2003-2004 Nervous System Pharmacology Review 26 December 2015 9:45 AM.
Pharmacology of Nervous System
Transcript of Pharmacology of Nervous System
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Pharmacology of Nervous System
Learn anatomy and physiology here
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Talk Plan
Classification
Definitions
Neurotransmitters
Drugs acting on CNS
CNS depressants
CNS stimulants
Miscellaneous
Drugs acting on PNS
Sympathetic NS
Parasympathetic NS
Adrenergic drugs
Antiadrenergic drugs
Cholinergic drugs
Anticholinergic drugs
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NERVOUS SYSTEM
CNS PNS
Brain Spinal Cord
Efferent Division
Afferent Division
ANS SNS(Sk. Muscles- Motor)
Sympathetic Parasympathetic EntericSk. Muscles (Sensory)
Nerves
Sm. Muscles & Glands(ANS)
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CNS Pharmacology
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Neurons:Structural &
Functional Unit of NS (10 billion
neurons in brain)
• Chemical substances • Carry messages from
one neuron to another • or from a neuron to
body tissues e.g. Sk. muscles
Neuro- transmitters
:
A Neuron
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Synapse:Small gap separating neurons
Receptors: Macro-molecules
Lipoprotein in nature
Situated on or inside the cell
membrane
Having recognition properties
Synapse
Axon terminal of Presynaptic neuron
Dendrite of Postsynaptic neuron
Fig: Synapse
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Process of Typical Synaptic Connection
Presynaptic membrane or element
Neurotransmitters
Released in Synaptic Cleft
Post synaptic membrane (receptors or ion channels)
Exert action
Action Potential
Activates Ca++ ion Channel
Ca2+ Channel
Na+
K+
Exocytosis of neurotransmitters
+++AP+++- - - -
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Neurotransmitters in CNS
I. Amino acids : Ach, GABA, Glutamate, Glycine
II. Monoamines : NE, Dopamine, Serotonin
III. Peptides : Opioid peptides, Neurotensin, Substance P,
Somatostatin, Neuropeptide Y
IV. Nitric oxide
V. Endocannabinoids
VI. Histamine
VII. Tachykinins
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Drugs acting on CNS
Mainly two groups: CNS depressants CNS stimulants
(Neuraleptics)
Sedatives ….
Hypnotics ….
Narcotics ….
GA …..
Diazepam, Oxagepam etc.
Clobazepam, Nitrazepam etc.
Morphine, Codeine etc.
Barbiturates, Halothane etc.
Directly acting on CNS
Cortical ….
Medullary ….
Spinal ….
Caffeine, Aminophylline, Amphetamine, Ephedrine etc.
Picrotoxin, Adrenaline, Nikethamide etc.
Strychnine, Brucine etc.
Reflexly acting on CNS(Nicotine, Lobetine etc.)
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Drugs acting on CNSAnxiolytics
BarbituratesParkinson’s disease
drugsCNS stimulants
BenzodiazepinesAnticonvulsants
Dopamine antagonistsCholinergics & anticholinergic
PsychedelicsSedatives Hynotics
Tranquilizers Antipsychotics
AnaestheticsAntidepressants
Antiemetics & emetics
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CNS Depressants: Anxiolytics and Sedative-HypnoticsSedatives (anxiolytic): Anxiolytic drug
Reduce anxiety, excitement,
nervousness, irritability
Exert calming effect
Mild depression of CNS
Don’t cause sleep
Little or no effect on motor or
mental functions
Depress CNS to the point that they cause normal sleep
Hypnotics:
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Dose dependent depression of CNS
Non Benzodiazepine Sedative-Hypnotic drugs{
Sedatives
}Hypnotics
Hig
her
Dos
e
Low
er
Dos
e Progressive Depression of CNS
Sedation
Hypnosis
Narcosis
GA
Coma
Death
CNS Depressants: Anxiolytics and Sedative-Hypnotics
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Classification: Sedatives-Hypnotics
I. Benzodiazepines
II. Barbiturates
III. Newer agents (Non-benzodiazepines)
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Sedatives-Hypnotics: BenzodiazepinesBenzene ring fused to seven membered diazepine ring
Frequently prescribed
Favourable side effect
Efficacy, safety
Classification
a) Short acting (t1/2 < 5 hrs)
Midazolam, Triazolam etc.
