Cholinergic Drugs & Anticholinesterase

Question 1

Effects of stimulating M1 receptor

Answer 1

Increases gastric secretion & motility

Question 2

Effects of stimulating M2 receptor

Hint: inhibitory

Answer 2

1. Myocardial inhibition
2. Inhibits release of neurotransmitters
3. Relaxation of sphincter

Question 3

Effects of stimulating M3 receptors

Answer 3

1. Increases secretion
2. Increases GI motility
3. Release of NO from endothelial cells –> vasodilation
4. Contraction of detrusor muscle & relaxation of sphincter –> urination
5. Contraction of iris sphincter –> miosis (pupillary constriction); contraction of ciliary muscle –> cyclospasm (near vision) –> decreases IOP
6. Bronchoconstriction –> asthma

Question 4

Name 2 muscarinic receptor agonists apart from acetylcholine

Answer 4

1. Methacholine

2. Pilocarpine

Question 5

What is edrophonium and what is its use?

Answer 5

Edrophonium: short- acting reversible anticholinesterase

Use: diagnose MG & differentiate myasthenic & cholinergic crises

Question 6

Why is neostigmine preferred over physostigmine for treatment of MG?

Answer 6

Neostigmine less lipid soluble

Doesn’t cross BBB easily

Produces peripheral effect

Question 7

What is physostigmine used for?

Answer 7

Treat atropine poisoning

Question 8

What is tacrine used for?

Answer 8

Treat Alzheimer’s

Question 9

Bond between organophosphate & acetylcholinesterase unbreakable after ___.

Answer 9

Aging

Question 10

What is used to reactivate AchE before aging?

Answer 10

Pralidoxime

Question 11

Antidote for organophosphate poisoning after damage is done

Answer 11

Atropine

Question 12

Organophosphates are reversible antiAchEs. True/False?

Answer 12

False

Question 13

Name 4 reversible antiAchEs

Answer 13

1. Edrophonium
2. Neostigmine
3. Physostigmine
4. Tacrine