflammatory appetite ldquothe munchiesrdquo It is one of the most well-known effects of marijuana the
powerful surge in appetite many users feel after smoking or ingesting the drug colloquially known as the munchies
Marinol
THC in a sesame oil suspension
Cannabinoid ReceptorsBeforethe 1980s it was often speculated that
cannabinoids produced their effects through non specific interaction with cell membranes instead of interacting with specific receptors
The discovery of the first cannabinoid receptors in the 1980s helped to resolve this debate These receptors are common in animals and have been found in mammals birds fishes and reptiles
There are currently two known types of cannabinoid receptors CB1 and CB2
CB1 ReceptorsFound primarily in the brain (specifically basal ganglia limbic
system including the hippocampus and cerebellum)1048766Most dense in brain regions involved with thinking and memory
attention and control of movement1048766Also present in both male and female reproductive systems as
well as in the lungs liver and kidneys1048766Appear to be responsible for the euphoric and anticonvulsive
effects of Cannabis1048766Essentially absent in the medulla oblongata the part of the brain
that is responsible for respiratory and cardiovascular functions
Thus there is no risk of respiratory or cardiovascular failure as there is with many other drugs
CB2 Receptor
CB2 receptors are almost exclusively found in the immune system (T cells macrophages B cells) with the greatest density in the spleen
1048766CB2 receptors appear to be responsible for the anti-inflammatory and possible other therapeutic effects of Cannabis
1048766Also expressed on peripheral nerve terminals
Cannabis and Δ9- (THC) for weight loss
bull Obesity is one of the highest preventable causes of morbidity and mortality in the developed world It has been well known for a long time that exposure to cannabis produces an increase of appetite (a phenomenon referred to as the munchies) This phenomenon led to an exploration of the role of the endocannabinoid system in the regulation of obesity and associated metabolic syndrome This effort subsequently led to the development of a successful therapeutic approach for obesity that consisted of blocking the cannabinoid CB1 receptors using ligands such as Rimonabant in order to produce weight loss and improve metabolic profile
What is obesity
Obesity is characterized by an abnormal accumulation of body fat usually 20 percent or more over an individuals ideal body weight Obesity results when the size or number of fat cells in a persons body increases When a person gains weight these fat cells first increase in size and later in number When a person starts losing weight the cells decreas ein size but their number generally stays the same This is part of the reason that once you gain a significant amount of weight it is more difficult to lose it
The clinical definition of obesity is a body mass index(BMI)of 30 or higher BMI = Weight (in kg) Height (in meters) Squared
Rimonabant
bull Acompliareg(Sanofi-Aventis)
launched in Europe in 2006 for
oral treatment of obesity at 20 mg
once daily
Selective blocker of central
and peripheral CB1 receptors
It reduces food intake and improves lipid and glucose metabolism
Rimonabant
Despite being efficacious Rimonabant was associated with increased rates of depression and anxiety and therefore removed from the market
- Cannabis
- Slide 2
- Slide 3
- Cannabis spp
- Slide 5
- Slide 6
- Hemp
- What is Marijuana
- Marijuana ndash History of Use
- HempvsMarijuana-1
- HempvsMarijuana-2
- HempvsMarijuana-3
- Cannabis Biology
- Chemical constituents of Cannabis
- What is a cannabinoid
- What are cannabinoids
- Natural cannabinoids
- Slide 18
- Representative cannabinoids
- Slide 20
- Endocannabinoids
- Structure of THC and synthetic analogs
- Slide 23
- Slide 24
- THC
- Results of SAR
- Modes of Absorption
- Smoking and the Body
- Slide 29
- Slide 30
- Metabolites
- Slide 32
- Slide 33
- Cannabis Pharmacology
- Slide 35
- Therapeutic
- Marinol
- Cannabinoid Receptors
- CB1 Receptors
- CB2 Receptor
- Cannabis and Δ9- (THC) for weight loss
- What is obesity
- Slide 43
- Slide 44
- Rimonabant
- Slide 46
- Slide 47
- Slide 48
-
Endocannabinoids
bull Anandamide (Sanskrit ananda inner bliss) is one endocannabinoid It is found in chocolate (though there is some controversy over whether the small quantity has any effect on the body) It is about as potent as THC
Structure of THC and synthetic analogs
Lipophilic side chain Most potent analog 100s
times more potent than THC
with 4 major cannabinoids in the plant
bull 2 isomers a trans-delta-9-THC and a delta-8-THC
bull A cannabidiol (the 2nd most abundant psychoactive ingredient after THC)
bull A cannabinol a decomposition product of THC that accumulates as cannabis samples age
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
THC
bull Variedly aromatic ring (C Ring)
O
O
H
11rsquo-di-methyl-pyrane ring (B ring)
Variedly unsaturated cyclohexyl ring (A ring)
Results of SAR
bull Psychoactive properties are (-) trans-enatioselective
bull Length lipophilicity C3 alkyl chain
bull Phenolic hydroxyl-group
bull C9 substitute
O
O
H
Modes of Absorption
bull The most common method of absorption is smoking Either in a loosely rolled cigarette called a joint or through a pipe or water pipe
Smoking and the Body
THC enters the body through the Lungs
The smoke is inhaled and held in the lungsAll affect how much THC will enter the plasmaTHC crosses the blood barrier through the capillaries in the lungs
After inhalation THC can reach the brain in about 14 seconds
After a 6 min smoking period peak blood levels reached at about 7 min (100 ngml plasma)
Most THC is absorbed from the blood within 30 min
Moves rapidly into the brain and across the bloodbrainplacental barrier Because fatty chains make it very lipid soluble
Half-life is about 19 hours Can store in fat cells
Established physiological effects are dose related
Lethal dose for THC use has now been studied and no human deaths have been reported due to intoxication from cannabis
Metabolites
bull Radioactively labeled delta-9-THC has been found to persist in the body as an active metabolite as long as 8 days after use
Primary metabolite has a half-life of 50 hours The complete elimination of the drug can take as long as 6 weeks
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
23 of metabolites are excreted in feces13 of metabolites are excreted in urine
Cannabis Pharmacology
Primary Cannabinoids from Cannabis are
bull Cannabinol (CBN) Cannabidiol (CBD) and Tetrahydrocannabinol (THC)
bull THC (-9-THC ) is the only one with significant psychoactive properties
bull CBN - 110 th activity of THC CBD - none
bull 2 isomers a trans-delta-9-THC and a delta-8-THC
bull A cannabidiol (the 2nd most abundant psychoactive ingredient after THC)
bull A cannabinol a decomposition product of THC that accumulates as cannabis samples age
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
Therapeutic
bull Antiemeticbull Reduction of intra-ocular tensionbull Analgesicbull Muscle relaxant bull Anti-convulsant bull Anti-inflammatory appetite ldquothe munchiesrdquo It is one of the most well-known effects of marijuana the
powerful surge in appetite many users feel after smoking or ingesting the drug colloquially known as the munchies
Marinol
THC in a sesame oil suspension
Cannabinoid ReceptorsBeforethe 1980s it was often speculated that
cannabinoids produced their effects through non specific interaction with cell membranes instead of interacting with specific receptors
The discovery of the first cannabinoid receptors in the 1980s helped to resolve this debate These receptors are common in animals and have been found in mammals birds fishes and reptiles
There are currently two known types of cannabinoid receptors CB1 and CB2
CB1 ReceptorsFound primarily in the brain (specifically basal ganglia limbic
system including the hippocampus and cerebellum)1048766Most dense in brain regions involved with thinking and memory
attention and control of movement1048766Also present in both male and female reproductive systems as
well as in the lungs liver and kidneys1048766Appear to be responsible for the euphoric and anticonvulsive
effects of Cannabis1048766Essentially absent in the medulla oblongata the part of the brain
that is responsible for respiratory and cardiovascular functions
Thus there is no risk of respiratory or cardiovascular failure as there is with many other drugs
CB2 Receptor
CB2 receptors are almost exclusively found in the immune system (T cells macrophages B cells) with the greatest density in the spleen
1048766CB2 receptors appear to be responsible for the anti-inflammatory and possible other therapeutic effects of Cannabis
1048766Also expressed on peripheral nerve terminals
Cannabis and Δ9- (THC) for weight loss
bull Obesity is one of the highest preventable causes of morbidity and mortality in the developed world It has been well known for a long time that exposure to cannabis produces an increase of appetite (a phenomenon referred to as the munchies) This phenomenon led to an exploration of the role of the endocannabinoid system in the regulation of obesity and associated metabolic syndrome This effort subsequently led to the development of a successful therapeutic approach for obesity that consisted of blocking the cannabinoid CB1 receptors using ligands such as Rimonabant in order to produce weight loss and improve metabolic profile
What is obesity
Obesity is characterized by an abnormal accumulation of body fat usually 20 percent or more over an individuals ideal body weight Obesity results when the size or number of fat cells in a persons body increases When a person gains weight these fat cells first increase in size and later in number When a person starts losing weight the cells decreas ein size but their number generally stays the same This is part of the reason that once you gain a significant amount of weight it is more difficult to lose it
The clinical definition of obesity is a body mass index(BMI)of 30 or higher BMI = Weight (in kg) Height (in meters) Squared
Rimonabant
bull Acompliareg(Sanofi-Aventis)
launched in Europe in 2006 for
oral treatment of obesity at 20 mg
once daily
Selective blocker of central
and peripheral CB1 receptors
It reduces food intake and improves lipid and glucose metabolism
Rimonabant
Despite being efficacious Rimonabant was associated with increased rates of depression and anxiety and therefore removed from the market
- Cannabis
- Slide 2
- Slide 3
- Cannabis spp
- Slide 5
- Slide 6
- Hemp
- What is Marijuana
- Marijuana ndash History of Use
- HempvsMarijuana-1
- HempvsMarijuana-2
- HempvsMarijuana-3
- Cannabis Biology
- Chemical constituents of Cannabis
- What is a cannabinoid
- What are cannabinoids
- Natural cannabinoids
- Slide 18
- Representative cannabinoids
- Slide 20
- Endocannabinoids
- Structure of THC and synthetic analogs
- Slide 23
- Slide 24
- THC
- Results of SAR
- Modes of Absorption
- Smoking and the Body
- Slide 29
- Slide 30
- Metabolites
- Slide 32
- Slide 33
- Cannabis Pharmacology
- Slide 35
- Therapeutic
- Marinol
- Cannabinoid Receptors
- CB1 Receptors
- CB2 Receptor
- Cannabis and Δ9- (THC) for weight loss
- What is obesity
- Slide 43
- Slide 44
- Rimonabant
- Slide 46
- Slide 47
- Slide 48
-
Structure of THC and synthetic analogs
Lipophilic side chain Most potent analog 100s
times more potent than THC
with 4 major cannabinoids in the plant
bull 2 isomers a trans-delta-9-THC and a delta-8-THC
bull A cannabidiol (the 2nd most abundant psychoactive ingredient after THC)
bull A cannabinol a decomposition product of THC that accumulates as cannabis samples age
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
THC
bull Variedly aromatic ring (C Ring)
O
O
H
11rsquo-di-methyl-pyrane ring (B ring)
Variedly unsaturated cyclohexyl ring (A ring)
Results of SAR
bull Psychoactive properties are (-) trans-enatioselective
bull Length lipophilicity C3 alkyl chain
bull Phenolic hydroxyl-group
bull C9 substitute
O
O
H
Modes of Absorption
bull The most common method of absorption is smoking Either in a loosely rolled cigarette called a joint or through a pipe or water pipe
Smoking and the Body
THC enters the body through the Lungs
The smoke is inhaled and held in the lungsAll affect how much THC will enter the plasmaTHC crosses the blood barrier through the capillaries in the lungs
After inhalation THC can reach the brain in about 14 seconds
After a 6 min smoking period peak blood levels reached at about 7 min (100 ngml plasma)
Most THC is absorbed from the blood within 30 min
Moves rapidly into the brain and across the bloodbrainplacental barrier Because fatty chains make it very lipid soluble
Half-life is about 19 hours Can store in fat cells
Established physiological effects are dose related
Lethal dose for THC use has now been studied and no human deaths have been reported due to intoxication from cannabis
Metabolites
bull Radioactively labeled delta-9-THC has been found to persist in the body as an active metabolite as long as 8 days after use
