Cholinergic Receptor Agonists

Question 1

Varenicline tartrate (Chantix)

Answer 1

-alpha4beta2 Nicotinic receptor
partial agonist

-Activates nicotinic receptor much less than nicotine;
Blocks nicotine from binding

-well tolerated

-Side effects:
• GI related (nausea,
constipation, gas, vomiting)
• Altered dreams

Question 2

Acetylcholine Clinical Use (M, N)

Answer 2

Intraocular use for miosis during surgery

Cholinesterase activity

Question 3

Carbachol Clinical Use (M, N)

Answer 3

Intraocular use for miosis during surgery, glaucoma

Question 4

Pilocarpine Clinical Use (M)

Answer 4

Glaucoma

Question 5

Bethanechol Clinical Use (M)

Answer 5

Urinary retention, post-operative ileus

Question 6

Varenicline Clinical Use (N)

Answer 6

Smoking Cessation

Question 7

Direct Acting Cholinergic Receptor Agonists: Esters

Answer 7

• Acetylcholine
• Carbachol (Isoptocarbachol)
• Methacholine (Provocholine)
• Bethanechol (Urecholine)

Question 8

Direct Acting Cholinergic Receptor Agonists: Alkaloids and synthetic analogs

Answer 8

• muscarine
• nicotene (nicorette)
• pilocarpine (isoptocarpine)

Question 9

Nicotene

Answer 9

• dibasic (2 basic nitrogens)

- nicotinic receptors less stereoselective