Cholinergic Agonists & Antagonists

Question 1

Which type of cholinergic agonists bind & activate M or N receptors?

Answer 1

Direct-acting agonists

Question 2

What are some affects of direct-acting cholinergic agonists?

Answer 2

NO-mediated vasodilation of endothelium (M3)

Decrease in cardiac rate and conduction (M2)

Question 3

Name the three esters of choline

Answer 3

Acetylcholine
Bethanechol
Methacholine

Question 4

Which ester of choline is rapidly hydrolyzed, is an agonist of M and N receptors, and is used to get miosis of the eye lens?

Answer 4

Acetylcholine

Question 5

Which ester of choline is more resistant to hydrolysis, is an agonist for M receptors, and is used to stimulate urination & contraction of the bladder?

Answer 5

Bethanechol

Question 6

Which ester of choline is more resistant to hydrolysis, is an M agonist, and is used to diagnose hyperreactivity of bronchial airways?

Answer 6

Methacholine

Question 7

Name the two alkaloids

Answer 7

Pilocarpine

Nicotine

Question 8

Which alkaloid is a partial M agonist, a tertiary amine, and is used to treat dry mouth and help relieve symptoms of glaucoma patients?
Also CF diagnostic measure to stimulate sweat glands for collection.

Answer 8

Pilocarpine

Question 9

Which alkaloid is an agonist of N receptors, a tertiary amine, and depolarizes ANS ganglia for initial stimulation resulting in paralysis?

Answer 9

Nicotine

Question 10

Which type of cholinergic agonists inhibit acetylcholinesterase leading to an increase in endogenous acetylcholine?

Answer 10

Indirect-acting agonists

Question 11

Name the 3 types of indirect-acting cholinergic agonists?

Answer 11

Edrophonium
Carbamates
Organophosphates

Question 12

Which indirect-acting agonist binds reversibly to the active site, is short-lived, is a quaternary ammonium, and is used to DIAGNOSE myasthenia gravis?

Answer 12

Edrophonium

Question 13

Which carbamate is a tertiary amine and is used on anticholinergic drug OD’s?

Answer 13

Physostigmine

Question 14

Which carbamate is a quaternary amine, stimulates urination, and is used to TREAT myasthenia gravis?

Answer 14

Neostigmine

Question 15

Which carbamate is a quaternary amine, and TREATS myasthenia gravis?

Answer 15

Pyridostigmine

Question 16

Which organophosphate is an insecticide?

Answer 16

Malathion

Question 17

Which organophosphate is a highly toxic nerve agent?

Answer 17

Sarin

Question 18

Which drug can be an antidote to our indirect-acting agonists?

Answer 18

Pralidoxime (stimulate acetylcholinesterase)

Question 19

Which M receptor antagonist is reversibly competitive, a tertiary amine, an antidote for cholinergic agonists, and is also used to block respiratory secretions prior to surgery?

Answer 19

Atropine

Question 20

Which M receptor antagonist prevents motion sickness?

Answer 20

Scopolamine

Acts on M1

Question 21

Which M receptor antagonist treats COPD and asthma?

Answer 21

Ipratropium

Question 22

What M receptor antagonist produces myadriasis?

Answer 22

Tropicamide

Question 23

Which N receptor antagonist was used in hypertensive cases?

Answer 23

Hexamethonium

Question 24

Which Nm competitive antagonist acts as a non-depolarizing blocker to relax skeletal muscle?

Answer 24

Tubocurarine

Question 25

Which Nm agonist acts as a depolarizing blocker and desensitizes the receptor by stimulating it?
Commonly used in intubations and ECTs

Answer 25

Succinylcholine

Question 26

What drug acts presynaptically to inhibit acetylcholine release?

Answer 26

Botox