b) Intermediate acting (t1/2 8-40 hrs)
Lorazepam, Temazepam etc.
c) Long acting (t1/2 40-250 hrs)
Diazepam, Nitrazepam etc.
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MOA of Benzodiazepines
Benzodiazepines
Binds with specific regulatory site on GABA receptor in brain
Enhance GABA activity
Opening of Cl- channels (Enhancement of Cl- conductance)
Hyperpolarization of cells
Depression of CNS
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Pharmacological action: Benzodiazepines
• Anxiolytic• Sedation & induction of sleep• Muscle relaxation (skeletal)• Anticonvulsant effects• Anterograde amnesia• Decrease dose of anaesthetic
CNS effect
s:
Peripheral action:
Neuromuscular blockade (high
dose)
Coronary vasodilation (IV)
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Adverse effects & Choice: Benzodiazepines
a)Normal dose:
b)Acute overdose: Prolong sleep
c)Tolerance & dependency
d)Decrease libido
Dry mouth Light headache Confusion Ataxia Impair driving skill
Adverse effectsAntianxiety (Diazepam)Hypnotics
(Temazepam)Anticonvulsants
(Lorazepam)Anti-tetanus(Diazepam)
Antidepressant(Aprazolam)
Cho
ice
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Sedatives-Hypnotics: Barbiturates
Malonic acid
Barbituric acid
Barbiturates
• Acts within seconds, DOA: 30 mins• Main use: IV anaesthetic
Ultra-short acting(e.g. Thiopental-Na)
• DOA: 2 hours• Main use: Sedative
Short acting(e.g. Pentobarbital)
• DOA: 3-5 hours• Main use: Hypnotic
Intermediate acting(e.g. Amobarbital)
Long acting(Phenobarbitone)
DOA: > 6 hours Main use: Anticonvulsant
Classificatin
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Barbiturates: MOA
Barbiturates + GABAA receptor
Activation of GABA receptor
Opening of Cl- Channel duration of GABA gated channels opening
Hyperpolarization of cells
Potentiate GABA inhibitory action
Barbiturates + AMPA
receptor
Inhibition of AMPA receptor
Inhibition of Glutamate
Depression of CNS
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Barbiturates: Indications & Adverse effects
Anticonvulsants
Sedative & Hypnotics
IV anesthesia
Hyperbilirubinemia
Kernicterous
Cholestasis
DrowsinessOver excitement
Night mares & night terrorsWeakness
Allergic skin reactionLocalized or diffuse painPsychologic dependence
Tolerance
Indications Adverse effects
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Sedatives-Hypnotics: Newer drugs Anxiety & Sleep Disorder
Buspirone & analogs (ipsapirone, gepirone,
tandospirone)Zolpidem Zaleplon
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CNS Depressants: Tranquilizers
Produce calmness & quietness
Reduce anxiety, tension & aggression
Also called “PEACE PILL”
Example: Major: Phenothiazine derivatives (Chlorpromazine,
Promethazine etc.), Reserpine etc.
