Cholinomimetics

Question 1

Bethanechol

Answer 1

Class: Carbamic Ester
MOA: Direct muscarinic cholinomimetic
Uses: Post-operative and neurogenic ileus; urinary retention
SE: SLUDGE

Question 2

Pilocarpine (Salagen)

Answer 2

Class: Ester alkaloid
MOA: Direct muscarinic cholinomimetic
Uses: Glaucoma (ACh activates papillary sphincter and ciliary muscles of eye)
SE: SLUDGE

Question 3

Cevimiline

Answer 3

Class: Ester alkaloid
MOA: Direct muscarinic cholinomimetic
Uses: Dry mouth (in, e.g., Sjogren’s, post-radiation therapy; via increased salivation)
SE: SLUDGE

Question 4

Nicotine

Answer 4

Class: Ester alkaloid
MOA: Direct nicotinic cholinomimetic
Uses: Smoking cessation (reduces cravings)

Question 5

Neostigmine (Prostigmin)

Answer 5

Class: Carbamate
MOA: Indirect AChE inhibitor (short acting)
Uses: Post-operative and neurogenic ileus; urinary retention; myasthenia gravis; reversal of neuromuscular blockade
SE: SLUDGE + general increase in cholinergic neurotransmission; paralysis

Question 6

Physostigmine (Eserine)

Answer 6

Class: Carbamate
MOA: Indirect AChE inhibitor (short acting)
Uses: Glaucoma (ACh activates papillary sphincter and ciliary muscles of eye)
SE: SLUDGE + general increase in cholinergic neurotransmission; paralysis

Question 7

Donepezil (Aricept)

Answer 7

Class: Non-ester
MOA: Indirect AChE inhibitor
Uses: Alzheimer’s (amplifies endogenous ACh in brain)
SE: SLUDGE + general increase in cholinergic neurotransmission; paralysis

Question 8

Edrophonium (Enlon)

Answer 8

Class: Non-ester
MOA: Indirect AChE inhibitor (v. short acting)
Uses: Myasthenia gravis (differentiating deficiency versus ACh crisis); ileus
SE: SLUDGE + general increase in cholinergic neurotransmission; paralysis

Question 9

Echothiophate (Phospholine)

Answer 9

Class: Organophosphate
MOA: Indirect AChE inhibitor (long acting)
Uses: Glaucoma (ACh activates papillary sphincter and ciliary muscles of eye)
SE: SLUDGE + general increase in cholinergic neurotransmission; paralysis

Question 10

Pralidoxime (Protopam)

Answer 10

Class: Strong nucleophile
MOA: Regenerates phosphorylated AChE
Uses: Poisoning by nerve gas, insecticide

Question 11

Soman

Answer 11

Class: Organophosphate
MOA: Very potent indirect AChE inhibitor
Uses: Volatile nerve gas
SE: SLUDGE + general increase in cholinergic neurotransmission; paralysis; Death
Misc: Treat with pralidoxime and atropine before aging