Worksheet B

Worksheet B - John Diep Bimm118 Cholinergic System Drug...

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John Diep Bimm118 Cholinergic System Direct Parasympathomimetics – drugs that mimic ACh and mostly binds mAChR Indirect Parasympathomimetics – drugs that inhibit ACh-Esterase; raises [ACh] Muscarinic Parasympatholytics – competitive antagonists Nicotinic Parasympatholytics – neuromuscular junction blockers; muscle relaxants 1 Drug Names/Classes Used for: Parasympathomimetics Indirect ACh R Agonists Reversible Carbamates (Physo stigmine) Indicated for glaucoma. Antidote for atropine poisoning. Quarternary Alcohol (edrophonium) Diagnose Myasthenia Gravis Horny Goat Weed Indicated for erectile dysfunction Irreversible (Organo- Phosphates) Insecticide (mala thione ) Insects… Nerve Gas (Sarin) Lethal. Use atropine as antidote. Direct ACh R Agonists Carbachol Indicated for glaucoma Bethanechol Indicated for urinary retention. Pilocarpine Indicated for Glaucoma Parasympatholytics mACh R Blockers Atropine Causes pupil dilation, increases HR (indicated for bradycardia), reduces bronchosecretion (for surgery) Antidote for organophosphate poisoning. Scopolamine Indicated for motion sickness; antiemetic drug delivered transdermally Pirenzipine Indicated for peptic ulcers; selectively blocks M1 Receptors, reduces gastric acid secretion nACh R Blocerks Non- Depolarizing Tubocuraraine Poison; respiratory paralysis. Muscle relaxant. Competitive antagonists Pan curonium Atra curium Muscle relaxants; competitive antagonists Depolarizin g Succinylcholine/ Suxamethonium Muscle relaxants nACh R agonists, but has parasympatholytic effect
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John Diep Bimm118 Non-Depolarizing – competitive antagonists; competes with ACh to prevent depolarization Depolarizing – nACh R agonist; initially mimics ACh causing depolarization but it is not hydrolyzed by ACh-Esterase so the depolarization is prolonged, inhibiting other signals Nicotine Low Concentration – acts as a direct nAChR agonist High Concentration – has an antagonistic effect on nAChR due to channel inactivation; similar to succinylcholine. nAChR = nicotinic acetylcholine receptor mAChR = muscarinic acetylcholine receptor 2
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John Diep Bimm118 Adrenergic System Drug Name/Class Used For: Sympathomimetics Indirect Agonists MAO Inhibitors (Tranylcypromine, Moclobemide) Indicated for depression; inhibits metabolism of NE/E, DA, and 5HT; many side effects Ephedrine Found in diet pills; displaces NE from storage vesicles Amphetamines Ritalin ADD Fenfluramine diet pills Displaces NE from storage, inhibits reuptake, inhibits MAO Direct Agonists Non-selective Epinephrine(Adrenaline) Indicated for anaphylactic shock and used as an adjuvant in local anesthetics. Dilates bronchii. Norepinephrine (Noradrenaline) Limited clinical use. Selective
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Worksheet B - John Diep Bimm118 Cholinergic System Drug...

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