Minor: Benzodiazepines, Phenobarbitone etc
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CNS Depressants: Anticonvulsant Drugs
Used to treat epileptic seizures
More accurately
called antiepileptic
drugs
carbamazepine (Epitol, Tegretol)
clonazepam (Klonopin)
diazepam (Valium)
divalproex (Depakote)
phenytoin (Dilantin)
Examples
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Anticonvulsant Drugs: MOA
Principle:
Depolarization of nerve: Convulsion
Repolarization of nerve: Returning to normal state
Blocking of Na+ channels
Enhance GABA mediated synaptic inhibition
Ca2+ channel blockade
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Analgesics
Natural (Opium alkaloid):Morphine,
codeine etc:
Synthetic:Pethedine,
Fentanyl etc
Narcotic
Non-Narcotic
NSAIDs Salicylates Paracetamol
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Narcotic VS Non-narcotic analgesic
Narcotic
Highly potent
Addicting
Depress CNS
No AI & AP action
Low TI
Opioid Antagonists… e.g. Naloxane
Addicting Drugs …. e.g. Morphine, Heroin
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Opioids: Actions & MOA (General)
AnalgesiaRespiratory depression
Constipation Urinary Retention
Cough suppressionEmesisMiosis
SedationEuphoria/ Dysphoria
Actions
Elimination of pain
Inhibition of cell firing
Increase K+ efflux, Reduce Ca+ influx, Decrease cAMP
Stimulation of opioid receptors: mu(µ), delta(δ), kappa(ƙ)
MOA
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CNS Stimulants Directly acting on CNS:
i. Cortical stimulants (Amphetamine,
Aminophylline)
ii. Medullary stimulants (Picrotoxin,
Nikethamide)
iii. Spinal stimulants (Strychnine, Brucine)
Reflexly acting on CNS: Nicotine, Ammonia etc.
Mild hyper-excitability
Severe hyper-excitability
Mild convulsion
Severe convulsion
Progressive Grade of CNS excitation
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Miscellaneous
Parkinsonism Levodopa,Amantadine etc.
Multiple Sklerosis Baclofen,Tizanidine etc.
Alzheimer’s Disease Donepezil, tacrine etc.
Myasthenia Gravis azathioprine
Schizophrenia Psychotropic Drugs
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PNS Pharmacology
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PNS: Autonomic VS SomaticSL. NO.
AUTONOMIC SOMATIC
01 Two neurons…to supply smooth muscles & glands
Single neuron to connect CNS to skeletal muscle
02 Peripheral ganglia present Peripheral ganglia absent Synapses are entirely within CNS
03 Pr.G. nerves are myelinatedPo.G. nerves are non-myelinated
Nerves are myelinated
04 Dessection of nerve: some level of spontaneous activity
Dessection of nerve: Paralysis & atrophy of sk. muscles
05 Ach(ganglia & parasym. Neuroeffector junc.)NE(sym. Neuroeffector junc.)
Ach at neuroeffector junc.
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ANS: ClassificationTwo sets of neurons: Afferent: Send impulses to CNS for interpretation Efferent: Receive impulses from the brain & transmits
from the spinal cord to effector organ cells
2 branches: Sympathetic NS Parasympathetic NS
*Ganglia: Contains nerve endings of pre-G. nerve fibers & cell bodies of post-G. nerve fibers
Preganglionic nerve: connects CNS to gangliaPostsynaptic nerve: connects ganglia to organs
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Sympathetic VS Parasympathetic Nerves
SL. NO.
SYMPATHETIC PARASYMPATHETIC
01 Arise from thoraco-lumber (T1 to L3) region of spinal cord
Arise from cranio-sacral (III, VII, IX, X, S2 – S4 region of CNS
02 Ganglia are nearer to CNS. Ratio of Pre & PostG. fibers is generally 1: 20 or more. So, PostG. fibers are longer
Ganglia are away from CNS (close to organs). Ratio is generally 1:1. So, postG. fibers are shorter
03 Ach (in ganglia) & NE (at neuroeffector junc.)
Ach in both ganglia & neuroeffector junc.