Primary metabolite has a half-life of 50 hours The complete elimination of the drug can take as long as 6 weeks
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
23 of metabolites are excreted in feces13 of metabolites are excreted in urine
Cannabis Pharmacology
Primary Cannabinoids from Cannabis are
bull Cannabinol (CBN) Cannabidiol (CBD) and Tetrahydrocannabinol (THC)
bull THC (-9-THC ) is the only one with significant psychoactive properties
bull CBN - 110 th activity of THC CBD - none
bull 2 isomers a trans-delta-9-THC and a delta-8-THC
bull A cannabidiol (the 2nd most abundant psychoactive ingredient after THC)
bull A cannabinol a decomposition product of THC that accumulates as cannabis samples age
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
Therapeutic
bull Antiemeticbull Reduction of intra-ocular tensionbull Analgesicbull Muscle relaxant bull Anti-convulsant bull Anti-inflammatory appetite ldquothe munchiesrdquo It is one of the most well-known effects of marijuana the
powerful surge in appetite many users feel after smoking or ingesting the drug colloquially known as the munchies
Marinol
THC in a sesame oil suspension
Cannabinoid ReceptorsBeforethe 1980s it was often speculated that
cannabinoids produced their effects through non specific interaction with cell membranes instead of interacting with specific receptors
The discovery of the first cannabinoid receptors in the 1980s helped to resolve this debate These receptors are common in animals and have been found in mammals birds fishes and reptiles
There are currently two known types of cannabinoid receptors CB1 and CB2
CB1 ReceptorsFound primarily in the brain (specifically basal ganglia limbic
system including the hippocampus and cerebellum)1048766Most dense in brain regions involved with thinking and memory
attention and control of movement1048766Also present in both male and female reproductive systems as
well as in the lungs liver and kidneys1048766Appear to be responsible for the euphoric and anticonvulsive
effects of Cannabis1048766Essentially absent in the medulla oblongata the part of the brain
that is responsible for respiratory and cardiovascular functions
Thus there is no risk of respiratory or cardiovascular failure as there is with many other drugs
CB2 Receptor
CB2 receptors are almost exclusively found in the immune system (T cells macrophages B cells) with the greatest density in the spleen
1048766CB2 receptors appear to be responsible for the anti-inflammatory and possible other therapeutic effects of Cannabis
1048766Also expressed on peripheral nerve terminals
Cannabis and Δ9- (THC) for weight loss
bull Obesity is one of the highest preventable causes of morbidity and mortality in the developed world It has been well known for a long time that exposure to cannabis produces an increase of appetite (a phenomenon referred to as the munchies) This phenomenon led to an exploration of the role of the endocannabinoid system in the regulation of obesity and associated metabolic syndrome This effort subsequently led to the development of a successful therapeutic approach for obesity that consisted of blocking the cannabinoid CB1 receptors using ligands such as Rimonabant in order to produce weight loss and improve metabolic profile
What is obesity
Obesity is characterized by an abnormal accumulation of body fat usually 20 percent or more over an individuals ideal body weight Obesity results when the size or number of fat cells in a persons body increases When a person gains weight these fat cells first increase in size and later in number When a person starts losing weight the cells decreas ein size but their number generally stays the same This is part of the reason that once you gain a significant amount of weight it is more difficult to lose it
The clinical definition of obesity is a body mass index(BMI)of 30 or higher BMI = Weight (in kg) Height (in meters) Squared
Rimonabant
bull Acompliareg(Sanofi-Aventis)
launched in Europe in 2006 for
oral treatment of obesity at 20 mg
once daily
Selective blocker of central
and peripheral CB1 receptors
It reduces food intake and improves lipid and glucose metabolism
Rimonabant
Despite being efficacious Rimonabant was associated with increased rates of depression and anxiety and therefore removed from the market
- Cannabis
- Slide 2
- Slide 3
- Cannabis spp
- Slide 5
- Slide 6
- Hemp
- What is Marijuana
- Marijuana ndash History of Use
- HempvsMarijuana-1
- HempvsMarijuana-2
- HempvsMarijuana-3
- Cannabis Biology
- Chemical constituents of Cannabis
- What is a cannabinoid
- What are cannabinoids
- Natural cannabinoids
- Slide 18
- Representative cannabinoids
- Slide 20
- Endocannabinoids
- Structure of THC and synthetic analogs
- Slide 23
- Slide 24
- THC
- Results of SAR
- Modes of Absorption
- Smoking and the Body
- Slide 29
- Slide 30
- Metabolites
- Slide 32
- Slide 33
- Cannabis Pharmacology
- Slide 35
- Therapeutic
- Marinol
- Cannabinoid Receptors
- CB1 Receptors
- CB2 Receptor
- Cannabis and Δ9- (THC) for weight loss
- What is obesity
- Slide 43
- Slide 44
- Rimonabant
- Slide 46
- Slide 47
- Slide 48
-
with 4 major cannabinoids in the plant
bull 2 isomers a trans-delta-9-THC and a delta-8-THC
bull A cannabidiol (the 2nd most abundant psychoactive ingredient after THC)
bull A cannabinol a decomposition product of THC that accumulates as cannabis samples age
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
THC
bull Variedly aromatic ring (C Ring)
O
O
H
11rsquo-di-methyl-pyrane ring (B ring)
Variedly unsaturated cyclohexyl ring (A ring)
Results of SAR
bull Psychoactive properties are (-) trans-enatioselective
bull Length lipophilicity C3 alkyl chain
bull Phenolic hydroxyl-group
bull C9 substitute
O
O
H
Modes of Absorption
bull The most common method of absorption is smoking Either in a loosely rolled cigarette called a joint or through a pipe or water pipe
Smoking and the Body
THC enters the body through the Lungs
The smoke is inhaled and held in the lungsAll affect how much THC will enter the plasmaTHC crosses the blood barrier through the capillaries in the lungs
After inhalation THC can reach the brain in about 14 seconds
After a 6 min smoking period peak blood levels reached at about 7 min (100 ngml plasma)
Most THC is absorbed from the blood within 30 min
Moves rapidly into the brain and across the bloodbrainplacental barrier Because fatty chains make it very lipid soluble
Half-life is about 19 hours Can store in fat cells
Established physiological effects are dose related
Lethal dose for THC use has now been studied and no human deaths have been reported due to intoxication from cannabis
Metabolites
bull Radioactively labeled delta-9-THC has been found to persist in the body as an active metabolite as long as 8 days after use
Primary metabolite has a half-life of 50 hours The complete elimination of the drug can take as long as 6 weeks
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
23 of metabolites are excreted in feces13 of metabolites are excreted in urine
Cannabis Pharmacology
Primary Cannabinoids from Cannabis are
bull Cannabinol (CBN) Cannabidiol (CBD) and Tetrahydrocannabinol (THC)
bull THC (-9-THC ) is the only one with significant psychoactive properties
bull CBN - 110 th activity of THC CBD - none
bull 2 isomers a trans-delta-9-THC and a delta-8-THC
bull A cannabidiol (the 2nd most abundant psychoactive ingredient after THC)
bull A cannabinol a decomposition product of THC that accumulates as cannabis samples age
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
Therapeutic
bull Antiemeticbull Reduction of intra-ocular tensionbull Analgesicbull Muscle relaxant bull Anti-convulsant bull Anti-inflammatory appetite ldquothe munchiesrdquo It is one of the most well-known effects of marijuana the
powerful surge in appetite many users feel after smoking or ingesting the drug colloquially known as the munchies
Marinol
THC in a sesame oil suspension
Cannabinoid ReceptorsBeforethe 1980s it was often speculated that
cannabinoids produced their effects through non specific interaction with cell membranes instead of interacting with specific receptors
The discovery of the first cannabinoid receptors in the 1980s helped to resolve this debate These receptors are common in animals and have been found in mammals birds fishes and reptiles
There are currently two known types of cannabinoid receptors CB1 and CB2
CB1 ReceptorsFound primarily in the brain (specifically basal ganglia limbic
system including the hippocampus and cerebellum)1048766Most dense in brain regions involved with thinking and memory
attention and control of movement1048766Also present in both male and female reproductive systems as
well as in the lungs liver and kidneys1048766Appear to be responsible for the euphoric and anticonvulsive
effects of Cannabis1048766Essentially absent in the medulla oblongata the part of the brain
that is responsible for respiratory and cardiovascular functions
Thus there is no risk of respiratory or cardiovascular failure as there is with many other drugs
CB2 Receptor
CB2 receptors are almost exclusively found in the immune system (T cells macrophages B cells) with the greatest density in the spleen
1048766CB2 receptors appear to be responsible for the anti-inflammatory and possible other therapeutic effects of Cannabis
1048766Also expressed on peripheral nerve terminals
Cannabis and Δ9- (THC) for weight loss
bull Obesity is one of the highest preventable causes of morbidity and mortality in the developed world It has been well known for a long time that exposure to cannabis produces an increase of appetite (a phenomenon referred to as the munchies) This phenomenon led to an exploration of the role of the endocannabinoid system in the regulation of obesity and associated metabolic syndrome This effort subsequently led to the development of a successful therapeutic approach for obesity that consisted of blocking the cannabinoid CB1 receptors using ligands such as Rimonabant in order to produce weight loss and improve metabolic profile
What is obesity
Obesity is characterized by an abnormal accumulation of body fat usually 20 percent or more over an individuals ideal body weight Obesity results when the size or number of fat cells in a persons body increases When a person gains weight these fat cells first increase in size and later in number When a person starts losing weight the cells decreas ein size but their number generally stays the same This is part of the reason that once you gain a significant amount of weight it is more difficult to lose it
The clinical definition of obesity is a body mass index(BMI)of 30 or higher BMI = Weight (in kg) Height (in meters) Squared
Rimonabant
bull Acompliareg(Sanofi-Aventis)
launched in Europe in 2006 for
oral treatment of obesity at 20 mg
once daily
Selective blocker of central
and peripheral CB1 receptors
It reduces food intake and improves lipid and glucose metabolism
Rimonabant
Despite being efficacious Rimonabant was associated with increased rates of depression and anxiety and therefore removed from the market
- Cannabis
- Slide 2
- Slide 3
- Cannabis spp
- Slide 5
- Slide 6
- Hemp
- What is Marijuana
- Marijuana ndash History of Use
- HempvsMarijuana-1
- HempvsMarijuana-2
- HempvsMarijuana-3
- Cannabis Biology
- Chemical constituents of Cannabis
- What is a cannabinoid
- What are cannabinoids
- Natural cannabinoids
- Slide 18
- Representative cannabinoids
- Slide 20
- Endocannabinoids
- Structure of THC and synthetic analogs
- Slide 23
- Slide 24
- THC
- Results of SAR
- Modes of Absorption
- Smoking and the Body
- Slide 29
- Slide 30
- Metabolites
- Slide 32
- Slide 33
- Cannabis Pharmacology
- Slide 35
- Therapeutic
- Marinol
- Cannabinoid Receptors
- CB1 Receptors
- CB2 Receptor
- Cannabis and Δ9- (THC) for weight loss
- What is obesity
- Slide 43
- Slide 44
- Rimonabant
- Slide 46
- Slide 47
- Slide 48
-
THC
bull Variedly aromatic ring (C Ring)
O
O
H
11rsquo-di-methyl-pyrane ring (B ring)
Variedly unsaturated cyclohexyl ring (A ring)
Results of SAR
bull Psychoactive properties are (-) trans-enatioselective
bull Length lipophilicity C3 alkyl chain
bull Phenolic hydroxyl-group
bull C9 substitute
O
O
H
Modes of Absorption
bull The most common method of absorption is smoking Either in a loosely rolled cigarette called a joint or through a pipe or water pipe
Smoking and the Body
THC enters the body through the Lungs
The smoke is inhaled and held in the lungsAll affect how much THC will enter the plasmaTHC crosses the blood barrier through the capillaries in the lungs
After inhalation THC can reach the brain in about 14 seconds
After a 6 min smoking period peak blood levels reached at about 7 min (100 ngml plasma)
Most THC is absorbed from the blood within 30 min
Moves rapidly into the brain and across the bloodbrainplacental barrier Because fatty chains make it very lipid soluble
Half-life is about 19 hours Can store in fat cells
Established physiological effects are dose related
Lethal dose for THC use has now been studied and no human deaths have been reported due to intoxication from cannabis
Metabolites
