Cholinomimetic agents

Question 1

Name four Direct agonists

Answer 1

Bethanechol
Carbachol
Methacholine
Pilocarpine

Question 2

Mechanism of Action and clinical application of Bethanecol

Answer 2

MOA: Activates bladder smooth muscle; resistant to AChE. No nicotinic activity.

Use for: Urinary retention.

Question 3

Mechanism of Action and clinical application of Carbachol

Answer 3

MOA: Carbon copy of acetylcholine (but resistant to
AChE).
Constricts pupil and relieves intraocular pressure in open-angle glaucoma.

Question 4

Used as challenge test for Diagnosis of Asthma

Answer 4

Methacoline

Question 5

Methacoline MOA

Answer 5

Stimulates muscarinic receptors in airway when

inhaled.

Question 6

Pilocarpine MOA

Answer 6

Contracts ciliary muscle of eye (open-angle glaucoma),
pupillary sphincter (closed-angle glaucoma);
resistant to AChE,
can cross bloodbrain barrier (tertiary amine)

Question 7

Potent stimulator of sweat, tears, and saliva

Open-angle and closed-angle glaucoma, xerostomia (Sjögren syndrome).

Answer 7

Pilocarpine

Question 8

Name the Indirect agonists (anticholinesterases)

Answer 8

Donepezil, rivastigmine, galantamine
Edrophonium
Neostigmine
Physostigmine
Pyridostigmine

Question 9

1st line for Alzheimer disease

Answer 9

Donepezil,
rivastigmine,
galantamine

Question 10

Historically used to diagnose myasthenia gravis;

replaced by anti-AChR Ab (anti-acetylcholine receptor antibody) test.

Answer 10

Edrophonium

Question 11

Does Neostigmine penetrates the CNS?

Answer 11

No

It is a quaternary amine.

Question 12

Clinical applications of Neostigmine

Answer 12

Postoperative and neurogenic ileus
urinary retention,
myasthenia gravis,
reversal of neuromuscular junction blockade (postoperative).

Question 13

Can Physostigmine cross the BBB?

Answer 13

yes

It can Freely cross the BBB, it is a tertiary amine.

Question 14

Clinical applications of Physostigmine

Answer 14

Antidote for anticholinergic toxicity;

physostigmine “phyxes” atropine overdose.

Question 15

Increases muscle strength and ACh

Answer 15

Pyridostigmine

Question 16

Clinical applications of Pyridostigmine

Answer 16

Myasthenia gravis (long acting); 
does not penetrate CNS (quaternary amine).

Question 17

Which pharms are used to control pyridostigmine side effects?

Answer 17

glycopyrrolate, hyoscyamine, or propantheline

Question 18

Muscarinic effects of Anticholinesterase

Answer 18

DUMBBELSS
Diarrhea, 
Urination, 
Miosis, 
Bronchospasm,
Bradycardia, 
Emesis, 
Lacrimation, 
Sweating,
Salivation

Question 19

Muscarinic effects are reversed by_________

Answer 19

Atropine

Question 20

Nicotinic effects of Anticholinesterase

Answer 20

Neuromuscular blockade (mechanism similar to
succinylcholine).

Question 21

Nicotinic effects Reversed by _____________

Answer 21

Pralidoxime (quaternary amine)

does not readily cross BBB.

Question 22

Anticholinesterase CNS effects

Answer 22

Respiratory depression, lethargy, seizures, coma.