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Definition
Mechanism: choline ester with quaternary ammonium group (poorly absorbed, low penetration of CNS); muscarinic receptor agonist; less susceptible to hydrolysis relative to acetylcholine Treatment: diagnose asthma Side effects:nausea, vomiting, diarrhea, salivation, sweating, cutaneous vasodilation bronchial constriction. Atropine for overdose |
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Definition
Mechanism: choline ester with quaternary ammonium group (poorly absorbed, low penetration of CNS); muscarinic receptor agonist; parasympathetic effects (contraction of ciliary muscle which lowers intraocular pressure) Treatment: used topically as miotic agent for glaucoma Side effects:nausea, vomiting, diarrhea, salivation, sweating, cutaneous vasodilation bronchial constriction Antidote: atropine |
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Definition
Mechanism: choline ester with quaternary ammonium group (poorly absorbed, low penetration of CNS); muscarinic receptor (M3) agonist, beta-methyl group gives selectivity for muscarinic group, parasympathetic effects Treatment: promotes GI and urinary tract motility due to non-obstructive causes Side effects: nausea, vomiting, diarrhea, salivation, sweating, cutaneous vasodilation bronchial constriction |
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Definition
Mechanism: cholinomimetic alkaloid (acts like acetylcholine); quaternary amine; derived from mushroom Treatment: parasympathetic action Side effects: ingestion of mushroom will induce salivation, sweating, and lacrimation within 15-30 minutes and systemic action within 2 hours Antidote: atropine |
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Term
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Definition
Mechanism: cholinomimetic alkaloid, tertiary amine (well-absorbed, penetrates CNS); excreted by kidney; not an ester so not hydrolyzed by acetylcholinesterase Treatment: sialogogue (increases salivation), miotic agent; Sjogren's syndrome and after radiation therapy Side effects: parasympathetic action |
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Definition
"Dry as a bone, blind as a bat, red as a beet, mad as a hatter" (inhibition of secretions, tachycardia, mydriasis and cycloplegia, inhibition of GI motility, relaxation of bronchial, biliary and urinary tract smooth muscles, excitatory effects on CNS) Mechanism: muscarinic antagonist; tertiary amine Treatment: sinus bradycardia Side effects: atropine poisoning in children |
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Definition
Mechanism: muscarinic antagonist; targets M1 receptor (sympathetic); significant CNS effects (sedation), transdermal route Treatment: motion sickness and nausea from chemotherapy; used to facilitate endoscopy by relaxing GI SM Side effects: impaired speech; thirst, blurred vision, difficulty urinating, tachycardia, hallucinations, delirium (date rape drug) |
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Definition
Mechanism: muscarinic receptor antagonist; tertiary amine Treatment: Parkinsons, acute dystonia caused by antipsychotic meds Side effects:increased thirst, impaired speech, etc. |
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Definition
Mechanism: quaternary amine Treatment: decrease oral secretions, decrease GI spasms, treats peptic ulcers, prevents bradycardia during surgical procedures Side effects: same as all muscarinic antagonists |
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Term
Tolterodine (oxybutynin, darifenacin) |
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Definition
Mechanisms: muscarinic antagonist, M3 selectivity, tertiary amine Treatment: T+D for urinary incontinence adults, O relieves bladder spasm after urologic surgery Side effect: xerostomia (cotton mouth; less with D) |
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Definition
Mechanism: synthetic analog of atropine, quaternary ammonium, acts locally Treatment: inhalation for asthma, COPD (although recent report suggests major adverse cardiovascular events in patients treated for COPD) Side effects: Cardiovascular events (MI, stroke) |
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Definition
Mechanism: muscarinic antagonist, tertiary amine Treatment: dilates pupil for ophtho exam (mydriatic) Side effect:cycloplegia (loss of accomodation) |
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Term
Nicotine, Succinylcholine |
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Definition
Mechanism: nicotinic receptor agonist, but blocks channel in open position (depolarizing blockade); readily absorbed in all tissue. Succinylcholine works through polarizing blockade (requires sufficiently high concentration) Treatment: nicotine available in transdermal patch preparations for smoking cessation programs, succinylcholine is a skeletal muscle relaxant Side effects: acute fatal dose (40 mg) causes vomiting, convulsions, coma and respiratory paralysis, fasciculations and then paralysis, hypertension, cardiac arrhythmic; chronic effects: cigarette addiction Overdose treated with atropine, convulsions treated with diazepam, neuromuscular blockade requires mechanical respiration; metabolized and excreted rapidly |
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Term
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Definition
Mechanism: Nicotinic receptor antagonist; ganglion blocking drugs Treatment: hypertension, and dissecting aortic aneurysm Side effects: cycloplegia, orthostatic hypotension, constipation, urinary retention, sexual dysfunction |
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Term
Tubocurarine and Pancuronium |
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Definition
Mechanism: nicotinic receptor antagonist, nondepolarizing neuromuscular-blocking drug (competitively blocks channel in closed state); skeletal muscle relaxant Treatment: facilitate surgery (intra-abdominal and thoracic procedures) Side effects: -- |
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Definition
Mechanism: quaternary alcohol, reversible inhibitor of AChE, short duration of action Treatment: diagnostic test in patients exhibiting muscle weakness (myasthenia gravis or Eaton-Lambert syndrome); assess adequacy of treatment for MG Side effects: DUMBBELSS (diarrhea, urination, miosis, bronchoconstriction, bradycardia, excitation of skeletal and CNS, lacrimation, salivation, sweating) |
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Definition
Mechanism: quaternary amine, cholinesterase inhibitor, duration of action determined by stability of enzyme-inhibitor complex: 0.5-2 hours Treatment: myasthenia gravis, ileus, reversal of neuromuscular blockade Side effects: DUMBBELSS (diarrhea, urination, miosis, bronchoconstriction, bradycardia, excitation of skeletal and CNS, lacrimation, salivation, sweating) |
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Definition
Mechanism: tertiary amine, duration of action (0.5 to 2 hours) Treatment: glaucoma, reversal of muscarinic blockade; useful in cases of anticholinergic drug poisoning (atropine intoxication or overdosage of tricyclic antidepressants) Side effects: more toxic than neostigmine, DUMBBELSS (diarrhea, urination, miosis, bronchoconstriction, bradycardia, excitation of skeletal and CNS, lacrimation, salivation, sweating) |
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Definition
Mechanism: quaternary amine, DOA: 3 to 6 hours Treatment: MG Side effects: DUMBBELSS (diarrhea, urination, miosis, bronchoconstriction, bradycardia, excitation of skeletal and CNS, lacrimation, salivation, sweating) |
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Term
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Definition
Mechanism: organophosphate that is highly polar (not well-absorbed), stable in aqueous solution, DOA: 100 hours Treatment: glaucoma Side effects: potential chemical warfare nerve agents, DUMBBELSS Antidote: with organophosphate poisoning, administer pralidoxime IV |
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Term
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Definition
Mechanism: cholinesterase regenerator compound; strong nucleophile (charged, does not enter CNS) that can reverse the phosphorous-enzyme bond and regenerate active serine Treatment: organophosphate poisoning |
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Term
Tacrine (Donepezil, rivastigmine, galantamine) |
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Definition
Mechanism: anticholinesterase Treatment: Alzheimer's disease Side effects: hepatotoxicity |
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