bull Radioactively labeled delta-9-THC has been found to persist in the body as an active metabolite as long as 8 days after use
Primary metabolite has a half-life of 50 hours The complete elimination of the drug can take as long as 6 weeks
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
23 of metabolites are excreted in feces13 of metabolites are excreted in urine
Cannabis Pharmacology
Primary Cannabinoids from Cannabis are
bull Cannabinol (CBN) Cannabidiol (CBD) and Tetrahydrocannabinol (THC)
bull THC (-9-THC ) is the only one with significant psychoactive properties
bull CBN - 110 th activity of THC CBD - none
bull 2 isomers a trans-delta-9-THC and a delta-8-THC
bull A cannabidiol (the 2nd most abundant psychoactive ingredient after THC)
bull A cannabinol a decomposition product of THC that accumulates as cannabis samples age
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
Therapeutic
bull Antiemeticbull Reduction of intra-ocular tensionbull Analgesicbull Muscle relaxant bull Anti-convulsant bull Anti-inflammatory appetite ldquothe munchiesrdquo It is one of the most well-known effects of marijuana the
powerful surge in appetite many users feel after smoking or ingesting the drug colloquially known as the munchies
Marinol
THC in a sesame oil suspension
Cannabinoid ReceptorsBeforethe 1980s it was often speculated that
cannabinoids produced their effects through non specific interaction with cell membranes instead of interacting with specific receptors
The discovery of the first cannabinoid receptors in the 1980s helped to resolve this debate These receptors are common in animals and have been found in mammals birds fishes and reptiles
There are currently two known types of cannabinoid receptors CB1 and CB2
CB1 ReceptorsFound primarily in the brain (specifically basal ganglia limbic
system including the hippocampus and cerebellum)1048766Most dense in brain regions involved with thinking and memory
attention and control of movement1048766Also present in both male and female reproductive systems as
well as in the lungs liver and kidneys1048766Appear to be responsible for the euphoric and anticonvulsive
effects of Cannabis1048766Essentially absent in the medulla oblongata the part of the brain
that is responsible for respiratory and cardiovascular functions
Thus there is no risk of respiratory or cardiovascular failure as there is with many other drugs
CB2 Receptor
CB2 receptors are almost exclusively found in the immune system (T cells macrophages B cells) with the greatest density in the spleen
1048766CB2 receptors appear to be responsible for the anti-inflammatory and possible other therapeutic effects of Cannabis
1048766Also expressed on peripheral nerve terminals
Cannabis and Δ9- (THC) for weight loss
bull Obesity is one of the highest preventable causes of morbidity and mortality in the developed world It has been well known for a long time that exposure to cannabis produces an increase of appetite (a phenomenon referred to as the munchies) This phenomenon led to an exploration of the role of the endocannabinoid system in the regulation of obesity and associated metabolic syndrome This effort subsequently led to the development of a successful therapeutic approach for obesity that consisted of blocking the cannabinoid CB1 receptors using ligands such as Rimonabant in order to produce weight loss and improve metabolic profile
What is obesity
Obesity is characterized by an abnormal accumulation of body fat usually 20 percent or more over an individuals ideal body weight Obesity results when the size or number of fat cells in a persons body increases When a person gains weight these fat cells first increase in size and later in number When a person starts losing weight the cells decreas ein size but their number generally stays the same This is part of the reason that once you gain a significant amount of weight it is more difficult to lose it
The clinical definition of obesity is a body mass index(BMI)of 30 or higher BMI = Weight (in kg) Height (in meters) Squared
Rimonabant
bull Acompliareg(Sanofi-Aventis)
launched in Europe in 2006 for
oral treatment of obesity at 20 mg
once daily
Selective blocker of central
and peripheral CB1 receptors
It reduces food intake and improves lipid and glucose metabolism
Rimonabant
Despite being efficacious Rimonabant was associated with increased rates of depression and anxiety and therefore removed from the market
- Cannabis
- Slide 2
- Slide 3
- Cannabis spp
- Slide 5
- Slide 6
- Hemp
- What is Marijuana
- Marijuana ndash History of Use
- HempvsMarijuana-1
- HempvsMarijuana-2
- HempvsMarijuana-3
- Cannabis Biology
- Chemical constituents of Cannabis
- What is a cannabinoid
- What are cannabinoids
- Natural cannabinoids
- Slide 18
- Representative cannabinoids
- Slide 20
- Endocannabinoids
- Structure of THC and synthetic analogs
- Slide 23
- Slide 24
- THC
- Results of SAR
- Modes of Absorption
- Smoking and the Body
- Slide 29
- Slide 30
- Metabolites
- Slide 32
- Slide 33
- Cannabis Pharmacology
- Slide 35
- Therapeutic
- Marinol
- Cannabinoid Receptors
- CB1 Receptors
- CB2 Receptor
- Cannabis and Δ9- (THC) for weight loss
- What is obesity
- Slide 43
- Slide 44
- Rimonabant
- Slide 46
- Slide 47
- Slide 48
-
Results of SAR
bull Psychoactive properties are (-) trans-enatioselective
bull Length lipophilicity C3 alkyl chain
bull Phenolic hydroxyl-group
bull C9 substitute
O
O
H
Modes of Absorption
bull The most common method of absorption is smoking Either in a loosely rolled cigarette called a joint or through a pipe or water pipe
Smoking and the Body
THC enters the body through the Lungs
The smoke is inhaled and held in the lungsAll affect how much THC will enter the plasmaTHC crosses the blood barrier through the capillaries in the lungs
After inhalation THC can reach the brain in about 14 seconds
After a 6 min smoking period peak blood levels reached at about 7 min (100 ngml plasma)
Most THC is absorbed from the blood within 30 min
Moves rapidly into the brain and across the bloodbrainplacental barrier Because fatty chains make it very lipid soluble
Half-life is about 19 hours Can store in fat cells
Established physiological effects are dose related
Lethal dose for THC use has now been studied and no human deaths have been reported due to intoxication from cannabis
Metabolites
bull Radioactively labeled delta-9-THC has been found to persist in the body as an active metabolite as long as 8 days after use
Primary metabolite has a half-life of 50 hours The complete elimination of the drug can take as long as 6 weeks
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
23 of metabolites are excreted in feces13 of metabolites are excreted in urine
Cannabis Pharmacology
Primary Cannabinoids from Cannabis are
bull Cannabinol (CBN) Cannabidiol (CBD) and Tetrahydrocannabinol (THC)
bull THC (-9-THC ) is the only one with significant psychoactive properties
bull CBN - 110 th activity of THC CBD - none
bull 2 isomers a trans-delta-9-THC and a delta-8-THC
bull A cannabidiol (the 2nd most abundant psychoactive ingredient after THC)
bull A cannabinol a decomposition product of THC that accumulates as cannabis samples age
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
Therapeutic
bull Antiemeticbull Reduction of intra-ocular tensionbull Analgesicbull Muscle relaxant bull Anti-convulsant bull Anti-inflammatory appetite ldquothe munchiesrdquo It is one of the most well-known effects of marijuana the
powerful surge in appetite many users feel after smoking or ingesting the drug colloquially known as the munchies
Marinol
THC in a sesame oil suspension
Cannabinoid ReceptorsBeforethe 1980s it was often speculated that
cannabinoids produced their effects through non specific interaction with cell membranes instead of interacting with specific receptors
The discovery of the first cannabinoid receptors in the 1980s helped to resolve this debate These receptors are common in animals and have been found in mammals birds fishes and reptiles
There are currently two known types of cannabinoid receptors CB1 and CB2
CB1 ReceptorsFound primarily in the brain (specifically basal ganglia limbic
system including the hippocampus and cerebellum)1048766Most dense in brain regions involved with thinking and memory
attention and control of movement1048766Also present in both male and female reproductive systems as
well as in the lungs liver and kidneys1048766Appear to be responsible for the euphoric and anticonvulsive
effects of Cannabis1048766Essentially absent in the medulla oblongata the part of the brain
that is responsible for respiratory and cardiovascular functions
Thus there is no risk of respiratory or cardiovascular failure as there is with many other drugs
CB2 Receptor
CB2 receptors are almost exclusively found in the immune system (T cells macrophages B cells) with the greatest density in the spleen
1048766CB2 receptors appear to be responsible for the anti-inflammatory and possible other therapeutic effects of Cannabis
1048766Also expressed on peripheral nerve terminals
Cannabis and Δ9- (THC) for weight loss
bull Obesity is one of the highest preventable causes of morbidity and mortality in the developed world It has been well known for a long time that exposure to cannabis produces an increase of appetite (a phenomenon referred to as the munchies) This phenomenon led to an exploration of the role of the endocannabinoid system in the regulation of obesity and associated metabolic syndrome This effort subsequently led to the development of a successful therapeutic approach for obesity that consisted of blocking the cannabinoid CB1 receptors using ligands such as Rimonabant in order to produce weight loss and improve metabolic profile
What is obesity
Obesity is characterized by an abnormal accumulation of body fat usually 20 percent or more over an individuals ideal body weight Obesity results when the size or number of fat cells in a persons body increases When a person gains weight these fat cells first increase in size and later in number When a person starts losing weight the cells decreas ein size but their number generally stays the same This is part of the reason that once you gain a significant amount of weight it is more difficult to lose it
The clinical definition of obesity is a body mass index(BMI)of 30 or higher BMI = Weight (in kg) Height (in meters) Squared
Rimonabant
bull Acompliareg(Sanofi-Aventis)
launched in Europe in 2006 for
oral treatment of obesity at 20 mg
once daily
Selective blocker of central
and peripheral CB1 receptors
It reduces food intake and improves lipid and glucose metabolism
Rimonabant
Despite being efficacious Rimonabant was associated with increased rates of depression and anxiety and therefore removed from the market
- Cannabis
- Slide 2
- Slide 3
- Cannabis spp
- Slide 5
- Slide 6
- Hemp
- What is Marijuana
- Marijuana ndash History of Use
- HempvsMarijuana-1
- HempvsMarijuana-2
- HempvsMarijuana-3
- Cannabis Biology
- Chemical constituents of Cannabis
- What is a cannabinoid
- What are cannabinoids
- Natural cannabinoids
- Slide 18
- Representative cannabinoids
- Slide 20
- Endocannabinoids
- Structure of THC and synthetic analogs
- Slide 23
- Slide 24
- THC
- Results of SAR
- Modes of Absorption
- Smoking and the Body
- Slide 29
- Slide 30
- Metabolites
- Slide 32
- Slide 33
- Cannabis Pharmacology
- Slide 35
- Therapeutic
- Marinol
- Cannabinoid Receptors
- CB1 Receptors
- CB2 Receptor
- Cannabis and Δ9- (THC) for weight loss
- What is obesity
- Slide 43
- Slide 44
- Rimonabant
- Slide 46
- Slide 47
- Slide 48
-
Modes of Absorption
bull The most common method of absorption is smoking Either in a loosely rolled cigarette called a joint or through a pipe or water pipe
Smoking and the Body
THC enters the body through the Lungs
The smoke is inhaled and held in the lungsAll affect how much THC will enter the plasmaTHC crosses the blood barrier through the capillaries in the lungs
After inhalation THC can reach the brain in about 14 seconds
After a 6 min smoking period peak blood levels reached at about 7 min (100 ngml plasma)
Most THC is absorbed from the blood within 30 min
Moves rapidly into the brain and across the bloodbrainplacental barrier Because fatty chains make it very lipid soluble
Half-life is about 19 hours Can store in fat cells
Established physiological effects are dose related
Lethal dose for THC use has now been studied and no human deaths have been reported due to intoxication from cannabis
Metabolites
bull Radioactively labeled delta-9-THC has been found to persist in the body as an active metabolite as long as 8 days after use
Primary metabolite has a half-life of 50 hours The complete elimination of the drug can take as long as 6 weeks
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
23 of metabolites are excreted in feces13 of metabolites are excreted in urine
Cannabis Pharmacology
Primary Cannabinoids from Cannabis are
bull Cannabinol (CBN) Cannabidiol (CBD) and Tetrahydrocannabinol (THC)
bull THC (-9-THC ) is the only one with significant psychoactive properties
bull CBN - 110 th activity of THC CBD - none
