3rd Pharmacy N bases - Include alkaloids derived from immidazole ring, the nucleotides (xanthine...
Transcript of 3rd Pharmacy N bases - Include alkaloids derived from immidazole ring, the nucleotides (xanthine...
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Mohammed N. Sabir
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3rd Pharmacy – N.41
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A group of alkaloids
in which the
nitrogen atom is not
hetercyclic
(Protoalkaloids) also called atypical alkaloids.
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Most are derivatives
of Phenylethylamine
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Examples on alkaloids
belongs to this class:-
1-Ephedrine
2-Cathinone
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3-Colchicine
4-Capsaicine
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1-Ephedra (ma huang)
The overground part of
Ephedra sinica (Ephedrales
or Ginetaceae)
In Chinese:
ma = astringent
huang = yellow
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This plant has been used in
Chinese herbal medicine
since 5000 years ago;
While in modern medicine since
1923.
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The plant is indigenous to
China and to many parts in
Asia including Kurdistan
Region-Iraq.
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The plant is a shrub with
about 50-100cm height.
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The major alkaloid is Ephedrine (-)-Erythro-α-[1
(methylamino)ethyl]benzyl alcohol
Production is either by extraction from the plant or chemical
synthesis.
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Chemical synthesis from benzylhydroxymethyl ketone and methylamine.
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Ephedrine occur as white
needle-like crystals soluble in
water, alcohol, chloroform,
ether and petroleum ether.
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It is structure similarity to the
endogenous catecholamines
makes it potent
sympathomimetic agent,
stimulating both α and β-
adrenergic receptors.
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Ephedrine and
Pseudoephedrine are mixed
action adrenergic agonists.
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Medicinal uses (Ephedrine sulphate and Ephedrine. HCl)…
o Bronchodilator.
o Allergy.
o Cough suppressant.
o Increase BP during shock.
o Vasoconstrictor.
o Decrease inflammation and mucus secretion.
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Adenylate cyclase
ATP c-AMP
PKA (c-AMP dependent PK)
Ca++
Na+
Ca++
Beta adrenergic activity
PharmacologicAction
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Alpha 2 adrenergic activity
PharmacologicAction
Adenylate
cyclase
ATPc-AMP
PKA
(c-AMP dependent PK)
Ca++
Na+
Ca++
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beta2Muscle
beta2Muscle
Tissue Receptor Subtype
Heart beta1
Adipose tissue beta1beta3?
Vascular Smooth
Airway Smooth
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At large doses:-
1-
2-
3-
4-
5-
6-
Hypertension
Headache
Dizziness
Palpitation
Vomiting
Toxicities ofEphedrine
Nervousness and insomnia(CNS-effects)
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Available as (Ephedrinesulfate & Ephedrine HCl)
Pharmaceutical dosageforms:-
1-Tablets
2-Oral liquid dosage forms
3-Inhalations
4-Injections
Clinical uses:-
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Ephedrinederivatives
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Compounds with lessα-receptor affinity
N-MethylephedrineNorephedrine
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Colchicine
Is the dried ripe seed of
Colchicum automnale
(Fam: Liliaceae)
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Colchis = refers to the plant
flourishes
Autumnale = refers to the
Season where the plant
bloom
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The plant is indigenous to Europe and North Africa
The Arabs recommended the use of the corn for
Gout.
Colchicum contains the Colchicine (0.6-0.8%).
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Colchicine is a weak base and almost
lacks basicity since it does not react
with acids as other alkaloids do,
however; it is precipitated by the
detecting reagents.
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Biosynthesis
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- Inhibition of leucocyte migration.
- Reduction of lactic acid production.
- Decrease deposition of uric acid.
- Reduction of phagocytosis leading to decrease
the severity of inflammation.
Mechanism of action
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Colchicine is also antimitotic agent through affecting the
chromosomes of the cell, in which it will still divided but
without the formation of the spindle fibers and subsequent
cell division.
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For such activity, colchicine has been used in
investigation for its anticancer activity in
animals.
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Pathophysiology of Gout
Uric acid, the end product of purine
metabolism, is considered a waste product and
serves no known physiologic purpose in
humans.
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lacking the enzyme Urate-oxidase (Uricase), which further
degrades uric acid to allantoin, a substance that is more
water soluble and more readily excreted by the kidneys.
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Uricase
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Excessive uric acid accumulation contributes to
hyperuricemia (defined as an elevated serum uric
acid (sUA) level above 7mg/dl in men and above
6mg/dl in women)
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It is considered to be the principle cause of
gouty arthritis which describes acute and chronic
clinical manifestations caused by the deposition
of monosodium urate crystals in articular and
extra articular tissues.
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Urate crystals
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-Asymmetric swelling within joint on a radiograph
-First metatarsophalangeal joint
is tender or swollen
-Hyperuricemia
-Maximal inflammation
developed within 1 day
-Monoarthritis attack
-More than one acute arthritis
attack
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-Redness observed over joints
-Subcortical cysts -Unilateral
first metatarsophalangeal
joint attack
-Unilateral tarsal joint attack
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Recent research has identified hyperuricemia as an
independent risk factor for metabolic syndrome,
coronary artery disease, and chronic kidney disease.