04 Sym. Activities increases in stress & emergency
Parasym. Activity predominates during rest
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(Dilates pupil)
(Constricts pupil) Saliva
Saliva Rate
Rate
(Bronchial muscle relaxation)
(Bronchoconstriction)
Glycogen glucoseBile secretion
GIT Motility
Motility
Urine
Urine Sphincter contraction
Bladder relaxation
Sphincter relaxation
Bladder contraction
Preg-ContractionNonpreg-relaxation (Contraction)
ANS ĉ EFFECTS
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Sympathetic VS Parasympathetic: EFFECTSSL. NO.
TISSUES SYMPATHETIC PARASYMPATHETIC
01 Eye(Pupil) Dilation Constriction02 Sali. gland Saliva reduction (Dry mouth) Increased salivation03 Heart Increases heart rate Decreases heart rate04 Bronchus Smooth muscle relaxation SM contraction 05 Arteries Constriction Dilation06 GIT Decreased motility, secretion Increased motility, secretion07 Liver Convert glycogen to glucose Stimulates secretion of bile08 Bladder Sphincter contraction & sm
relaxationSphincter relaxation & sm contraction
09 Kidney Decreased urine Increased urine10 Uterus Contract(Pg.),Relax(Non-Pg) Contraction in both condition
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ANS: Neuro-Humoral Transmission
Sympathetic nerves (adrenergic) : NE or NA (PostG.)
Parasympathetic nerves (cholinergic): Ach (PostG.)
PreG. nerve endings of both (Sym. & Parasym.-in
ganglia) : ACh
Principal neurotransmitters:
Other neurotransmitters:NOSerotoninATPDopamine
GABA
Purines
peptidesEffector organs
CNS
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ANS: Sympathetic Nervous System (Adrenergic)
Drugs that mimic action
of SNS: Adrenergic drugs
Drugs that inhibit
action of
sympathomimetics:
Anti-adrenergic/
sympatholytic drugs
Neurotransmitters: NE, E, Dopamine
Phenylalanine
Tyrosine
DOPA
Dopamine
NE/NA
Epinephrine
PA hydroxylase in liver
Tyrosine hydroxylase
DOPA decarboxylase
Dopamine-β-hydroxylase
PNMT in AM
Stored within SV
Action potential
Influx of Ca2+
Fusion with SV
Exocytosis of NE
Acts on receptors
Synt
hesi
s of
cat
echo
lam
ines
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SNS (Adrenergic) : Classification Based on MOA: (3 categories)
i. Direct acting
ii. Indirect acting (e.g. Amphetamine)
iii. Mixed acting (e.g. Ephedrine)
α agonists Nonselective e.g. NE, Epinephrine
Selective (α1 & α2 agonists)e.g. Clonidine, Phenylephrine
β agonists Nonselective e.g. Isoproterenol
Selective (β1 & β2 agonists) e.g. Dobutamine, Salbutamol
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SNS (Adrenergic) : Receptors & action4 types of adrenergic receptors in organ cells:
α1 : Vasoconstriction of blood vessels, Inc. BP, Dec. GI motility,
Contracts UB sphincter, Dilates pupil, Contracts uterus
α2 : Inhibits release of NE, Dec. BP, Dec. intestinal secretion
β1 : Inc. heart rate & force of contraction of heart (cardiac
stimulant)
β2 : Relaxation of sm in bronchi (Bronchodilator), uterus,
peripheral BV, Stimulates insulin secretion
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Adrenergic Drugs: Clinical Uses
1) Cardiovascular systemCardiac arrest (Adrenaline)
Heart block (Isoproterenol)
Cardiogenic shock (Dobutamine, Dopamine)
2) Anaphylactic reaction Adrenaline
3) Miscellaneous
Prolong action of LA by vasoconstriction (Adrenaline)Bronchial asthma by Bronchodilation (salbutamol, adrenaline)
Allergic rhinitis (Adrenaline)