bull 2 isomers a trans-delta-9-THC and a delta-8-THC
bull A cannabidiol (the 2nd most abundant psychoactive ingredient after THC)
bull A cannabinol a decomposition product of THC that accumulates as cannabis samples age
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
Therapeutic
bull Antiemeticbull Reduction of intra-ocular tensionbull Analgesicbull Muscle relaxant bull Anti-convulsant bull Anti-inflammatory appetite ldquothe munchiesrdquo It is one of the most well-known effects of marijuana the
powerful surge in appetite many users feel after smoking or ingesting the drug colloquially known as the munchies
Marinol
THC in a sesame oil suspension
Cannabinoid ReceptorsBeforethe 1980s it was often speculated that
cannabinoids produced their effects through non specific interaction with cell membranes instead of interacting with specific receptors
The discovery of the first cannabinoid receptors in the 1980s helped to resolve this debate These receptors are common in animals and have been found in mammals birds fishes and reptiles
There are currently two known types of cannabinoid receptors CB1 and CB2
CB1 ReceptorsFound primarily in the brain (specifically basal ganglia limbic
system including the hippocampus and cerebellum)1048766Most dense in brain regions involved with thinking and memory
attention and control of movement1048766Also present in both male and female reproductive systems as
well as in the lungs liver and kidneys1048766Appear to be responsible for the euphoric and anticonvulsive
effects of Cannabis1048766Essentially absent in the medulla oblongata the part of the brain
that is responsible for respiratory and cardiovascular functions
Thus there is no risk of respiratory or cardiovascular failure as there is with many other drugs
CB2 Receptor
CB2 receptors are almost exclusively found in the immune system (T cells macrophages B cells) with the greatest density in the spleen
1048766CB2 receptors appear to be responsible for the anti-inflammatory and possible other therapeutic effects of Cannabis
1048766Also expressed on peripheral nerve terminals
Cannabis and Δ9- (THC) for weight loss
bull Obesity is one of the highest preventable causes of morbidity and mortality in the developed world It has been well known for a long time that exposure to cannabis produces an increase of appetite (a phenomenon referred to as the munchies) This phenomenon led to an exploration of the role of the endocannabinoid system in the regulation of obesity and associated metabolic syndrome This effort subsequently led to the development of a successful therapeutic approach for obesity that consisted of blocking the cannabinoid CB1 receptors using ligands such as Rimonabant in order to produce weight loss and improve metabolic profile
What is obesity
Obesity is characterized by an abnormal accumulation of body fat usually 20 percent or more over an individuals ideal body weight Obesity results when the size or number of fat cells in a persons body increases When a person gains weight these fat cells first increase in size and later in number When a person starts losing weight the cells decreas ein size but their number generally stays the same This is part of the reason that once you gain a significant amount of weight it is more difficult to lose it
The clinical definition of obesity is a body mass index(BMI)of 30 or higher BMI = Weight (in kg) Height (in meters) Squared
Rimonabant
bull Acompliareg(Sanofi-Aventis)
launched in Europe in 2006 for
oral treatment of obesity at 20 mg
once daily
Selective blocker of central
and peripheral CB1 receptors
It reduces food intake and improves lipid and glucose metabolism
Rimonabant
Despite being efficacious Rimonabant was associated with increased rates of depression and anxiety and therefore removed from the market
- Cannabis
- Slide 2
- Slide 3
- Cannabis spp
- Slide 5
- Slide 6
- Hemp
- What is Marijuana
- Marijuana ndash History of Use
- HempvsMarijuana-1
- HempvsMarijuana-2
- HempvsMarijuana-3
- Cannabis Biology
- Chemical constituents of Cannabis
- What is a cannabinoid
- What are cannabinoids
- Natural cannabinoids
- Slide 18
- Representative cannabinoids
- Slide 20
- Endocannabinoids
- Structure of THC and synthetic analogs
- Slide 23
- Slide 24
- THC
- Results of SAR
- Modes of Absorption
- Smoking and the Body
- Slide 29
- Slide 30
- Metabolites
- Slide 32
- Slide 33
- Cannabis Pharmacology
- Slide 35
- Therapeutic
- Marinol
- Cannabinoid Receptors
- CB1 Receptors
- CB2 Receptor
- Cannabis and Δ9- (THC) for weight loss
- What is obesity
- Slide 43
- Slide 44
- Rimonabant
- Slide 46
- Slide 47
- Slide 48
-
Smoking and the Body
THC enters the body through the Lungs
The smoke is inhaled and held in the lungsAll affect how much THC will enter the plasmaTHC crosses the blood barrier through the capillaries in the lungs
After inhalation THC can reach the brain in about 14 seconds
After a 6 min smoking period peak blood levels reached at about 7 min (100 ngml plasma)
Most THC is absorbed from the blood within 30 min
Moves rapidly into the brain and across the bloodbrainplacental barrier Because fatty chains make it very lipid soluble
Half-life is about 19 hours Can store in fat cells
Established physiological effects are dose related
Lethal dose for THC use has now been studied and no human deaths have been reported due to intoxication from cannabis
Metabolites
bull Radioactively labeled delta-9-THC has been found to persist in the body as an active metabolite as long as 8 days after use
Primary metabolite has a half-life of 50 hours The complete elimination of the drug can take as long as 6 weeks
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
23 of metabolites are excreted in feces13 of metabolites are excreted in urine
Cannabis Pharmacology
Primary Cannabinoids from Cannabis are
bull Cannabinol (CBN) Cannabidiol (CBD) and Tetrahydrocannabinol (THC)
bull THC (-9-THC ) is the only one with significant psychoactive properties
bull CBN - 110 th activity of THC CBD - none
bull 2 isomers a trans-delta-9-THC and a delta-8-THC
bull A cannabidiol (the 2nd most abundant psychoactive ingredient after THC)
bull A cannabinol a decomposition product of THC that accumulates as cannabis samples age
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
Therapeutic
bull Antiemeticbull Reduction of intra-ocular tensionbull Analgesicbull Muscle relaxant bull Anti-convulsant bull Anti-inflammatory appetite ldquothe munchiesrdquo It is one of the most well-known effects of marijuana the
powerful surge in appetite many users feel after smoking or ingesting the drug colloquially known as the munchies
Marinol
THC in a sesame oil suspension
Cannabinoid ReceptorsBeforethe 1980s it was often speculated that
cannabinoids produced their effects through non specific interaction with cell membranes instead of interacting with specific receptors
The discovery of the first cannabinoid receptors in the 1980s helped to resolve this debate These receptors are common in animals and have been found in mammals birds fishes and reptiles
There are currently two known types of cannabinoid receptors CB1 and CB2
CB1 ReceptorsFound primarily in the brain (specifically basal ganglia limbic
system including the hippocampus and cerebellum)1048766Most dense in brain regions involved with thinking and memory
attention and control of movement1048766Also present in both male and female reproductive systems as
well as in the lungs liver and kidneys1048766Appear to be responsible for the euphoric and anticonvulsive
effects of Cannabis1048766Essentially absent in the medulla oblongata the part of the brain
that is responsible for respiratory and cardiovascular functions
Thus there is no risk of respiratory or cardiovascular failure as there is with many other drugs
CB2 Receptor
CB2 receptors are almost exclusively found in the immune system (T cells macrophages B cells) with the greatest density in the spleen
1048766CB2 receptors appear to be responsible for the anti-inflammatory and possible other therapeutic effects of Cannabis
1048766Also expressed on peripheral nerve terminals
Cannabis and Δ9- (THC) for weight loss
bull Obesity is one of the highest preventable causes of morbidity and mortality in the developed world It has been well known for a long time that exposure to cannabis produces an increase of appetite (a phenomenon referred to as the munchies) This phenomenon led to an exploration of the role of the endocannabinoid system in the regulation of obesity and associated metabolic syndrome This effort subsequently led to the development of a successful therapeutic approach for obesity that consisted of blocking the cannabinoid CB1 receptors using ligands such as Rimonabant in order to produce weight loss and improve metabolic profile
What is obesity
Obesity is characterized by an abnormal accumulation of body fat usually 20 percent or more over an individuals ideal body weight Obesity results when the size or number of fat cells in a persons body increases When a person gains weight these fat cells first increase in size and later in number When a person starts losing weight the cells decreas ein size but their number generally stays the same This is part of the reason that once you gain a significant amount of weight it is more difficult to lose it
The clinical definition of obesity is a body mass index(BMI)of 30 or higher BMI = Weight (in kg) Height (in meters) Squared
Rimonabant
bull Acompliareg(Sanofi-Aventis)
launched in Europe in 2006 for
oral treatment of obesity at 20 mg
once daily
Selective blocker of central
and peripheral CB1 receptors
It reduces food intake and improves lipid and glucose metabolism
Rimonabant
Despite being efficacious Rimonabant was associated with increased rates of depression and anxiety and therefore removed from the market
- Cannabis
- Slide 2
- Slide 3
- Cannabis spp
- Slide 5
- Slide 6
- Hemp
- What is Marijuana
- Marijuana ndash History of Use
- HempvsMarijuana-1
- HempvsMarijuana-2
- HempvsMarijuana-3
- Cannabis Biology
- Chemical constituents of Cannabis
- What is a cannabinoid
- What are cannabinoids
- Natural cannabinoids
- Slide 18
- Representative cannabinoids
- Slide 20
- Endocannabinoids
- Structure of THC and synthetic analogs
- Slide 23
- Slide 24
- THC
- Results of SAR
- Modes of Absorption
- Smoking and the Body
- Slide 29
- Slide 30
- Metabolites
- Slide 32
- Slide 33
- Cannabis Pharmacology
- Slide 35
- Therapeutic
- Marinol
- Cannabinoid Receptors
- CB1 Receptors
- CB2 Receptor
- Cannabis and Δ9- (THC) for weight loss
- What is obesity
- Slide 43
- Slide 44
- Rimonabant
- Slide 46
- Slide 47
- Slide 48
-
After a 6 min smoking period peak blood levels reached at about 7 min (100 ngml plasma)
Most THC is absorbed from the blood within 30 min
Moves rapidly into the brain and across the bloodbrainplacental barrier Because fatty chains make it very lipid soluble
Half-life is about 19 hours Can store in fat cells
Established physiological effects are dose related
Lethal dose for THC use has now been studied and no human deaths have been reported due to intoxication from cannabis
Metabolites
bull Radioactively labeled delta-9-THC has been found to persist in the body as an active metabolite as long as 8 days after use
Primary metabolite has a half-life of 50 hours The complete elimination of the drug can take as long as 6 weeks
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
23 of metabolites are excreted in feces13 of metabolites are excreted in urine
Cannabis Pharmacology
Primary Cannabinoids from Cannabis are
bull Cannabinol (CBN) Cannabidiol (CBD) and Tetrahydrocannabinol (THC)
bull THC (-9-THC ) is the only one with significant psychoactive properties
bull CBN - 110 th activity of THC CBD - none
bull 2 isomers a trans-delta-9-THC and a delta-8-THC
bull A cannabidiol (the 2nd most abundant psychoactive ingredient after THC)
bull A cannabinol a decomposition product of THC that accumulates as cannabis samples age
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
Therapeutic
bull Antiemeticbull Reduction of intra-ocular tensionbull Analgesicbull Muscle relaxant bull Anti-convulsant bull Anti-inflammatory appetite ldquothe munchiesrdquo It is one of the most well-known effects of marijuana the
powerful surge in appetite many users feel after smoking or ingesting the drug colloquially known as the munchies
Marinol
THC in a sesame oil suspension
Cannabinoid ReceptorsBeforethe 1980s it was often speculated that
cannabinoids produced their effects through non specific interaction with cell membranes instead of interacting with specific receptors
The discovery of the first cannabinoid receptors in the 1980s helped to resolve this debate These receptors are common in animals and have been found in mammals birds fishes and reptiles
There are currently two known types of cannabinoid receptors CB1 and CB2
CB1 ReceptorsFound primarily in the brain (specifically basal ganglia limbic
system including the hippocampus and cerebellum)1048766Most dense in brain regions involved with thinking and memory
attention and control of movement1048766Also present in both male and female reproductive systems as