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Gout refers to disease that occurs in response to
the presence of crystals of monosodium urate
(MSU) in joints, bones, and soft tissues.
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Consist of the fresh leaves of
Catha edulis (Celastraceae)Khat
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The plant is a tree native to
tropical East Africa.
The plant part that is rich
with the alkaloid is the leaf.
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Fresh leaves contains more
alkaloids when compared to
the old ones which contains
the less active metabolite
(+)-norephedrine.
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The leaves are Chewed
habitually by the
inhabitants.
Inhibiting the sensation of
hunger and fatigue.
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The WHO does not classify Khat a
habitual drug that cause
addiction, however; France
consider it as one of the
narcotics.
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Catha edulis contains
phenylalkylamine alkaloid (-)-
cathinone.
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Cathinone actions are analogues to (+)-amphetamine
including:-
Induction of catecholamine release from storage sites (CNS
stimulant action).
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Psychological effects include
▪Euphoria
▪Anxiety
▪Increased
▪Alertness
libido
▪Concentration
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- Energy
- Self-esteem
- Self-confidence
- Sociability
- Irritability
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- Aggression
- Psychomotor agitation
- Repetitive and obsessive behavior
- Paranoia
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With chronic and/or high doses, amphetamine psychosis
can occur.
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Capsaicin…
Derived from Capsicum annuum (Solanaceae)
Chili pepper.
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Used topically as circulatory stimulant and
analgesic for arthritis , neuropathy, neuralgia
and as anesthetic.
Also used in psoriasis to decrease itching and
inflammation.
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It binds selectively to a protein capsaicin receptor (CR)
on the membranes of pain and heat-sensing neurons.
CR is a heat-activated calcium channel that opens
between (37 – 45)°C .
Upon binding it causes the channel to open below 37°C, which is
why capsaicin is linked to the sensation of heat.
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Prolonged activation causes depletion of
presynaptic substance P.
Neurons that do not contain capsaicin receptors
will be unaffected.
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A study in 2003 showed that capsaicin
regulate blood sugar levels through
affecting carbohydrate breakdown after meals.
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Oil of Capsicum
Oil of Capsicum derived from chili pepper (Capsicum spp.)
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Medicinal uses:-
1- Analgesic (topical ointments, dermal patches) in
concentrations 0.025-0.25%.
2- In nasal sprays as decongestant anti-inflammatory.
3- In arthritis.
4- Neuralgia.
5- Reduce itching and inflammation (as creams in
psoriasis).
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Purinebases
- Include alkaloids derived from
immidazole ring, the nucleotides
(xanthine bases)
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Those which retaintherapeutic activities are:-
1-Caffeine (1,3,7-trimethylxanthine)
2-Theophylline (1,3-
dimethylxanthine)
3-Theobromine (3,7-
dimethylxanthine)
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Base Numbering
structures of the five major purine (R) and pyrimidine (Y)
bases of nucleic acids in their dominant tautomeric forms
and with the IUPAC numbering system
Source: Blackburn and Gait, Nucleic acids in chemistry and biology, Oxford University Press New York 1996.5/16/2017 68
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Methylxanthines
are biosynthesized from Aspartic
acid, Glycine, Glutamine
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1- Caffiene
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A purine alkaloid belongs to xanthine
class.
White crystalline powder with bitter
taste.
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Caffeine is found in
varying quantities in
the seeds, leaves, and
fruit of some plants
like (Camelia sinensis,
Coffea arabica)
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ServiceSize
CoffeesCaffeine (mg)
200) (16 oz. = 266)
Starbucks Brewed Coffee (Grande) 16 oz. 320
Dunkin' Donuts regular coffee 16 oz. 206
Coffee, generic instant 8 oz. 93 (range: 27-173)
Starbucks Espresso, doppio 2 oz. 150
Starbucks Espresso, solo 1 oz. 75
Espresso, generic 1 oz. 40 (range: 30-90)
Starbucks Espresso decaffeinated 1 oz. 4
Einstein Bros. Espresso 1 oz. 75
Starbucks Frappuccino Blended Coffee Beverages, average 9.5 oz. 115
Coffee, generic decaffeinated 8 oz. 5 (range: 3-12)
Starbucks Vanilla Latte (Grande) 16 oz. 150
Einstein Bros. regular coffee 16 oz. 300
Coffee, generic brewed 8 oz. 133 (range: 102-
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Teas Service Size
8 oz.
