Cholinomimetics Flashcards
Bethanechol
Class: Direct acting carbamic acid ester
Mechanism: Direct-acting muscarinic cholinomimetic
Therapeutics: Post-operative and neurogenic ileus; urinary retention (bowel and bladder smooth muscle ACh-innervated)
Side Effects: SLUDGE
Muscarine
Class: Direct acting non-ester alkaloid
Mechanism:Direct-acting muscarinic cholinomimetic
Side Effects: SLUDGE
Pilocarpine (Salagen)
Class: Direct acting non-ester alkaloid
Mechanism: Direct-acting muscarinic cholinomimetic
Therapeutics: Glaucoma (ACh activates papillary sphincter and ciliary muscles of eye)
Side Effects: SLUDGE
Cevimeline (Evoxac)
Class: Direct acting non-ester alkaloid
Mechanism: Direct-acting muscarinic cholinomimetic
Therapeutics: Dry mouth (in, e.g., Sjogren’s, post-radiation therapy; via increased salivation)
Side Effects: SLUDGE
Nicotine (NRT)
Class: Direct acting non-ester alkaloid
Mechanism: Direct-acting nicotinic cholinomimetic
Therapeutics: Smoking cessation (reduces cravings)
Neostigmine (Prostigmin)
Class: Indirect acting carbamate
Mechanism: AChE inhibitor (short acting)
Therapeutics: Post-operative and neurogenic ileus; urinary retention; myasthenia gravis; reversal of neuromuscular blockade
Side Effects: SLUDGE + general increase in cholinergic neurotransmission; paralysis
Physostigmine (Eserine)
Class: Indirect acting carbamate
Mechanism: AChE inhibitor (short acting)
Therapeutics: Glaucoma (ACh activates papillary sphincter and ciliary muscles of eye)
Side Effects: SLUDGE + general increase in cholinergic neurotransmission; paralysis
Donepezil (Aricept)
Class: Indirect acting non-ester
Mechanism: AChE inhibitor
Therapeutics: Alzheimer’s (amplifies endogenous ACh in brain)
Side Effects: SLUDGE + general increase in cholinergic neurotransmission; paralysis
Edrophonium (Enlon)
Class:Indirect acting non-ester
Mechanism:AChE inhibitor (v. short acting)
Therapeutics: Myasthenia gravis (differentiating deficiency versus ACh crisis); ileus
Side Effects: SLUDGE + general increase in cholinergic neurotransmission; paralysis
Echothiophate (Phospholine)
Class: Indirect acting organophosphate
Mechanism: AChE inhibitor (long acting)
Therapeutics: Glaucoma (ACh activates papillary sphincter and ciliary muscles of eye)
Side Effects: SLUDGE + general increase in cholinergic neurotransmission; paralysis
Pralidoxime (Protopam)
Class:Strong nucleophile
Mechanism: Regenerates phosphorylated AChE
Therapeutics: Poisoning by nerve gas, insecticide