well as in the lungs liver and kidneys1048766Appear to be responsible for the euphoric and anticonvulsive
effects of Cannabis1048766Essentially absent in the medulla oblongata the part of the brain
that is responsible for respiratory and cardiovascular functions
Thus there is no risk of respiratory or cardiovascular failure as there is with many other drugs
CB2 Receptor
CB2 receptors are almost exclusively found in the immune system (T cells macrophages B cells) with the greatest density in the spleen
1048766CB2 receptors appear to be responsible for the anti-inflammatory and possible other therapeutic effects of Cannabis
1048766Also expressed on peripheral nerve terminals
Cannabis and Δ9- (THC) for weight loss
bull Obesity is one of the highest preventable causes of morbidity and mortality in the developed world It has been well known for a long time that exposure to cannabis produces an increase of appetite (a phenomenon referred to as the munchies) This phenomenon led to an exploration of the role of the endocannabinoid system in the regulation of obesity and associated metabolic syndrome This effort subsequently led to the development of a successful therapeutic approach for obesity that consisted of blocking the cannabinoid CB1 receptors using ligands such as Rimonabant in order to produce weight loss and improve metabolic profile
What is obesity
Obesity is characterized by an abnormal accumulation of body fat usually 20 percent or more over an individuals ideal body weight Obesity results when the size or number of fat cells in a persons body increases When a person gains weight these fat cells first increase in size and later in number When a person starts losing weight the cells decreas ein size but their number generally stays the same This is part of the reason that once you gain a significant amount of weight it is more difficult to lose it
The clinical definition of obesity is a body mass index(BMI)of 30 or higher BMI = Weight (in kg) Height (in meters) Squared
Rimonabant
bull Acompliareg(Sanofi-Aventis)
launched in Europe in 2006 for
oral treatment of obesity at 20 mg
once daily
Selective blocker of central
and peripheral CB1 receptors
It reduces food intake and improves lipid and glucose metabolism
Rimonabant
Despite being efficacious Rimonabant was associated with increased rates of depression and anxiety and therefore removed from the market
- Cannabis
- Slide 2
- Slide 3
- Cannabis spp
- Slide 5
- Slide 6
- Hemp
- What is Marijuana
- Marijuana ndash History of Use
- HempvsMarijuana-1
- HempvsMarijuana-2
- HempvsMarijuana-3
- Cannabis Biology
- Chemical constituents of Cannabis
- What is a cannabinoid
- What are cannabinoids
- Natural cannabinoids
- Slide 18
- Representative cannabinoids
- Slide 20
- Endocannabinoids
- Structure of THC and synthetic analogs
- Slide 23
- Slide 24
- THC
- Results of SAR
- Modes of Absorption
- Smoking and the Body
- Slide 29
- Slide 30
- Metabolites
- Slide 32
- Slide 33
- Cannabis Pharmacology
- Slide 35
- Therapeutic
- Marinol
- Cannabinoid Receptors
- CB1 Receptors
- CB2 Receptor
- Cannabis and Δ9- (THC) for weight loss
- What is obesity
- Slide 43
- Slide 44
- Rimonabant
- Slide 46
- Slide 47
- Slide 48
-
Metabolites
bull Radioactively labeled delta-9-THC has been found to persist in the body as an active metabolite as long as 8 days after use
Primary metabolite has a half-life of 50 hours The complete elimination of the drug can take as long as 6 weeks
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
23 of metabolites are excreted in feces13 of metabolites are excreted in urine
Cannabis Pharmacology
Primary Cannabinoids from Cannabis are
bull Cannabinol (CBN) Cannabidiol (CBD) and Tetrahydrocannabinol (THC)
bull THC (-9-THC ) is the only one with significant psychoactive properties
bull CBN - 110 th activity of THC CBD - none
bull 2 isomers a trans-delta-9-THC and a delta-8-THC
bull A cannabidiol (the 2nd most abundant psychoactive ingredient after THC)
bull A cannabinol a decomposition product of THC that accumulates as cannabis samples age
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
Therapeutic
bull Antiemeticbull Reduction of intra-ocular tensionbull Analgesicbull Muscle relaxant bull Anti-convulsant bull Anti-inflammatory appetite ldquothe munchiesrdquo It is one of the most well-known effects of marijuana the
powerful surge in appetite many users feel after smoking or ingesting the drug colloquially known as the munchies
Marinol
THC in a sesame oil suspension
Cannabinoid ReceptorsBeforethe 1980s it was often speculated that
cannabinoids produced their effects through non specific interaction with cell membranes instead of interacting with specific receptors
The discovery of the first cannabinoid receptors in the 1980s helped to resolve this debate These receptors are common in animals and have been found in mammals birds fishes and reptiles
There are currently two known types of cannabinoid receptors CB1 and CB2
CB1 ReceptorsFound primarily in the brain (specifically basal ganglia limbic
system including the hippocampus and cerebellum)1048766Most dense in brain regions involved with thinking and memory
attention and control of movement1048766Also present in both male and female reproductive systems as
well as in the lungs liver and kidneys1048766Appear to be responsible for the euphoric and anticonvulsive
effects of Cannabis1048766Essentially absent in the medulla oblongata the part of the brain
that is responsible for respiratory and cardiovascular functions
Thus there is no risk of respiratory or cardiovascular failure as there is with many other drugs
CB2 Receptor
CB2 receptors are almost exclusively found in the immune system (T cells macrophages B cells) with the greatest density in the spleen
1048766CB2 receptors appear to be responsible for the anti-inflammatory and possible other therapeutic effects of Cannabis
1048766Also expressed on peripheral nerve terminals
Cannabis and Δ9- (THC) for weight loss
bull Obesity is one of the highest preventable causes of morbidity and mortality in the developed world It has been well known for a long time that exposure to cannabis produces an increase of appetite (a phenomenon referred to as the munchies) This phenomenon led to an exploration of the role of the endocannabinoid system in the regulation of obesity and associated metabolic syndrome This effort subsequently led to the development of a successful therapeutic approach for obesity that consisted of blocking the cannabinoid CB1 receptors using ligands such as Rimonabant in order to produce weight loss and improve metabolic profile
What is obesity
Obesity is characterized by an abnormal accumulation of body fat usually 20 percent or more over an individuals ideal body weight Obesity results when the size or number of fat cells in a persons body increases When a person gains weight these fat cells first increase in size and later in number When a person starts losing weight the cells decreas ein size but their number generally stays the same This is part of the reason that once you gain a significant amount of weight it is more difficult to lose it
The clinical definition of obesity is a body mass index(BMI)of 30 or higher BMI = Weight (in kg) Height (in meters) Squared
Rimonabant
bull Acompliareg(Sanofi-Aventis)
launched in Europe in 2006 for
oral treatment of obesity at 20 mg
once daily
Selective blocker of central
and peripheral CB1 receptors
It reduces food intake and improves lipid and glucose metabolism
Rimonabant
Despite being efficacious Rimonabant was associated with increased rates of depression and anxiety and therefore removed from the market
- Cannabis
- Slide 2
- Slide 3
- Cannabis spp
- Slide 5
- Slide 6
- Hemp
- What is Marijuana
- Marijuana ndash History of Use
- HempvsMarijuana-1
- HempvsMarijuana-2
- HempvsMarijuana-3
- Cannabis Biology
- Chemical constituents of Cannabis
- What is a cannabinoid
- What are cannabinoids
- Natural cannabinoids
- Slide 18
- Representative cannabinoids
- Slide 20
- Endocannabinoids
- Structure of THC and synthetic analogs
- Slide 23
- Slide 24
- THC
- Results of SAR
- Modes of Absorption
- Smoking and the Body
- Slide 29
- Slide 30
- Metabolites
- Slide 32
- Slide 33
- Cannabis Pharmacology
- Slide 35
- Therapeutic
- Marinol
- Cannabinoid Receptors
- CB1 Receptors
- CB2 Receptor
- Cannabis and Δ9- (THC) for weight loss
- What is obesity
- Slide 43
- Slide 44
- Rimonabant
- Slide 46
- Slide 47
- Slide 48
-
Primary metabolite has a half-life of 50 hours The complete elimination of the drug can take as long as 6 weeks
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
23 of metabolites are excreted in feces13 of metabolites are excreted in urine
Cannabis Pharmacology
Primary Cannabinoids from Cannabis are
bull Cannabinol (CBN) Cannabidiol (CBD) and Tetrahydrocannabinol (THC)
bull THC (-9-THC ) is the only one with significant psychoactive properties
bull CBN - 110 th activity of THC CBD - none
bull 2 isomers a trans-delta-9-THC and a delta-8-THC
bull A cannabidiol (the 2nd most abundant psychoactive ingredient after THC)
bull A cannabinol a decomposition product of THC that accumulates as cannabis samples age
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
Therapeutic
bull Antiemeticbull Reduction of intra-ocular tensionbull Analgesicbull Muscle relaxant bull Anti-convulsant bull Anti-inflammatory appetite ldquothe munchiesrdquo It is one of the most well-known effects of marijuana the
powerful surge in appetite many users feel after smoking or ingesting the drug colloquially known as the munchies
Marinol
THC in a sesame oil suspension
Cannabinoid ReceptorsBeforethe 1980s it was often speculated that
cannabinoids produced their effects through non specific interaction with cell membranes instead of interacting with specific receptors
The discovery of the first cannabinoid receptors in the 1980s helped to resolve this debate These receptors are common in animals and have been found in mammals birds fishes and reptiles
There are currently two known types of cannabinoid receptors CB1 and CB2
CB1 ReceptorsFound primarily in the brain (specifically basal ganglia limbic
system including the hippocampus and cerebellum)1048766Most dense in brain regions involved with thinking and memory
attention and control of movement1048766Also present in both male and female reproductive systems as
well as in the lungs liver and kidneys1048766Appear to be responsible for the euphoric and anticonvulsive
effects of Cannabis1048766Essentially absent in the medulla oblongata the part of the brain
that is responsible for respiratory and cardiovascular functions
Thus there is no risk of respiratory or cardiovascular failure as there is with many other drugs
CB2 Receptor
CB2 receptors are almost exclusively found in the immune system (T cells macrophages B cells) with the greatest density in the spleen
1048766CB2 receptors appear to be responsible for the anti-inflammatory and possible other therapeutic effects of Cannabis
1048766Also expressed on peripheral nerve terminals
Cannabis and Δ9- (THC) for weight loss
bull Obesity is one of the highest preventable causes of morbidity and mortality in the developed world It has been well known for a long time that exposure to cannabis produces an increase of appetite (a phenomenon referred to as the munchies) This phenomenon led to an exploration of the role of the endocannabinoid system in the regulation of obesity and associated metabolic syndrome This effort subsequently led to the development of a successful therapeutic approach for obesity that consisted of blocking the cannabinoid CB1 receptors using ligands such as Rimonabant in order to produce weight loss and improve metabolic profile
What is obesity
Obesity is characterized by an abnormal accumulation of body fat usually 20 percent or more over an individuals ideal body weight Obesity results when the size or number of fat cells in a persons body increases When a person gains weight these fat cells first increase in size and later in number When a person starts losing weight the cells decreas ein size but their number generally stays the same This is part of the reason that once you gain a significant amount of weight it is more difficult to lose it
The clinical definition of obesity is a body mass index(BMI)of 30 or higher BMI = Weight (in kg) Height (in meters) Squared
Rimonabant
bull Acompliareg(Sanofi-Aventis)
launched in Europe in 2006 for
oral treatment of obesity at 20 mg
once daily
Selective blocker of central
and peripheral CB1 receptors
It reduces food intake and improves lipid and glucose metabolism
Rimonabant
Despite being efficacious Rimonabant was associated with increased rates of depression and anxiety and therefore removed from the market
- Cannabis
- Slide 2
- Slide 3
- Cannabis spp
- Slide 5
- Slide 6
- Hemp
- What is Marijuana
- Marijuana ndash History of Use
- HempvsMarijuana-1
- HempvsMarijuana-2
- HempvsMarijuana-3
- Cannabis Biology
- Chemical constituents of Cannabis
- What is a cannabinoid
- What are cannabinoids
- Natural cannabinoids
- Slide 18