Dilating pupil (Ephedrine)
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Anti-adrenergic Drugs (Sympatholytic Drugs)
Classification Adrenergic neuron blockers
(e.g. Methyldopa, Reserpine)
Adrenergic receptor blockers
(α & β antagonists)
α-agonists β-agonistsα1 (e.g. Prazocin) β1 (e.g. Atenolol)
α2 (e.g. Idazoxan) β2 (e.g. Butoxamine)
Non-selective (e.g. Tolazoline)
Non-selective (e.g. Propranolol)
General IndicationsHypertensionVisceral ischemiaAngina pectorisMyocardial infarctionCardiac dysrhythmias
Adverse effectsHypotension
Bradycardia
Edema
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ANS: Parasympathetic Nervous System (Cholinergic) Neurotransmitter: ACh
CH3COO- + ATP + CoA = CH3COSCoA
(Acetyl-Co-A)
Choline + Acetyl-Co-A
Ach (stored in SV)
Action Potential
Opening of Ca2+ channel
Influx of Ca2+
Fusion of SV ĉ Axonal
membrane
Exocytosis of Ach
Acts on receptor of
PostG. Neuron
Action
Pres
ynap
tic n
euro
n &
oth
er c
ells
CATAChE in synaptic cleft Inhibits ACh
Post
syna
ptic
neur
on
CH3COO- + ATP + CoA = CH3COSCoA
(Acetyl-Co-A)
Choline + Acetyl-Co-A
Ach (stored in SV)
Action Potential
Opening of Ca2+ channel
Influx of Ca2+
Fusion of SV ĉ Axonal
membrane
Exocytosis of Ach
Acts on receptor of
PostG. Neuron
Action
Pres
ynap
tic n
euro
n &
oth
er c
ells
AChE in synaptic cleft Inhibits ACh
Post
syna
ptic
neur
on
Drugs that mimic
action of Parasym. NS:
Cholinergic/
Parasympathomimetic
drugs
Drugs inhibits action of
parasympathomimetics
: Anti-Cholinergic/
Parasympatholytic drugs
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Parasym. NS (Cholinergic) : Classification
Direct acting (e.g. Ach, Pilocarpine, Arecoline)
Indirect acting
Irreversible AChE agents (e.g. Malathion, Carbaryl)
Reversible AChE agents (e.g. Physostigmine,Neostigmine)
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Cholinergic receptors & Responses
Types :Muscarinic receptors (M1, M2, M3, M4, M5) & Nicotinic receptors (Nm, Nn)
Vasodilation
Dec. cardiac output
Inc. GI motility, tone
& secretion
Relax of GI
sphincters
Sweating
Contracts gall
bladder
Bronchoconstriction
Causes urination
Inc. tone & motility
of uterus
Miosis
Muscarinic responses Muscular fasciculations
Paralysis (long term
action)
Release of adrenaline
from Adrenal medulla
(Inc. BP)
Nicotinic responses
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Cholinergic Drugs: Clinical Uses
Myasthenia gravis* (Physostigmine, Neostigmine)
Glaucoma: To reduce IOP (Physostigmine 0.5-1%)
Ruminal impaction (Physostigmine 30-40 mg SC inj. In cattle)
To control ectoparasites (Carbaryl, Trichlorfon)
As antidote in atropine poisoning (Physostigmine)
Urinary retention (Neostigmine)
In snake bite: specially cobra bite (Neostigmine + atropine to
prevent res. Paralysis)
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Anticholinergic (Parasympatholytic) DrugsNonselective muscarinic receptor antagonists (Atropine, Scopolamine)
Selective muscarinic antagonists (e.g. Pirenzepine-M1 antagonists)
Clinical uses To dilate pupil (Homatropine)
In bronchial asthma (Ipratropium)
In OPI, carbamate & Myshroom poisoning)
As anti-parkinsonism drug
As anti-emetic
As spasmolytic
Dec. hypermotility of GIT
Dec. hypertonicity of uterus, UB, Ureter, BronchiolesAs pre-anesthetic (Atropine sulfate)
Peptic ulcer (Pirenzepine)
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Thanks To All