L 16-17

Question 1

Non-selective, direct acting cholinergic agonists

Answer 1

Acetylcholine

Methacholine, Carbachol

Question 2

Selective, direct acting cholinergic agonists

Answer 2

Bethanechol, Pilocarpine

selective for Muscarinic

Question 3

Effect of Ach IV infusion

Answer 3

Acts on M3 receptors to cause inc NO–> inc cGMP –> vasodilation

Question 4

Choline Esters

Answer 4

Resist AchE better than Ach

Methacholine, Carbachol, Bethanechol

Question 5

Alkaloids

Answer 5

Like Muscarine

Pilocarpine, Nicotine

Question 6

Drug to increase GI activity

Answer 6

Bethanechol

Question 7

Drug to increase salivation

Answer 7

Pilocarpine

Question 8

Drug to help increase bladder function

Answer 8

Bethanechol

Question 9

Drug to increase lacrimation, salivation, sweat etc.

Answer 9

Pilocarpine

Question 10

Best drug for dry mouth

Answer 10

Pilocarpine can be used, but has side effects from stimulating all M receptors
Cevimeline: better because M3 specific

Question 11

Nicotine overdose

Answer 11

Nicotine goes to the brain quickly and causes CNS problems
Cardiac will first beat faster causing hypertension and arrhythmias before causing hypotension
Nicotinic receptors desensitize quickly and lead to paralysis
Treat with Atropine to block M receptors and decrease PS response

Question 12

Varenicline

Answer 12

Partial N agonist
Used to decrease cravings from nicotine withdrawal
Side effects: flatulence, psychosis. vomiting

Question 13

What are drugs that end in -stigmine or -onium?

Answer 13

Cholinesterase inhibitors

Question 14

Acetylcholine

Answer 14

Non-selective cholinergic agonist

Question 15

Bethanechol

Answer 15

M-selective cholinergic agonist
In choline ester group
Used for GI and Bladder problems

Question 16

Carbachol

Answer 16

Non-selective cholinergic agonist

Choline ester group

Question 17

Pilocarpine

Answer 17

M-selective cholinergic agonist
used in eye, and for glands
Alkaloid

Question 18

Methacholine

Answer 18

Non-selective cholinergic agonist

Choline ester

Question 19

Neostigmine

Answer 19

Cholinesterase inhibitor
Cleaved by AchE, then occupies site
Duration 2-4hr
No CNS
Poor oral absorption
Use: inc bladder function, Myasthenia Gravis, reverse N.M. blockade in surgery

Question 20

Physostigmine

Answer 20

Cholinesterase inhibitor
Crosses CNS–>side effects
Only good for Atropine overdose

Question 21

Pyridostigmine

Answer 21

Cholinesterase inhibitor

Longer duration 4-6hr

Question 22

Edrophonium

Answer 22

Cholinesterase inhibitor
Short duration 5-20 min
Injection only, no CNS
Use: diagnose Myasthenia Gravis

Question 23

Organophosphates

Answer 23

Cholinesterase inhibitor
Lipid soluble–>storage and slow release
Becomes irreversible with aging

Question 24

Pralidoxime (2-PAM)

Answer 24

Prevents aging of organophosphates
Doesn’t work with carbamates
No CNS
Can itself bind AchE so must only be used in correct amount

Question 25

General Effects of AchE Inhibitors

Answer 25

In general, Parasympathetic effects dominate

Question 26

Donepezil

Answer 26

Cholinesterase inhibitor
Used for Alzheimers because some inc in PS activity causes inc alertness and better memory
Has long duration and low peripheral effects

Question 27

Echothiophate

Answer 27

Organophosphate but not lipid soluble

Used in eye, effects last for days because not well absorbed

Question 28

Symptoms of AchE Toxicity

Answer 28

High Ach=> high Parasymp. effects including SLUDGE
Neuromuscular effects => desensitization and paralysis
Muscarinic agonist has no muscle effect
Treatment: Atropine, 2-PAM
If carbamate: atropine only, no 2-PAM