- Representative cannabinoids
- Slide 20
- Endocannabinoids
- Structure of THC and synthetic analogs
- Slide 23
- Slide 24
- THC
- Results of SAR
- Modes of Absorption
- Smoking and the Body
- Slide 29
- Slide 30
- Metabolites
- Slide 32
- Slide 33
- Cannabis Pharmacology
- Slide 35
- Therapeutic
- Marinol
- Cannabinoid Receptors
- CB1 Receptors
- CB2 Receptor
- Cannabis and Δ9- (THC) for weight loss
- What is obesity
- Slide 43
- Slide 44
- Rimonabant
- Slide 46
- Slide 47
- Slide 48
-
Cannabis Pharmacology
Primary Cannabinoids from Cannabis are
bull Cannabinol (CBN) Cannabidiol (CBD) and Tetrahydrocannabinol (THC)
bull THC (-9-THC ) is the only one with significant psychoactive properties
bull CBN - 110 th activity of THC CBD - none
bull 2 isomers a trans-delta-9-THC and a delta-8-THC
bull A cannabidiol (the 2nd most abundant psychoactive ingredient after THC)
bull A cannabinol a decomposition product of THC that accumulates as cannabis samples age
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
Therapeutic
bull Antiemeticbull Reduction of intra-ocular tensionbull Analgesicbull Muscle relaxant bull Anti-convulsant bull Anti-inflammatory appetite ldquothe munchiesrdquo It is one of the most well-known effects of marijuana the
powerful surge in appetite many users feel after smoking or ingesting the drug colloquially known as the munchies
Marinol
THC in a sesame oil suspension
Cannabinoid ReceptorsBeforethe 1980s it was often speculated that
cannabinoids produced their effects through non specific interaction with cell membranes instead of interacting with specific receptors
The discovery of the first cannabinoid receptors in the 1980s helped to resolve this debate These receptors are common in animals and have been found in mammals birds fishes and reptiles
There are currently two known types of cannabinoid receptors CB1 and CB2
CB1 ReceptorsFound primarily in the brain (specifically basal ganglia limbic
system including the hippocampus and cerebellum)1048766Most dense in brain regions involved with thinking and memory
attention and control of movement1048766Also present in both male and female reproductive systems as
well as in the lungs liver and kidneys1048766Appear to be responsible for the euphoric and anticonvulsive
effects of Cannabis1048766Essentially absent in the medulla oblongata the part of the brain
that is responsible for respiratory and cardiovascular functions
Thus there is no risk of respiratory or cardiovascular failure as there is with many other drugs
CB2 Receptor
CB2 receptors are almost exclusively found in the immune system (T cells macrophages B cells) with the greatest density in the spleen
1048766CB2 receptors appear to be responsible for the anti-inflammatory and possible other therapeutic effects of Cannabis
1048766Also expressed on peripheral nerve terminals
Cannabis and Δ9- (THC) for weight loss
bull Obesity is one of the highest preventable causes of morbidity and mortality in the developed world It has been well known for a long time that exposure to cannabis produces an increase of appetite (a phenomenon referred to as the munchies) This phenomenon led to an exploration of the role of the endocannabinoid system in the regulation of obesity and associated metabolic syndrome This effort subsequently led to the development of a successful therapeutic approach for obesity that consisted of blocking the cannabinoid CB1 receptors using ligands such as Rimonabant in order to produce weight loss and improve metabolic profile
What is obesity
Obesity is characterized by an abnormal accumulation of body fat usually 20 percent or more over an individuals ideal body weight Obesity results when the size or number of fat cells in a persons body increases When a person gains weight these fat cells first increase in size and later in number When a person starts losing weight the cells decreas ein size but their number generally stays the same This is part of the reason that once you gain a significant amount of weight it is more difficult to lose it
The clinical definition of obesity is a body mass index(BMI)of 30 or higher BMI = Weight (in kg) Height (in meters) Squared
Rimonabant
bull Acompliareg(Sanofi-Aventis)
launched in Europe in 2006 for
oral treatment of obesity at 20 mg
once daily
Selective blocker of central
and peripheral CB1 receptors
It reduces food intake and improves lipid and glucose metabolism
Rimonabant
Despite being efficacious Rimonabant was associated with increased rates of depression and anxiety and therefore removed from the market
- Cannabis
- Slide 2
- Slide 3
- Cannabis spp
- Slide 5
- Slide 6
- Hemp
- What is Marijuana
- Marijuana ndash History of Use
- HempvsMarijuana-1
- HempvsMarijuana-2
- HempvsMarijuana-3
- Cannabis Biology
- Chemical constituents of Cannabis
- What is a cannabinoid
- What are cannabinoids
- Natural cannabinoids
- Slide 18
- Representative cannabinoids
- Slide 20
- Endocannabinoids
- Structure of THC and synthetic analogs
- Slide 23
- Slide 24
- THC
- Results of SAR
- Modes of Absorption
- Smoking and the Body
- Slide 29
- Slide 30
- Metabolites
- Slide 32
- Slide 33
- Cannabis Pharmacology
- Slide 35
- Therapeutic
- Marinol
- Cannabinoid Receptors
- CB1 Receptors
- CB2 Receptor
- Cannabis and Δ9- (THC) for weight loss
- What is obesity
- Slide 43
- Slide 44
- Rimonabant
- Slide 46
- Slide 47
- Slide 48
-
bull 2 isomers a trans-delta-9-THC and a delta-8-THC
bull A cannabidiol (the 2nd most abundant psychoactive ingredient after THC)
bull A cannabinol a decomposition product of THC that accumulates as cannabis samples age
After ingestion delta-9 is converted in the liver to 11-Hydroxy THC which is equally as potent and active
Therapeutic
bull Antiemeticbull Reduction of intra-ocular tensionbull Analgesicbull Muscle relaxant bull Anti-convulsant bull Anti-inflammatory appetite ldquothe munchiesrdquo It is one of the most well-known effects of marijuana the
powerful surge in appetite many users feel after smoking or ingesting the drug colloquially known as the munchies
Marinol
THC in a sesame oil suspension
Cannabinoid ReceptorsBeforethe 1980s it was often speculated that
cannabinoids produced their effects through non specific interaction with cell membranes instead of interacting with specific receptors
The discovery of the first cannabinoid receptors in the 1980s helped to resolve this debate These receptors are common in animals and have been found in mammals birds fishes and reptiles
There are currently two known types of cannabinoid receptors CB1 and CB2
CB1 ReceptorsFound primarily in the brain (specifically basal ganglia limbic
system including the hippocampus and cerebellum)1048766Most dense in brain regions involved with thinking and memory
attention and control of movement1048766Also present in both male and female reproductive systems as
well as in the lungs liver and kidneys1048766Appear to be responsible for the euphoric and anticonvulsive
effects of Cannabis1048766Essentially absent in the medulla oblongata the part of the brain
that is responsible for respiratory and cardiovascular functions
Thus there is no risk of respiratory or cardiovascular failure as there is with many other drugs
CB2 Receptor
CB2 receptors are almost exclusively found in the immune system (T cells macrophages B cells) with the greatest density in the spleen
1048766CB2 receptors appear to be responsible for the anti-inflammatory and possible other therapeutic effects of Cannabis
1048766Also expressed on peripheral nerve terminals
Cannabis and Δ9- (THC) for weight loss
bull Obesity is one of the highest preventable causes of morbidity and mortality in the developed world It has been well known for a long time that exposure to cannabis produces an increase of appetite (a phenomenon referred to as the munchies) This phenomenon led to an exploration of the role of the endocannabinoid system in the regulation of obesity and associated metabolic syndrome This effort subsequently led to the development of a successful therapeutic approach for obesity that consisted of blocking the cannabinoid CB1 receptors using ligands such as Rimonabant in order to produce weight loss and improve metabolic profile
What is obesity
Obesity is characterized by an abnormal accumulation of body fat usually 20 percent or more over an individuals ideal body weight Obesity results when the size or number of fat cells in a persons body increases When a person gains weight these fat cells first increase in size and later in number When a person starts losing weight the cells decreas ein size but their number generally stays the same This is part of the reason that once you gain a significant amount of weight it is more difficult to lose it
The clinical definition of obesity is a body mass index(BMI)of 30 or higher BMI = Weight (in kg) Height (in meters) Squared
Rimonabant
bull Acompliareg(Sanofi-Aventis)
launched in Europe in 2006 for
oral treatment of obesity at 20 mg
once daily
Selective blocker of central
and peripheral CB1 receptors
It reduces food intake and improves lipid and glucose metabolism
Rimonabant
Despite being efficacious Rimonabant was associated with increased rates of depression and anxiety and therefore removed from the market
- Cannabis
- Slide 2
- Slide 3
- Cannabis spp
- Slide 5
- Slide 6
- Hemp
- What is Marijuana
- Marijuana ndash History of Use
- HempvsMarijuana-1
- HempvsMarijuana-2
- HempvsMarijuana-3
- Cannabis Biology
- Chemical constituents of Cannabis
- What is a cannabinoid
- What are cannabinoids
- Natural cannabinoids
- Slide 18
- Representative cannabinoids
- Slide 20
- Endocannabinoids
- Structure of THC and synthetic analogs
- Slide 23
- Slide 24
- THC
- Results of SAR
- Modes of Absorption
- Smoking and the Body
- Slide 29
- Slide 30
- Metabolites
- Slide 32
- Slide 33
- Cannabis Pharmacology
- Slide 35
- Therapeutic
- Marinol
- Cannabinoid Receptors
- CB1 Receptors
- CB2 Receptor
- Cannabis and Δ9- (THC) for weight loss
- What is obesity
- Slide 43
- Slide 44
- Rimonabant
- Slide 46
- Slide 47
- Slide 48
-
Therapeutic
bull Antiemeticbull Reduction of intra-ocular tensionbull Analgesicbull Muscle relaxant bull Anti-convulsant bull Anti-inflammatory appetite ldquothe munchiesrdquo It is one of the most well-known effects of marijuana the
powerful surge in appetite many users feel after smoking or ingesting the drug colloquially known as the munchies
Marinol
THC in a sesame oil suspension
Cannabinoid ReceptorsBeforethe 1980s it was often speculated that
cannabinoids produced their effects through non specific interaction with cell membranes instead of interacting with specific receptors
The discovery of the first cannabinoid receptors in the 1980s helped to resolve this debate These receptors are common in animals and have been found in mammals birds fishes and reptiles
There are currently two known types of cannabinoid receptors CB1 and CB2
CB1 ReceptorsFound primarily in the brain (specifically basal ganglia limbic
system including the hippocampus and cerebellum)1048766Most dense in brain regions involved with thinking and memory
attention and control of movement1048766Also present in both male and female reproductive systems as
well as in the lungs liver and kidneys1048766Appear to be responsible for the euphoric and anticonvulsive
effects of Cannabis1048766Essentially absent in the medulla oblongata the part of the brain
that is responsible for respiratory and cardiovascular functions
Thus there is no risk of respiratory or cardiovascular failure as there is with many other drugs
CB2 Receptor
CB2 receptors are almost exclusively found in the immune system (T cells macrophages B cells) with the greatest density in the spleen
1048766CB2 receptors appear to be responsible for the anti-inflammatory and possible other therapeutic effects of Cannabis
1048766Also expressed on peripheral nerve terminals
Cannabis and Δ9- (THC) for weight loss
bull Obesity is one of the highest preventable causes of morbidity and mortality in the developed world It has been well known for a long time that exposure to cannabis produces an increase of appetite (a phenomenon referred to as the munchies) This phenomenon led to an exploration of the role of the endocannabinoid system in the regulation of obesity and associated metabolic syndrome This effort subsequently led to the development of a successful therapeutic approach for obesity that consisted of blocking the cannabinoid CB1 receptors using ligands such as Rimonabant in order to produce weight loss and improve metabolic profile
What is obesity
Obesity is characterized by an abnormal accumulation of body fat usually 20 percent or more over an individuals ideal body weight Obesity results when the size or number of fat cells in a persons body increases When a person gains weight these fat cells first increase in size and later in number When a person starts losing weight the cells decreas ein size but their number generally stays the same This is part of the reason that once you gain a significant amount of weight it is more difficult to lose it
