Cholinergic Antagonists/Anticholinergics

Question 1

What is Atropines mechanism of action?

Answer 1

-antimuscarinic agent competitive at M1,M2, and M3 receptors
-reversible tertiary amine
-prevents the binding of Acetylcholine

Question 2

What is the difference in uses for tertiary vs. quaternary amines?

Answer 2

-Tertiary amines are used in ocular and CNS applications
-Quaternary Amines are used in GI tract and peripheral applications, COPD

Question 3

What tertiary amine has a hydroxy ring?

Answer 3

-Scopolamine which has more lipophilicity and better CNS activity/penetration
-long lasting

Question 4

What receptor is Tolterodine (Detrol) appear to be selective for?

Answer 4

-M3
-clinically used for overactive bladder

Question 5

What structure does Succinylcholine and Tubocurarine resemble?

Answer 5

Acetylcholine

Question 6

Name the Neuromuscular blocking agents?

Answer 6

Succinylcholine (depolarizing)
Tubocurarine (non-depolarizing blockade)
-both clinically useful for intubation

Question 7

What is Hexamethonium mechanism of action?

Answer 7

-antagonist at nicotinic receptors in autonomic ganglia; blocks all SNS and PSNS activity
-long list of side effects so not clinically used