ACh activators and AChE inhibitors

Question 1

Bethanechol

Answer 1

Direct acting muscarinic, increases IP3 and DAG; bladder and bowel atony; Oral, IM activity; poor lipid solubility (does not enter CNS); 0.3-2 hours

Question 2

Pilocarpine

Answer 2

Direct acting muscarinic, increases IP3 and DAG; Sjogrens syndrome (increases salivation), cystic fibrosis sweat test, used in glaucoma (causes miosis, cyclospasm); oral, IM; good lipid solubility, topical activity in eye

Question 3

Methacholine

Answer 3

induces bronchospasm

Question 4

Muscarine

Answer 4

Direct acting muscarinic, increases IP3 and DAG; low lipid solubility but readily absorbed from gut

Question 5

Nicotine

Answer 5

Direct acting nicotinic, activates all nicotinic receptors, opens sodium potassium channels in ganglia and neuuromuscual end plates; smokin cesstion; high lipid solubility; absorbed by all routes; 4-6 hours

Question 6

Carbachol

Answer 6

activates both muscarinic and nicotinic; typical cholinergic response

Question 7

Varenicline

Answer 7

partial agonist of N receptors; smoking cessation; high lipid solubility; oral activity; 12 hours

Question 8

Edrophonium

Answer 8

inhibitor of choinesterase (amplifier of endogenousely released Ach); reversal of Nm block by nondepolarizing drugs; diagnosis of myasthenia gravis; highly polar; IV; 5-10 minutes

Question 9

Neostigmine

Answer 9

inhibitor of choinesterase (amplifier of endogenousely released Ach); reversal of Nm block by nondepolarizing drugs; treatment of myasthenia gravis; moderately polar; orally active; 2-4 hours

Question 10

Physostigmine

Answer 10

inhibitor of choinesterase (amplifier of endogenousely released Ach); reversal of atropine poisoning; occasionally used in acute glaucoma; lipid soluble; can be used topically in the eye; 2-4 hours

Question 11

Pyridostigmine

Answer 11

inhibitor of choinesterase (amplifier of endogenousely released Ach); reversal of Nm block by nondepolarizing drugs; treatment of myasthenia gravis; moderately polar; orally active; 4-8 hours

Question 12

Parathion

Answer 12

inhibitor of choinesterase (amplifier of endogenousely released Ach); insecticide only; highly lipid soluble; days to weeks

Question 13

Malathion

Answer 13

inhibitor of choinesterase (amplifier of endogenousely released Ach); insecticide only; highly lipid soluble but metabolized to inactive products in mammals and birds; days

Question 14

Sarin

Answer 14

inhibitor of choinesterase (amplifier of endogenousely released Ach); nerve gas and terrorist threat; highly lipid soluble; very rapid action

Question 15

Ecothiophate

Answer 15

inhibitor of choinesterase (amplifier of endogenousely released Ach); Glaucoma