The clinical definition of obesity is a body mass index(BMI)of 30 or higher BMI = Weight (in kg) Height (in meters) Squared
Rimonabant
bull Acompliareg(Sanofi-Aventis)
launched in Europe in 2006 for
oral treatment of obesity at 20 mg
once daily
Selective blocker of central
and peripheral CB1 receptors
It reduces food intake and improves lipid and glucose metabolism
Rimonabant
Despite being efficacious Rimonabant was associated with increased rates of depression and anxiety and therefore removed from the market
- Cannabis
- Slide 2
- Slide 3
- Cannabis spp
- Slide 5
- Slide 6
- Hemp
- What is Marijuana
- Marijuana ndash History of Use
- HempvsMarijuana-1
- HempvsMarijuana-2
- HempvsMarijuana-3
- Cannabis Biology
- Chemical constituents of Cannabis
- What is a cannabinoid
- What are cannabinoids
- Natural cannabinoids
- Slide 18
- Representative cannabinoids
- Slide 20
- Endocannabinoids
- Structure of THC and synthetic analogs
- Slide 23
- Slide 24
- THC
- Results of SAR
- Modes of Absorption
- Smoking and the Body
- Slide 29
- Slide 30
- Metabolites
- Slide 32
- Slide 33
- Cannabis Pharmacology
- Slide 35
- Therapeutic
- Marinol
- Cannabinoid Receptors
- CB1 Receptors
- CB2 Receptor
- Cannabis and Δ9- (THC) for weight loss
- What is obesity
- Slide 43
- Slide 44
- Rimonabant
- Slide 46
- Slide 47
- Slide 48
-
Marinol
THC in a sesame oil suspension
Cannabinoid ReceptorsBeforethe 1980s it was often speculated that
cannabinoids produced their effects through non specific interaction with cell membranes instead of interacting with specific receptors
The discovery of the first cannabinoid receptors in the 1980s helped to resolve this debate These receptors are common in animals and have been found in mammals birds fishes and reptiles
There are currently two known types of cannabinoid receptors CB1 and CB2
CB1 ReceptorsFound primarily in the brain (specifically basal ganglia limbic
system including the hippocampus and cerebellum)1048766Most dense in brain regions involved with thinking and memory
attention and control of movement1048766Also present in both male and female reproductive systems as
well as in the lungs liver and kidneys1048766Appear to be responsible for the euphoric and anticonvulsive
effects of Cannabis1048766Essentially absent in the medulla oblongata the part of the brain
that is responsible for respiratory and cardiovascular functions
Thus there is no risk of respiratory or cardiovascular failure as there is with many other drugs
CB2 Receptor
CB2 receptors are almost exclusively found in the immune system (T cells macrophages B cells) with the greatest density in the spleen
1048766CB2 receptors appear to be responsible for the anti-inflammatory and possible other therapeutic effects of Cannabis
1048766Also expressed on peripheral nerve terminals
Cannabis and Δ9- (THC) for weight loss
bull Obesity is one of the highest preventable causes of morbidity and mortality in the developed world It has been well known for a long time that exposure to cannabis produces an increase of appetite (a phenomenon referred to as the munchies) This phenomenon led to an exploration of the role of the endocannabinoid system in the regulation of obesity and associated metabolic syndrome This effort subsequently led to the development of a successful therapeutic approach for obesity that consisted of blocking the cannabinoid CB1 receptors using ligands such as Rimonabant in order to produce weight loss and improve metabolic profile
What is obesity
Obesity is characterized by an abnormal accumulation of body fat usually 20 percent or more over an individuals ideal body weight Obesity results when the size or number of fat cells in a persons body increases When a person gains weight these fat cells first increase in size and later in number When a person starts losing weight the cells decreas ein size but their number generally stays the same This is part of the reason that once you gain a significant amount of weight it is more difficult to lose it
The clinical definition of obesity is a body mass index(BMI)of 30 or higher BMI = Weight (in kg) Height (in meters) Squared
Rimonabant
bull Acompliareg(Sanofi-Aventis)
launched in Europe in 2006 for
oral treatment of obesity at 20 mg
once daily
Selective blocker of central
and peripheral CB1 receptors
It reduces food intake and improves lipid and glucose metabolism
Rimonabant
Despite being efficacious Rimonabant was associated with increased rates of depression and anxiety and therefore removed from the market
- Cannabis
- Slide 2
- Slide 3
- Cannabis spp
- Slide 5
- Slide 6
- Hemp
- What is Marijuana
- Marijuana ndash History of Use
- HempvsMarijuana-1
- HempvsMarijuana-2
- HempvsMarijuana-3
- Cannabis Biology
- Chemical constituents of Cannabis
- What is a cannabinoid
- What are cannabinoids
- Natural cannabinoids
- Slide 18
- Representative cannabinoids
- Slide 20
- Endocannabinoids
- Structure of THC and synthetic analogs
- Slide 23
- Slide 24
- THC
- Results of SAR
- Modes of Absorption
- Smoking and the Body
- Slide 29
- Slide 30
- Metabolites
- Slide 32
- Slide 33
- Cannabis Pharmacology
- Slide 35
- Therapeutic
- Marinol
- Cannabinoid Receptors
- CB1 Receptors
- CB2 Receptor
- Cannabis and Δ9- (THC) for weight loss
- What is obesity
- Slide 43
- Slide 44
- Rimonabant
- Slide 46
- Slide 47
- Slide 48
-
Cannabinoid ReceptorsBeforethe 1980s it was often speculated that
cannabinoids produced their effects through non specific interaction with cell membranes instead of interacting with specific receptors
The discovery of the first cannabinoid receptors in the 1980s helped to resolve this debate These receptors are common in animals and have been found in mammals birds fishes and reptiles
There are currently two known types of cannabinoid receptors CB1 and CB2
CB1 ReceptorsFound primarily in the brain (specifically basal ganglia limbic
system including the hippocampus and cerebellum)1048766Most dense in brain regions involved with thinking and memory
attention and control of movement1048766Also present in both male and female reproductive systems as
well as in the lungs liver and kidneys1048766Appear to be responsible for the euphoric and anticonvulsive
effects of Cannabis1048766Essentially absent in the medulla oblongata the part of the brain
that is responsible for respiratory and cardiovascular functions
Thus there is no risk of respiratory or cardiovascular failure as there is with many other drugs
CB2 Receptor
CB2 receptors are almost exclusively found in the immune system (T cells macrophages B cells) with the greatest density in the spleen
1048766CB2 receptors appear to be responsible for the anti-inflammatory and possible other therapeutic effects of Cannabis
1048766Also expressed on peripheral nerve terminals
Cannabis and Δ9- (THC) for weight loss
bull Obesity is one of the highest preventable causes of morbidity and mortality in the developed world It has been well known for a long time that exposure to cannabis produces an increase of appetite (a phenomenon referred to as the munchies) This phenomenon led to an exploration of the role of the endocannabinoid system in the regulation of obesity and associated metabolic syndrome This effort subsequently led to the development of a successful therapeutic approach for obesity that consisted of blocking the cannabinoid CB1 receptors using ligands such as Rimonabant in order to produce weight loss and improve metabolic profile
What is obesity
Obesity is characterized by an abnormal accumulation of body fat usually 20 percent or more over an individuals ideal body weight Obesity results when the size or number of fat cells in a persons body increases When a person gains weight these fat cells first increase in size and later in number When a person starts losing weight the cells decreas ein size but their number generally stays the same This is part of the reason that once you gain a significant amount of weight it is more difficult to lose it
The clinical definition of obesity is a body mass index(BMI)of 30 or higher BMI = Weight (in kg) Height (in meters) Squared
Rimonabant
bull Acompliareg(Sanofi-Aventis)
launched in Europe in 2006 for
oral treatment of obesity at 20 mg
once daily
Selective blocker of central
and peripheral CB1 receptors
It reduces food intake and improves lipid and glucose metabolism
Rimonabant
Despite being efficacious Rimonabant was associated with increased rates of depression and anxiety and therefore removed from the market
- Cannabis
- Slide 2
- Slide 3
- Cannabis spp
- Slide 5
- Slide 6
- Hemp
- What is Marijuana
- Marijuana ndash History of Use
- HempvsMarijuana-1
- HempvsMarijuana-2
- HempvsMarijuana-3
- Cannabis Biology
- Chemical constituents of Cannabis
- What is a cannabinoid
- What are cannabinoids
- Natural cannabinoids
- Slide 18
- Representative cannabinoids
- Slide 20
- Endocannabinoids
- Structure of THC and synthetic analogs
- Slide 23
- Slide 24
- THC
- Results of SAR
- Modes of Absorption
- Smoking and the Body
- Slide 29
- Slide 30
- Metabolites
- Slide 32
- Slide 33
- Cannabis Pharmacology
- Slide 35
- Therapeutic
- Marinol
- Cannabinoid Receptors
- CB1 Receptors
- CB2 Receptor
- Cannabis and Δ9- (THC) for weight loss
- What is obesity
- Slide 43
- Slide 44
- Rimonabant
- Slide 46
- Slide 47
- Slide 48
-
CB1 ReceptorsFound primarily in the brain (specifically basal ganglia limbic
system including the hippocampus and cerebellum)1048766Most dense in brain regions involved with thinking and memory
attention and control of movement1048766Also present in both male and female reproductive systems as
well as in the lungs liver and kidneys1048766Appear to be responsible for the euphoric and anticonvulsive
effects of Cannabis1048766Essentially absent in the medulla oblongata the part of the brain
that is responsible for respiratory and cardiovascular functions
Thus there is no risk of respiratory or cardiovascular failure as there is with many other drugs
CB2 Receptor
CB2 receptors are almost exclusively found in the immune system (T cells macrophages B cells) with the greatest density in the spleen
1048766CB2 receptors appear to be responsible for the anti-inflammatory and possible other therapeutic effects of Cannabis
1048766Also expressed on peripheral nerve terminals
Cannabis and Δ9- (THC) for weight loss
bull Obesity is one of the highest preventable causes of morbidity and mortality in the developed world It has been well known for a long time that exposure to cannabis produces an increase of appetite (a phenomenon referred to as the munchies) This phenomenon led to an exploration of the role of the endocannabinoid system in the regulation of obesity and associated metabolic syndrome This effort subsequently led to the development of a successful therapeutic approach for obesity that consisted of blocking the cannabinoid CB1 receptors using ligands such as Rimonabant in order to produce weight loss and improve metabolic profile
What is obesity
Obesity is characterized by an abnormal accumulation of body fat usually 20 percent or more over an individuals ideal body weight Obesity results when the size or number of fat cells in a persons body increases When a person gains weight these fat cells first increase in size and later in number When a person starts losing weight the cells decreas ein size but their number generally stays the same This is part of the reason that once you gain a significant amount of weight it is more difficult to lose it
The clinical definition of obesity is a body mass index(BMI)of 30 or higher BMI = Weight (in kg) Height (in meters) Squared
Rimonabant
bull Acompliareg(Sanofi-Aventis)
launched in Europe in 2006 for
oral treatment of obesity at 20 mg
once daily
Selective blocker of central
and peripheral CB1 receptors
It reduces food intake and improves lipid and glucose metabolism
Rimonabant
Despite being efficacious Rimonabant was associated with increased rates of depression and anxiety and therefore removed from the market
- Cannabis
- Slide 2
- Slide 3
- Cannabis spp
- Slide 5
- Slide 6
- Hemp
- What is Marijuana
- Marijuana ndash History of Use
- HempvsMarijuana-1
- HempvsMarijuana-2
- HempvsMarijuana-3
- Cannabis Biology
- Chemical constituents of Cannabis
- What is a cannabinoid
- What are cannabinoids
- Natural cannabinoids
- Slide 18
- Representative cannabinoids
- Slide 20
- Endocannabinoids
- Structure of THC and synthetic analogs
- Slide 23
- Slide 24
- THC
- Results of SAR
- Modes of Absorption
- Smoking and the Body
- Slide 29
- Slide 30
- Metabolites
- Slide 32
- Slide 33
- Cannabis Pharmacology
- Slide 35
- Therapeutic
- Marinol
- Cannabinoid Receptors
- CB1 Receptors
- CB2 Receptor
- Cannabis and Δ9- (THC) for weight loss
- What is obesity
- Slide 43
- Slide 44
- Rimonabant
- Slide 46
- Slide 47
- Slide 48
-
CB2 Receptor
CB2 receptors are almost exclusively found in the immune system (T cells macrophages B cells) with the greatest density in the spleen
1048766CB2 receptors appear to be responsible for the anti-inflammatory and possible other therapeutic effects of Cannabis
1048766Also expressed on peripheral nerve terminals
Cannabis and Δ9- (THC) for weight loss
