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35 Cards in this Set
- Front
- Back
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acetylcholine
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cholinoceptor agonist; acetic acid ester of choline
muscarinic and nicotinic action organ system effects: muscarinic - eye - miosis, accommodation, aqueous humor outflow; CV - reduce periph vasc R, slow HR - direct!, vasodilation via NO (vasodilation masks constriction - direct effect on vasc SM), low dose causes an SNS reflex and incr in HR, larger ACh doses mask this and --> bradycardia; respiratory - contracts SM of bronchial tree, stimulates glands, exacerbates asthma; GI - secretions, peristalsis; GU - detrusor contraction, relaxes trigone and sphincter; glands - stims thermoreg sweat glands; nicotinic - autonomic ganglia - site of action, simulataneous SNS and PNS discharge, predominant tone predicts effects, SNS - vasculature, PNS - most other tissues, NMJ - muscle fasciculations, depolarization blockade --> flaccid paralysis poorly absorbed, poorly distributed to CNS; rapidly hydrolyzed |
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methacholine
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cholinoceptor agonist; acetic acid ester of methylcholine
methyl group - lower potency at nicotinic receptor, only muscarinic action see acetylcholine but ONLY muscarinic more resistant to hydrolysis |
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carbachol
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cholinoceptor agonist; carbamic acid ester of alcohol
muscarinic and nicotinic action very resistant to hydrolysis, longer duration of action |
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bethanechol
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cholinoceptor agonist; carbamic acid ester of alcohol
methyl group - lower potency at nicotinic receptor; only muscarinic action very resistant to hydrolysis, longer duration of action |
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pilocarpine
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cholinoceptor agonist; alkaloid
tertiary alkaloids - penetrate CNS |
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nicotine
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cholinoceptor agonist; alkaloid
tertiary alkaloids - penetrate CNS fatal at 40 mg, CNS stimulation - convulsions, coma, respiratory arrest, skeletal muscel end plate depolarization - respiratory paralysis, HTN and cardiac arrhythmias, tx is symptom directed - muscarinic and adrenergic antagonists and mech respiration; most sign toxicity - due to chronic use |
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lobeline
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cholinoceptor agonist; alkaloid
plant derivative similar to nicotine tertiary alkaloids - penetrate CNS |
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edrophonium
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cholinesterase inhibitor
simple alcohol w/ quaternary ammonium group, reversibly binds to active site CIs in general: CV GI/GU - tx clinical disorders related to inactivity of SM (postop ileus, congenital megacolon, urinary retention, etc.), eye - tx closed angle glaucome (outflow of aqueous humor), and skeletal muscle effects, amplify the actions of endogenous ACh, little effect on vasc smooth muscle and blood pressure, modify tone of PNS (does NOT innervate periph vasculature), at NMJ - low concentrations increase force of contraction, higher doses produce depolarizing neuromuscular blockade, tx myasthenia gravis (dx test), tx atropine and other pure anticholinergic intoxication, tx Alzheimers - CNS very short duration of action (2-10 min) SLUDGE: salivation, lacrimation, urinary incontinence, diarrhea, GI cramps, emesis; can be reversed by atrophine; poisoning also tx by: maintenance of vitals (respiration), decontamination to prevent further absorption, atropine parenterally in large doses; therapy may also include tx w/ pralidoxime to rescue un-aged inhibited enzyme |
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neostigmine
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cholinesterase inhibitor - carbamate
2-step hydrolysis, covalent bond of carbamoylated enzyme - resistant to hydration quaternary ammonium, stays in periphery! |
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physostigmine
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cholinesterase inhibitor - carbamate
2-step hydrolysis, covalent bond of carbamoylated enzyme - resistant to hydration tertiary ammonium - penetrates CNS, duration of effect depends on stability of inhibitor-enzyme complex |
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carbaryl
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cholinesterase inhibitor - carbamate
2-step hydrolysis, covalent bond of carbamoylated enzyme - resistant to hydration high lipid solubility, rapid CNS effects |
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pyridostigmine
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cholinesterase inhibitor - carbamate
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echothiophate
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cholinesterase inhibitor - organophosphate
high affinity for cholinesterase, long lasting inhibition, covalent P-enzyme bone is stable, lasts hundreds of hours (lifetime of enzyme), "aging" strengthens bond, but b4 aging, pralidoxime can restore enzyme fxn well absorbed topically, distributed to all parts of body, including CNS |
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soman
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cholinesterase inhibitor - organophosphate
high affinity for cholinesterase, long lasting inhiibtion; covalent P-enzyme bone is stable, lasts hundreds of hours (lifetime of enzyme), "aging" strengthens bond, but b4 aging, pralidoxime can restore enzyme fxn well absorbed topically, distributed to all parts of body, including CNS |
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sarin
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cholinesterase inhibitor - organophosphate
high affinity for cholinesterase, long lasting inhiibtion; covalent P-enzyme bone is stable, lasts hundreds of hours (lifetime of enzyme), "aging" strengthens bond, but b4 aging, pralidoxime can restore enzyme fxn well absorbed topically, distributed to all parts of body, including CNS |