Caffeine (mg)
53 (range: 40-120)Tea, brewed
Snapple, Lemon (and diet version) 16 oz. 42
Snapple Raspberry (and diet version) 16 oz. 42
Nestea 12 oz. 26
Arizona Iced Tea, green 16 oz. 15
Snapple, Kiwi Teawi 16 oz. 10
Snapple, Just Plain Unsweetened 16 oz. 18
Arizona Iced Tea, black 16 oz. 32
Snapple, Peach (and diet version) 16 oz. 42
Starbucks Tazo Chai Tea Latte (Grande) 16 oz. 100
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Chocolates/Candies/Other Service Size Caffeine (mg)
Hershey's Special Dark ChocolateBar
1.45 oz. 31
Hershey's Kisses 41g (9 pieces) 9Hot Cocoa 8 oz. 9 (range: 3-13)
Hershey's Chocolate Bar 1.55 oz. 9
Jolt Caffeinated Gum 1 stick 33
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Over-The-Counter Drugs Service Size Caffeine (mg)
Vivarin 1 tablet 200
Anacin (Maximum Strength) 2 tablets 64Excedrin (Extra Strength) 2 tablets 130
NoDoz (Maximum Strength) 1 tablet 200
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Theophylline Thebromine
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Mechanisms of action
Competitive nonselective phosphodiesterase
inhibitor, thereby increasing intracellular c-AMP,
and inhibiting TNF-α and leukotriene synthesis,
thus reducing inflammation and innate immunity
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Nonselective adenosine receptor antagonist,
antagonizing A1, A2, and A3 receptors which is
responsible for its cardiac effects
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Antibiotics
Mohammed N. Sabir
Pharmacognosy II, Third Year
15-May-17 1
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15-May-17 2
Lecture outline…
• Introduction & History
• Development trends
• Screening for Antibiotics
• Commercial production of antibiotics
• Increasing commercial yield
• Recovery & Isolation
• Manipulation of the formulation
• Rational antibiotic therapy
• Classification of antibiotics
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Introduction and History… Moldy breads & soy bean curds
15-May-17 3
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15-May-17 4
Pyocynase (first commercial antibiotic)
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15-May-17 5
Alexander Fleming and
Penicillin
1928
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Development of antibiotics… - Screening
- Isolation of mutant M.O.
- Isolation of metabolites
- Chemical modification
- In vitro assessment
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Screening for antibiotics… Method of screening
15-May-17 7
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Screening for antibiotics should be:- Simple
Rapid
Cheap
15-May-17 8
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15-May-17 9
Actinomycetes
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15-May-17 10
Cycloheximide or Phenol 1 :140
Disinfectant soil sample
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15-May-17 11
Inhibition zones
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Commercial production of antibiotics… Requirements for production
15-May-17 12
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15-May-17 13
Production involves large
fermentation tanks…
The Vegetative growth cultures
are kept through lyophilisation…
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15-May-17 14
Advantages of large standard inoculum…
1- Reduce incubation time.
2- Decrease the chance for contamination.
3- Provide optimal nutritional and environmental
conditions for growth.
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15-May-17 15
NH3N
Mycelial N2
Sugar (Glucose + Lactose)
pH
0 20 40 60 80 100 Time (Hours)
0
400
80
0
Pe
nici
llin
Conc
./ m
l
Nitr
ogen
gm
/l , S
ugar
gm
/100
ml
0
1
2
3
Penicillin
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Increasing commercial yield… Factors that affect Quantity and Quality of production
15-May-17 16
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15-May-17 17
Bacillus subtilis provide optimal yield of Bacitracin when
the C/N = 15
At lower or higher ratios the yield is less or produce
undesirable antibiotics.
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15-May-17 18
Phenyl acetamide and ampicillin… Phenyl acetic acid and penicillin G… Acyl moieties and Penicillin-V…
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15-May-17 19
Increasing Commercial Yield
-Specialized penicillins are prepared by semisynthetic processes.
-Mercaptothiazole in cultures of Streptomyces aureofacciens
enhances production without being incorporated to the AB
structure.
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15-May-17 20
Mercaptothiazole and tetracycline…
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15-May-17 21
Addition of enhancers…
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15-May-17 22 15-May-17 Pharmacognosy II - Antibiotics 22
In penicillin production Lysine inhibits the antibiotic
production.
Sugar Amonia
Α-amino adipic acid
-ve feedback (inhibition or repression)
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15-May-17 23
Biosynthetic pathway for penicillin-G
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Recovery & isolation…
15-May-17 24
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Purity of the product will decrease the toxicities, example:-
Vancomycin when purified, the nephrotoxicity will be decreased.
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-Masking microbial contamination for ABs (to be used
as injectable):-
1. Appropriate treatment before testing sterility.
2. Microfiltration.
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Manipulation of formulations… Chemical and physical Why we do formulation changes?
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Rational antibiotic therapy… Causative agent…
Sensitivity tests…
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Susceptibility tests are performed either by Kirby-Bauer
testing or by turbidity testing to determine a MIC.
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Criteria for ideal antibiotic...
Patient factors for selecting antibiotics…
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Classification of antibiotics…
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Cell-wall synthesis inhibitors…
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Pharmacognosy II - Antibiotics
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Classification of antibiotics…
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Katzung & Trevor’s Pharmacology 2005®
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Cell wall structure…
www.chemie.uni-hamburg.de
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Peptidoglycan…
en.wikipedia.org
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www.sigmaaldrich.com
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www.3dscience.com
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Mechanisms of resistance:-
1- Through changing the structure of PBPs.
2- Through production of β-lactamases (plasmid
mediated).
3- Through changing the structure of Porin.
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Chemistry of betalactams…
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Piperacillin Ticarcillin
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Vancomycin