bull Obesity is one of the highest preventable causes of morbidity and mortality in the developed world It has been well known for a long time that exposure to cannabis produces an increase of appetite (a phenomenon referred to as the munchies) This phenomenon led to an exploration of the role of the endocannabinoid system in the regulation of obesity and associated metabolic syndrome This effort subsequently led to the development of a successful therapeutic approach for obesity that consisted of blocking the cannabinoid CB1 receptors using ligands such as Rimonabant in order to produce weight loss and improve metabolic profile
What is obesity
Obesity is characterized by an abnormal accumulation of body fat usually 20 percent or more over an individuals ideal body weight Obesity results when the size or number of fat cells in a persons body increases When a person gains weight these fat cells first increase in size and later in number When a person starts losing weight the cells decreas ein size but their number generally stays the same This is part of the reason that once you gain a significant amount of weight it is more difficult to lose it
The clinical definition of obesity is a body mass index(BMI)of 30 or higher BMI = Weight (in kg) Height (in meters) Squared
Rimonabant
bull Acompliareg(Sanofi-Aventis)
launched in Europe in 2006 for
oral treatment of obesity at 20 mg
once daily
Selective blocker of central
and peripheral CB1 receptors
It reduces food intake and improves lipid and glucose metabolism
Rimonabant
Despite being efficacious Rimonabant was associated with increased rates of depression and anxiety and therefore removed from the market
- Cannabis
- Slide 2
- Slide 3
- Cannabis spp
- Slide 5
- Slide 6
- Hemp
- What is Marijuana
- Marijuana ndash History of Use
- HempvsMarijuana-1
- HempvsMarijuana-2
- HempvsMarijuana-3
- Cannabis Biology
- Chemical constituents of Cannabis
- What is a cannabinoid
- What are cannabinoids
- Natural cannabinoids
- Slide 18
- Representative cannabinoids
- Slide 20
- Endocannabinoids
- Structure of THC and synthetic analogs
- Slide 23
- Slide 24
- THC
- Results of SAR
- Modes of Absorption
- Smoking and the Body
- Slide 29
- Slide 30
- Metabolites
- Slide 32
- Slide 33
- Cannabis Pharmacology
- Slide 35
- Therapeutic
- Marinol
- Cannabinoid Receptors
- CB1 Receptors
- CB2 Receptor
- Cannabis and Δ9- (THC) for weight loss
- What is obesity
- Slide 43
- Slide 44
- Rimonabant
- Slide 46
- Slide 47
- Slide 48
-
Cannabis and Δ9- (THC) for weight loss
bull Obesity is one of the highest preventable causes of morbidity and mortality in the developed world It has been well known for a long time that exposure to cannabis produces an increase of appetite (a phenomenon referred to as the munchies) This phenomenon led to an exploration of the role of the endocannabinoid system in the regulation of obesity and associated metabolic syndrome This effort subsequently led to the development of a successful therapeutic approach for obesity that consisted of blocking the cannabinoid CB1 receptors using ligands such as Rimonabant in order to produce weight loss and improve metabolic profile
What is obesity
Obesity is characterized by an abnormal accumulation of body fat usually 20 percent or more over an individuals ideal body weight Obesity results when the size or number of fat cells in a persons body increases When a person gains weight these fat cells first increase in size and later in number When a person starts losing weight the cells decreas ein size but their number generally stays the same This is part of the reason that once you gain a significant amount of weight it is more difficult to lose it
The clinical definition of obesity is a body mass index(BMI)of 30 or higher BMI = Weight (in kg) Height (in meters) Squared
Rimonabant
bull Acompliareg(Sanofi-Aventis)
launched in Europe in 2006 for
oral treatment of obesity at 20 mg
once daily
Selective blocker of central
and peripheral CB1 receptors
It reduces food intake and improves lipid and glucose metabolism
Rimonabant
Despite being efficacious Rimonabant was associated with increased rates of depression and anxiety and therefore removed from the market
- Cannabis
- Slide 2
- Slide 3
- Cannabis spp
- Slide 5
- Slide 6
- Hemp
- What is Marijuana
- Marijuana ndash History of Use
- HempvsMarijuana-1
- HempvsMarijuana-2
- HempvsMarijuana-3
- Cannabis Biology
- Chemical constituents of Cannabis
- What is a cannabinoid
- What are cannabinoids
- Natural cannabinoids
- Slide 18
- Representative cannabinoids
- Slide 20
- Endocannabinoids
- Structure of THC and synthetic analogs
- Slide 23
- Slide 24
- THC
- Results of SAR
- Modes of Absorption
- Smoking and the Body
- Slide 29
- Slide 30
- Metabolites
- Slide 32
- Slide 33
- Cannabis Pharmacology
- Slide 35
- Therapeutic
- Marinol
- Cannabinoid Receptors
- CB1 Receptors
- CB2 Receptor
- Cannabis and Δ9- (THC) for weight loss
- What is obesity
- Slide 43
- Slide 44
- Rimonabant
- Slide 46
- Slide 47
- Slide 48
-
What is obesity
Obesity is characterized by an abnormal accumulation of body fat usually 20 percent or more over an individuals ideal body weight Obesity results when the size or number of fat cells in a persons body increases When a person gains weight these fat cells first increase in size and later in number When a person starts losing weight the cells decreas ein size but their number generally stays the same This is part of the reason that once you gain a significant amount of weight it is more difficult to lose it
The clinical definition of obesity is a body mass index(BMI)of 30 or higher BMI = Weight (in kg) Height (in meters) Squared
Rimonabant
bull Acompliareg(Sanofi-Aventis)
launched in Europe in 2006 for
oral treatment of obesity at 20 mg
once daily
Selective blocker of central
and peripheral CB1 receptors
It reduces food intake and improves lipid and glucose metabolism
Rimonabant
Despite being efficacious Rimonabant was associated with increased rates of depression and anxiety and therefore removed from the market
- Cannabis
- Slide 2
- Slide 3
- Cannabis spp
- Slide 5
- Slide 6
- Hemp
- What is Marijuana
- Marijuana ndash History of Use
- HempvsMarijuana-1
- HempvsMarijuana-2
- HempvsMarijuana-3
- Cannabis Biology
- Chemical constituents of Cannabis
- What is a cannabinoid
- What are cannabinoids
- Natural cannabinoids
- Slide 18
- Representative cannabinoids
- Slide 20
- Endocannabinoids
- Structure of THC and synthetic analogs
- Slide 23
- Slide 24
- THC
- Results of SAR
- Modes of Absorption
- Smoking and the Body
- Slide 29
- Slide 30
- Metabolites
- Slide 32
- Slide 33
- Cannabis Pharmacology
- Slide 35
- Therapeutic
- Marinol
- Cannabinoid Receptors
- CB1 Receptors
- CB2 Receptor
- Cannabis and Δ9- (THC) for weight loss
- What is obesity
- Slide 43
- Slide 44
- Rimonabant
- Slide 46
- Slide 47
- Slide 48
-
Obesity is characterized by an abnormal accumulation of body fat usually 20 percent or more over an individuals ideal body weight Obesity results when the size or number of fat cells in a persons body increases When a person gains weight these fat cells first increase in size and later in number When a person starts losing weight the cells decreas ein size but their number generally stays the same This is part of the reason that once you gain a significant amount of weight it is more difficult to lose it
The clinical definition of obesity is a body mass index(BMI)of 30 or higher BMI = Weight (in kg) Height (in meters) Squared
Rimonabant
bull Acompliareg(Sanofi-Aventis)
launched in Europe in 2006 for
oral treatment of obesity at 20 mg
once daily
Selective blocker of central
and peripheral CB1 receptors
It reduces food intake and improves lipid and glucose metabolism
Rimonabant
Despite being efficacious Rimonabant was associated with increased rates of depression and anxiety and therefore removed from the market
- Cannabis
- Slide 2
- Slide 3
- Cannabis spp
- Slide 5
- Slide 6
- Hemp
- What is Marijuana
- Marijuana ndash History of Use
- HempvsMarijuana-1
- HempvsMarijuana-2
- HempvsMarijuana-3
- Cannabis Biology
- Chemical constituents of Cannabis
- What is a cannabinoid
- What are cannabinoids
- Natural cannabinoids
- Slide 18
- Representative cannabinoids
- Slide 20
- Endocannabinoids
- Structure of THC and synthetic analogs
- Slide 23
- Slide 24
- THC
- Results of SAR
- Modes of Absorption
- Smoking and the Body
- Slide 29
- Slide 30
- Metabolites
- Slide 32
- Slide 33
- Cannabis Pharmacology
- Slide 35
- Therapeutic
- Marinol
- Cannabinoid Receptors
- CB1 Receptors
- CB2 Receptor
- Cannabis and Δ9- (THC) for weight loss
- What is obesity
- Slide 43
- Slide 44
- Rimonabant
- Slide 46
- Slide 47
- Slide 48
-
The clinical definition of obesity is a body mass index(BMI)of 30 or higher BMI = Weight (in kg) Height (in meters) Squared
Rimonabant
bull Acompliareg(Sanofi-Aventis)
launched in Europe in 2006 for
oral treatment of obesity at 20 mg
once daily
Selective blocker of central
and peripheral CB1 receptors
It reduces food intake and improves lipid and glucose metabolism
Rimonabant
Despite being efficacious Rimonabant was associated with increased rates of depression and anxiety and therefore removed from the market
- Cannabis
- Slide 2
- Slide 3
- Cannabis spp
- Slide 5
- Slide 6
- Hemp
- What is Marijuana
- Marijuana ndash History of Use
- HempvsMarijuana-1
- HempvsMarijuana-2
- HempvsMarijuana-3
- Cannabis Biology
- Chemical constituents of Cannabis
- What is a cannabinoid
- What are cannabinoids
- Natural cannabinoids
- Slide 18
- Representative cannabinoids
- Slide 20
- Endocannabinoids
- Structure of THC and synthetic analogs
- Slide 23
- Slide 24
- THC
- Results of SAR
- Modes of Absorption
- Smoking and the Body
- Slide 29
- Slide 30
- Metabolites
- Slide 32
- Slide 33
- Cannabis Pharmacology
- Slide 35
- Therapeutic
- Marinol
- Cannabinoid Receptors
- CB1 Receptors
- CB2 Receptor
- Cannabis and Δ9- (THC) for weight loss
- What is obesity
- Slide 43
- Slide 44
- Rimonabant
- Slide 46
- Slide 47
- Slide 48
-
Rimonabant
bull Acompliareg(Sanofi-Aventis)
launched in Europe in 2006 for
oral treatment of obesity at 20 mg
once daily
Selective blocker of central
and peripheral CB1 receptors
It reduces food intake and improves lipid and glucose metabolism
Rimonabant
Despite being efficacious Rimonabant was associated with increased rates of depression and anxiety and therefore removed from the market
- Cannabis
- Slide 2
- Slide 3
- Cannabis spp
- Slide 5
- Slide 6
- Hemp
- What is Marijuana
- Marijuana ndash History of Use
- HempvsMarijuana-1
- HempvsMarijuana-2
- HempvsMarijuana-3
- Cannabis Biology
- Chemical constituents of Cannabis
- What is a cannabinoid
- What are cannabinoids
- Natural cannabinoids
- Slide 18
- Representative cannabinoids
- Slide 20
- Endocannabinoids
- Structure of THC and synthetic analogs
- Slide 23
- Slide 24
- THC
- Results of SAR
- Modes of Absorption
- Smoking and the Body
- Slide 29
- Slide 30
- Metabolites
- Slide 32
- Slide 33
- Cannabis Pharmacology
- Slide 35
- Therapeutic
- Marinol
- Cannabinoid Receptors
- CB1 Receptors
- CB2 Receptor
- Cannabis and Δ9- (THC) for weight loss
- What is obesity
- Slide 43
- Slide 44
- Rimonabant
- Slide 46
- Slide 47
- Slide 48
-
Rimonabant
Despite being efficacious Rimonabant was associated with increased rates of depression and anxiety and therefore removed from the market
- Cannabis
- Slide 2
- Slide 3
- Cannabis spp
- Slide 5
- Slide 6
- Hemp
- What is Marijuana
- Marijuana ndash History of Use
- HempvsMarijuana-1
- HempvsMarijuana-2
- HempvsMarijuana-3
- Cannabis Biology
- Chemical constituents of Cannabis
- What is a cannabinoid
- What are cannabinoids
- Natural cannabinoids
- Slide 18
- Representative cannabinoids
- Slide 20
- Endocannabinoids
- Structure of THC and synthetic analogs
- Slide 23
- Slide 24
- THC
- Results of SAR
- Modes of Absorption
- Smoking and the Body
- Slide 29
- Slide 30
- Metabolites
- Slide 32
- Slide 33
- Cannabis Pharmacology
- Slide 35
- Therapeutic
- Marinol
- Cannabinoid Receptors
- CB1 Receptors
- CB2 Receptor
- Cannabis and Δ9- (THC) for weight loss
- What is obesity
- Slide 43
- Slide 44
- Rimonabant
- Slide 46
- Slide 47
- Slide 48
-
Despite being efficacious Rimonabant was associated with increased rates of depression and anxiety and therefore removed from the market
- Cannabis
- Slide 2
- Slide 3
- Cannabis spp
- Slide 5
- Slide 6
- Hemp
- What is Marijuana
- Marijuana ndash History of Use
- HempvsMarijuana-1
- HempvsMarijuana-2
- HempvsMarijuana-3
- Cannabis Biology
- Chemical constituents of Cannabis
- What is a cannabinoid
- What are cannabinoids
- Natural cannabinoids
- Slide 18
- Representative cannabinoids
- Slide 20
- Endocannabinoids
- Structure of THC and synthetic analogs
- Slide 23
- Slide 24
- THC
- Results of SAR
- Modes of Absorption
- Smoking and the Body
- Slide 29
- Slide 30
- Metabolites
- Slide 32
- Slide 33
- Cannabis Pharmacology
- Slide 35
- Therapeutic
- Marinol
- Cannabinoid Receptors
- CB1 Receptors
- CB2 Receptor
- Cannabis and Δ9- (THC) for weight loss
- What is obesity
- Slide 43
- Slide 44
- Rimonabant
- Slide 46
- Slide 47
- Slide 48
-