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Cholinergics

mhm

QuestionAnswer
Parasympathomimetic Fx Miosis, ciliary contraction, aq humor outflow, lacrimation, salivation + gastric secretion, gastric emptying + urination, EDRF/NO production (orphan M3, low dose), dec chrono/ino/dromotropy (M2, high doses), bronchoconstriction (M3), pulmonary secretions
Glaucoma Inc IOP > 30 mmHg due to resistance to outflow of aq humor. Primary - due to alteration in the eye; open angle - slow onset due to aging; angle closure/narrow angle - rapid onset due to obstruction (tx surgery)
Myasthenia gravis Auto-ABs attack Nm receptors: ptosis (droopy eyelids), diplopia (eye mvmt, vision), difficulty swallowing + chewing, weakness, dyspnea
Methacholine Methyl at β-carbon provides steric hindrance to AChE metab and imparts muscarinic selectivity
Carbachol Carbamylated ACh, slower rate of hydrolysis. Non-selective cholinergic agonist. Glaucoma: inc aq humor drainage thru trabecular meshwork into Schlemm's canal to bloodstream. SEs: short-term blurred far/dark vision
Bethanechol Carbamylated methacholine, slower rate of hydrolysis. Muscarinic agonist. Post-surgical GI/bladder atony: short-term tx promotes GI + bladder contraction. Contraindicated: PUD (XS secretions), urinary tract obstruction, systemic SE concern
Muscarine Naturally-occurring alkaloid. Muscarinic agonist
Pilocarpine Naturally-occurring alkaloid. Muscarinic agonist with CNS activity. Glaucoma: inc aq humor drainage thru trabecular meshwork into Schlemm's canal to bloodstream. SEs: short-term blurred far/dark vision
Edrophonium Competitive, reversible AChEI - drug hydrolyzed to form carbamylated enzyme, less readily hydrolyzed. Reversed by inc ACh. Used to diagnose myasthenia gravis: v short-acting, expected to improve skeletal muscle mvmt. SEs: systemic
Donepezil Competitive, reversible AChEI - drug hydrolyzed to form carbamylated enzyme, less readily regenerated. Reversed by inc ACh. CNS activity
Pyridostigmine Non-competitive, reversible AChEI - drug hydrolyzed to form carbamylated enzyme, less readily regenerated. Not displaced by ACh. Myasthenia gravis: slow onset, longer duration
Neostigmine Non-competitive, reversible AChEI - drug hydrolyzed to form carbamylated enzyme, less readily regenerated. Not displaced by ACh. Myasthenia gravis: rapid onset
Physostigmine Non-comp, reversible AChEI - drug hydrolyzed to form carbamylated enzyme, less readily regenerated. Not displaced by ACh. Glaucoma: inc aq humor drainage thru trabecular meshwork into Schlemm's canal to bloodstream. SEs: short-term blurred far/dark vision
Demarcarium Non-competitive, reversible AChEI - drug hydrolyzed to form carbamylated enzyme, less readily regenerated. Not displaced by ACh
Ambenonium Non-competitive, reversible AChEI - drug hydrolyzed to form carbamylated enzyme, less readily regenerated. Not displaced by ACh.
Echothiophate Irreversible AChEI - drug hydrolyzed to form phosphorylated enzyme, v resistant to hydrolysis, esp after aging. Glaucoma: inc aq humor drainage thru trabecular meshwork into Schlemm's canal to bloodstream. SEs: short-term blurred far/dark vision
Parathion + Malathion Insecticides. Irreversible AChEI - drug hydrolyzed to form phosphorylated enzyme, v resistant to hydrolysis, esp after aging
Sarin, Soman, Tabun Nerve gases. Irreversible AChEI - drug hydrolyzed to form phosphorylated enzyme, v resistant to hydrolysis, esp after aging
Pralidoxime (2-PAM) attaches to Ser site + nucleophilic attack dephosphorylates enzyme to regenerate. AChEI antidote
Created by: 1148100386
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