Cholinomimetics

Question 1

Bethanecol

Answer 1

Direct Acting Carbamic Ester. Direct acting muscarinic cholinomimetic. Post-op and neurogenic ileus; urinary retention (bowel and bladder smooth muscle Ach-innervated. SLUDGE.

Question 2

Muscarine

Answer 2

DIrect Acting Carbamic Ester. Direct acting muscarinic cholinomimetic. SLUDGE

Question 3

Pilocarpine

Answer 3

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

Question 4

Cevimeline

Answer 4

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

Question 5

Nicotine

Answer 5

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

Question 6

Neostigmine

Answer 6

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 .5-2 hrs

Question 7

Physostigmine

Answer 7

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 .5-2 hrs

Question 8

Donepezil

Answer 8

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

Question 9

Edrophonium

Answer 9

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

Question 10

Echothiophate

Answer 10

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 hrs

Question 11

Pralidoxime

Answer 11

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