Cholinomimetics

Question 1

Class;Mechanism:Therapeutics;SideEffects

Bethanechol (Urecholine)

Answer 1

Direct acting carbamic acid ester Direct-acting muscarinic cholinomimetic Post-operative and neurogenic ileus; urinary retention (bowel and bladder smooth muscle ACh-innervated) SLUDGE — —

Question 1

Class;Mechanism:Therapeutics;SideEffects

Muscarine

Answer 1

Direct acting non-ester alkaloid Direct-acting muscarinic cholinomimetic — SLUDGE — —

Question 2

Class;Mechanism:Therapeutics;SideEffects

Pilocarpine (Salagen)

Answer 2

Direct acting non-ester alkaloid Direct-acting muscarinic cholinomimetic Glaucoma (ACh activates papillary sphincter and ciliary muscles of eye) SLUDGE — —

Question 3

Class;Mechanism:Therapeutics;SideEffects

Cevimeline (Evoxac)

Answer 3

Direct acting non-ester alkaloid Direct-acting muscarinic cholinomimetic Dry mouth (in, e.g., Sjogren’s, post-radiation therapy; via increased salivation) SLUDGE — —

Question 4

Class;Mechanism:Therapeutics;SideEffects

Nicotine (NRT)

Answer 4

Direct acting non-ester alkaloid Direct-acting nicotinic cholinomimetic Smoking cessation (reduces cravings) — — —

Question 5

Class;Mechanism:Therapeutics;SideEffects

Neostigmine (Prostigmin)

Answer 5

Indirect acting carbamate AChE inhibitor (short acting) Post-operative and neurogenic ileus; urinary retention; myasthenia gravis; reversal of neuromuscular blockade SLUDGE + general increase in cholinergic neurotransmission; paralysis — Lasts 0.5-2 hours

Question 6

Class;Mechanism:Therapeutics;SideEffects

Physostigmine (Eserine)

Answer 6

Indirect acting carbamate AChE inhibitor (short acting) Glaucoma (ACh activates papillary sphincter and ciliary muscles of eye) SLUDGE + general increase in cholinergic neurotransmission; paralysis — Lasts 0.5-2 hours

Question 7

Class;Mechanism:Therapeutics;SideEffects

Donepezil (Aricept)

Answer 7

Indirect acting non-ester AChE inhibitor Alzheimer’s (amplifies endogenous ACh in brain) SLUDGE + general increase in cholinergic neurotransmission; paralysis — —

Question 8

Class;Mechanism:Therapeutics;SideEffects

Edrophonium (Enlon)

Answer 8

Indirect acting non-ester AChE inhibitor (v. short acting) Myasthenia gravis (differentiating deficiency versus ACh crisis); ileus SLUDGE + general increase in cholinergic neurotransmission; paralysis — Lasts 5-15 minutes

Question 9

Class;Mechanism:Therapeutics;SideEffects

Echothiophate (Phospholine)

Answer 9

Indirect acting organophosphate AChE inhibitor (long acting) Glaucoma (ACh activates papillary sphincter and ciliary muscles of eye) SLUDGE + general increase in cholinergic neurotransmission; paralysis — Lasts >100 hours

Question 10

Class;Mechanism:Therapeutics;SideEffects

Pralidoxime (Protopam)

Answer 10

Strong nucleophile Regenerates phosphorylated AChE Poisoning by nerve gas, insecticide — — —