Cholinergic Pharmacology

Question 1

Used for the treatment of bladder and bowel atony (post-surgery or spinal cord injury)

Answer 1

Betanechol

M3 receptor agonist

Question 2

Direct-acting muscarinic agonists

Answer 2

Bethanechol
Pilocarpine
Muscarine

Question 2

MOA of Bethanechol

Answer 2

Activates muscarinic receptors; increases IP3 and DAG

Question 3

Used for Sjogren’s syndrome (increases salivation); was used in glaucoma (causes ciliary muscle contraction, opening or trabecular meshwork, increased outflow)

Answer 3

Pilocarpine

M3 receptor agonist

Question 4

Triad of Sjogren Syndrome

Answer 4

Xerostomia
Xerophthalmia
Rheumatoid arthritis

Question 6

Alkaloid found in mushrooms; causes mushroom poisoning of fast-onset type

Answer 6

Muscarine

Question 7

Used for smoking cessation

Answer 7

Nicotine

Varenicline

Question 8

Indirect-acting cholinomimetic (alcohol)

Answer 8

Edrophonium

Shortest-acting cholinesterase inhibitor

Question 9

Direct-acting nicotinic agonists

Answer 9

Nicotine
Varenicline
Succinylcholine

Question 9

MOA of edrophonium

Answer 9

Inhibitor of cholinesterase; amplifier of endogenously released ACh

Question 9

Indications of edrophonium

Answer 9

Reversal of Nm block by nondepolarizing drugs; diagnosis of myasthenia gravis (Tensilon test)

Question 10

Indirect-acting cholinomimetic (organophosphates)

Answer 10

Insecticides:

Parathion
Malathion
Sarin
Tabun

Question 11

Indirect acting cholinomimetic (carbamates)

Answer 11

Neostigmime
Pyridostigmine
Physostigmine

Question 11

Indirect-acting cholinomimetic (for Alzheimer’s)

Answer 11

Rivastigmine
Galantamine
Donepezil
Tacrine (obsolete)

Question 12

Indirect-acting cholinomimetics

Answer 12

Edrophonium
Neostigmine
Pyridostigmine
Physostigmine
Rivastigmine
Galantamine
Donepezil
Tacrine

Question 12

Used for the treatment of myasthenia gravis

Answer 12

Neostigmine
(Indirect-acting cholinomimetic)

Others:
Pyridostigmine
Physostigmine

Question 13

Indirect-acting cholinomimetic used for the treatment of glaucoma

Answer 13

Physostigmine

Indirect-acting cholinomimetic

Question 13

Used for the reversal of severe atropine poisoning (IV)

Answer 13

Physostigmine

Question 14

How is Tensilon test performed?

Answer 14

Edrophonium 2mg is injected via IV after baseline muscle strength has been measured. If no rxn occurs after 45s, an additional 8mg may be injected. If the patient has MG, an improvement that lasts about 5min can usually be observed.

Question 15

Indirect-acting cholinomimetic used for the treatment of Alzheimer’s disease

Answer 15

Rivastigmine
(Indirect-acting cholinomimetic)

Others:
Galantamine
Donepezil
Tacrine (obsolete)

Question 16

Antidote for organophosphate poisoning (1st choice)

Answer 16

Atropine

Nonselective muscarinic antagonist

Question 17

Signs and symptoms of organophosphate poisoning

Answer 17

DUMBBELSS
Diarrhea
Urination
Miosis
Bronchospasm
Bradycardia
Excitation
Lacrimation
Sweating
Salivation

Question 18

Toxicities of atropine

Answer 18

All parasympatholytic effects plus sedation, delirium, hyperthermia, flushing

Question 19

MOA of Indirect-acting cholinomimetics

Answer 19

Inhibits acetylcholinesterase; amplifies endogenously released Ach

Question 20

Antidote for organophosphate poisoning and nerve gas poisoning

Answer 20

Pralidoxime | Cholinesterase regenerator

Question 21

Muscarinic antagonist used for asthma and COPD

Answer 21

Ipatropium | Tiotropium

Question 22

Muscarinic antagonist used for Parkinson's disease

Answer 22

Benztropine Biperiden Trihexyphenidyl

Question 23

Preferred bronchodilator in patients with comorbid COPD and heart disease

Answer 23

Ipatropium

Question 24

Muscarinic antagonist used for motion sickness

Answer 24

Scopolamine

Question 25

Contraindications to muscarinic blockers

Answer 25

Infants Hyperthermia due to decreased sweating Acute angle-closure glaucoma BPH

Question 26

Nondepolarizing neuromuscular blockers

Answer 26

Tubocurarine Pancuronium Atracurium Vecuronium

Question 27

Depolarizing neuromuscular blockers

Answer 27

Succinylcholine

Question 28

Chemical antagonist of organophosphates; used for organophosphate poisoning

Answer 28

Pralidoxime

Question 29

MOA of pralidoxime

Answer 29

Cholinesterase regenerator: | Binds phosphorus of organophosphate; breaks organophosphate bond with cholinesterase

Question 30

How is pralidoxime given?

Answer 30

Must be administered before 6-8 hours of organophosphate bond with cholinesterase occurs

Question 31

M1-selective antimuscarinic drugs

Answer 31

Pirenzepine | Telenzepine

Question 32

Indications of M1-selective antimuscarinic drugs (Pirenzepine, Telenzepine)

Answer 32

Peptic disease

Question 33

Antinicotinic ganglion blocker; blocks all autonomic effects

Answer 33

Hexamethonium

Question 35

M3 selective antimuscarinics

Answer 35

Darifenacin Fesoterodine Solifenacin Tolterodine

Question 36

The most dangerous effect of the antimuscarinic drugs in children and is potentially lethal in infants

Answer 36

Atropine fever

Question 37

A drug which causes vasodilation that can be blocked by atropine

Answer 37

Bethanechol

Question 38

Indications of M3-selective antimuscarinics

Answer 38

Urinary urgency; incontinence