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31 Cards in this Set
- Front
- Back
choline transporter (CHT) can be inhibited by
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hemicholiniums
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vesicle-associated transporter (VAT) can be inhibited by
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vesamicol
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VAMPs and SNAPs can be blocked by
(especially the VAMP synaptogamin) |
botulinum toxin
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Acetylcholine (Ach) receptors and effects at moderate dose
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M3 - vasodilation, decreased TPR, reflex tachycardia
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Acetylcholine (Ach) receptors and effects at high doses
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M2 - bradycardia, decreased AV conduction, negative inotrope
M3 - bronchial constriction, secretion, salivating, sweat, urine, tears |
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Methacholine characteristics and uses
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- longer half life
-diagnose bronchiolar hypersensitivity - dx belladonna alkaloid poisoning |
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Carbachol effects, uses, adverse effects
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nicotinic effects - autonomic ganglia, adrenal medulla, skeletal muscle
uses - topically in glaucoma adverse - high doses - muscarinic effects on the heart -- cardiac arrest |
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Bethanechol charac, uses
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-not susceptible to AchE, predominately M3, no nicotinic action
uses - reduce reflux (increase LES tone), urinary retention (detrusor contraction, decrease outlet resist of internal spincter) |
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muscarinic choline esters
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-acetylcholine
-methacholine -carbachol -bethanechol |
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muscarinic alkaloids
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-muscarine
-pilocarpine |
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muscarine characteristics and symptoms
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activates muscarinic receptors with 100-fold potency of Ach
not destroyed by AchE, longer half life no nicotinic activity sx - salivation, sweating, tear flow; large doses - abd pn, nausea, diarrhea, blurred vision, dyspnea |
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pilocarpine effects
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muscarinic - opthalmic effects predominate
- contracts spincter - miosis -frees canal of Schlemm (narrow angle) -enhances tone of trabecular network (wide angle) -contracts ciliary - accommodation |
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nicotinic alkaloids
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nicotine
succinylcholine (nicotinic receptor agonists) |
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nicotine effects and use and
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Nm - skeletal m contraction, depolarizing blockade
Nn - increased HR, vasoconstriction,gut motility and secretion, incresed resp rate, nausea and vomiting --for smoking cessation |
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contraindications of cholinoceptor agonists
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- peptic ulcers, GI disorders, asthma
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Drugs that block effects of muscarinic agonists
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- quinidine
- procainamide - tricyclic antidepressants |
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indirect acting cholinomimetics
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reversible - edrophonium, physostigmine, neostigmine, donepezil, tacrine
irreversible - echothiphosphate, malathion, parathion, sarin |
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erdophonium charac and uses
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short acting
dx - differentiate MG from cholinergic crisis |
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physostigmine charac and use
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-tertiary amine, enters CNS
- glaucoma, antidote in atropine od |
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neostigmine, pyridostigmine charac and use
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quternary amine, doesnt enter CNS
- ileus, urinary retention, MG, reversal of non-depolarizing NM blockers |
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Donepezil and Tacrine charac and use
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-lipid soluble (CNS)
-Alzheimer's |
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Organophosphates charac and use
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-lipid soluble, long-acting AchE irriversible inhibitors
- glaucoma (echothiophosphate) insecticides - malathion, parathion nerve gas - sarin |
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sx of AchE inhibitor intoxication
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Diarrhea
Urination Miosis Bronchiolar constriction Bradycardia Excitement Lacrimation Sweating Salivation |
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muscarinic receptor antagonists
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-atropine
-ipratropium -benzotropine |
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nicotinic receptor antagonists(Nn and Nm)
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hexamethonium
mecamylamine |
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neuromuscular blocking drugs
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non-depolarizing - D-turbocurarine
depolarizing - succinylcholine |
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ipratropium prop, effects, uses
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-M3 in bronchial SMCs and glands when inhaled, no CNS absorption
-decreases bronchoconstriction and secretions -chronic obstructive lung disease and asthma |
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benztropine prop, effects, uses
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-CNS absoption, muscarinic in brain
-dopaminergic-cholinergic balance, decrease GI/GU secretions, decrease motility, increase HR -parkinson's |
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ganglionic blocking agents
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hexamethonium and mecamylamine
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D-turbourarine charac
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-non-depolarizing neuromuscular blockers
-small doses prevent opening of Na channel |
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succinylcholine charac
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-persistent depolarization, augmented by AchE inhibitors
-repolarization but desensitized |