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malathion, parathion
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cholinesterase inhibitor - organophosphate
high affinity for cholinesterase, long lasting inhibtion; covalent P-enzyme bone is stable, lasts hundreds of hours (lifetime of enzyme), "aging" strengthens bond, but b4 aging, pralidoxime can restore enzyme fxn well absorbed topically, distributed to all parts of body, including CNS |
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isoflurophate
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cholinesterase inhibitor - organophosphate
high affinity for cholinesterase, long lasting inhibtion; covalent P-enzyme bone is stable, lasts hundreds of hours (lifetime of enzyme), "aging" strengthens bond, but b4 aging, pralidoxime can restore enzyme fxn well absorbed topically, distributed to all parts of body, including CNS |
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diisopropylfluorophosphate (DFP)
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cholinesterase inhibitor - organophosphate
high affinity for cholinesterase, long lasting inhibtion; covalent P-enzyme bone is stable, lasts hundreds of hours (lifetime of enzyme), "aging" strengthens bond, but b4 aging, pralidoxime can restore enzyme fxn well absorbed topically, distributed to all parts of body, including CNS |
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donepezil
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cholinesterase inhibitors - others
predominantly nicotinic, high activity in CNS alzheimers |
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tacrine
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cholinesterase inhibitors - others
anticholinesterase and cholinomimetic alzheimers |
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atropine
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anticholinergic - muscarinic antagonist
tertiary amine, causes reversible (competitive) blockade, not selective b/t M1, M2, and M3 subtypes eye or CNS effects; CNS - if toxic doses, agitation, hallucinations, coma (used w/ L-dopa in parkinsons) mydriasis, cycloplegia, contraind in acute glaucoma, CV - tachycardia, can cause cutaneous vasodilation; respiratory - bronchodilation, reduction of secretion, GI - reduces motility, reduces secretion, preop b4 abdominal surgery, GU - urinary retention, sweat glands - suppresses thermoreg sweating; therapeutic apps: Parkinsons, motion sickness, ophthalmoscopic exam, preop med (prevents laryngospasm), relieves bronchodilation (asthma and COPD), relief of vagal syncope, atropine esp - tx sinus bradycardia, cardiopulm resuscitation; travelers diarrhea, GI hypermotility, reversal of cholinergic poisoning - req tertiary, hyperhidrosis dry mouth, mydriasis, tachycardia, flushed skin, delirium - "dry as a bone, blind as a bat, red as a beet, mad as a hatter"; can be tx w/ physostigmine or symptom management; contraindications - glaucome (esp closed angle), prostatic hyperplasia, may increase gastric ulcer sx |
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scopolamine
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anticholinergic - muscarinic antagonist
tertiary amine eye or CNS effects |
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homatropine
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anticholinergic - muscarinic antagonist
tertiary amine eye or CNS effects |
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pirenzepine
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anticholinergic - muscarinic antagonist
tertiary amine, M1 selective eye or CNS effects |
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tropicamide
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anticholinergic - muscarinic antagonist
tertiary amine eye or CNS effects |
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tolterodine
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anticholinergic - muscarinic antagonist
tertiary amine (M3 - bladder) treats urinary urgency/frequency/incontinence |
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atropine methyl nitrate
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anticholinergic - muscarinic antagonist
quaternary amines peripheral effects |
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methscopolamine
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anticholinergic - muscarinic antagonist
quaternary amines peripheral effects |
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ipratropium
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anticholinergic - muscarinic antagonist
quaternary amines peripheral effects |
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propantheline
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anticholinergic - muscarinic antagonist
quaternary amines peripheral effects |
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glycopyrrolate
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anticholinergic - muscarinic antagonist
quaternary amines peripheral effects |
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hexamethonium
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anticholinergic - ganglionic blocking
eye - cycloplegia, mod dilation of pupil, CV - reduced arteriolar/venomotor tone, reduced BP, orthostatic hypotension, mod tachycardia, GI - reduced secretion/motility --> constipation, GU - hesitancy or urinary retention (esp w/ prostatic hyperplasia), impaired sexual fxn, blocks thermoreg sweating, responses to autonomic drugs altered - effector cell recpetors are not blocked so end-organ effects are present, but homeostatic reflexes are absent |
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trimethaphan
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anticholinergic - ganglionic blocking
lacks CNS effects |
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mecamylamine
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anticholinergic - ganglionic blocking
readily enters CNS sedation, tremor, choreiform movements, mental aberrations |
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pralidoxime (2-PAM)
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anticholinergic - cholinesterase regenerator
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