Cholinergic

Question 1

Direct agonist of cholinergic receptor

Answer 1

Binds to and Activates the receptor

Question 2

Indirect agonist of cholinergic receptor

Answer 2

Stimulates acetylcholine release or inhibits acetylcholinesterase (AChE)

Question 3

ACh (M,N)

Answer 3

Short-lived, agonist, degraded by AChE, intraocular use for miosis

Question 4

Methacholine (M)

Answer 4

Methyl on b carbon helps avoid AChE. Provocative test for hyperreactive airways

Question 5

Carbachol (M,N)

Answer 5

Carbamate functional group selective for M. Intraocular use for miosis during surgery and treatment of glaucoma

Question 6

Bethanechol (M)

Answer 6

Beta substitution makes it selective for muscarinic. Urinary retention, post-op ileus

Question 7

Pilocarpine (M)

Answer 7

Treats glaucoma (no charge so it can cross the BBB). Preferred stereochem is + for cholinergic drugs. Also used for the treatment of xerostomia following radiation of head and neck or treatment of Sjogren’s syndrom

Question 8

Side effects of Cholinergic drugs

Answer 8

Diarrhea, Urination, Miosis, Bradycardia, Bronchoconstriction, Emesis, Lacrimation, Salvation+ Sweating

Question 9

Varenicline (Chantix) MOA/Clinical use

Answer 9

a4b2 neuronal nicotinic receptor partial agonist which blocks nicotine binding and mimics nicotine and releases dopamine. Smoking cessation

Question 10

Bupropion (Wellbutrin) MOA/Clinical use

Answer 10

Weakly inhibits NET and DAT which increase NE and DA in the synaptic cleft. Depression, smoking cessation

Question 11

Glaucoma

Answer 11

increased intraocular pressure (decreased outflow or increased secretion)

Question 12

M3 agonist for the treatment of Glaucoma

Answer 12

Contraction facilitates outflow which decreases intraocular pressure