Cholinomimetics (direct acting cholinergics) Flashcards
What is methacholine?
Which receptors is it selective for?
What is its effect on the receptor?
Is it able to cross the BBB?
Selective mAChR agonist
polar; unable to cross BBB
*test for asthma (induce bronchoconstriction)
What is carbachol?
Which receptors is it selective for?
What is its effect on the receptor?
Is it able to cross the BBB?
Non-selective cholinergic agonist
polar; unable to cross BBB
What is bethanechol?
Which receptors is it selective for?
What is its effect on the receptor?
Is it able to cross the BBB?
Selective mAChR agonist
polar; unable to cross BBB
What is cevimeline?
Which receptors is it selective for?
What is its effect on the receptor?
Selective mAChR agonist
*xerostomia
What is pilocarpine?
Which receptors is it selective for?
What is its effect on the receptor?
Selective mAChR agonist
What is varenicline?
Which receptors is it selective for?
What is its effect on the receptor?
Is it able to cross the BBB?
Selective nAChR agonist
nonpolar; able to cross BBB
*chantix - smoking cessation
What cholinergics would be most effective in treating xerostomia in Sjögrens syndrome?
- cevimeline
- pilocarpine
What cholinergics would be most effective in treating non-obstructive GI disorders?
-bethanechol
What cholinergics would be most effective in treating urinary retention?
-bethanechol
What cholinergics would be most effective in treating glaucoma?
- carbachol
- pilocarpine
What cholinergics would be most effective in producing miosis?
- acetylcholine
- carbachol
- pilocarpine
What cholinergics would be most effective in stimulating/testing for asthma?
-methacholine
What cholinergics would be most effective in smoking cessation?
-varenicline
What are the major clinical uses of cholinergics?
- glaucoma
- accomdative esotropia
- non-obsrtuctive GI disorders
- xerostomia in Sjögrens
What are the side effects of muscarinic agonist toxicity?
BM SLUDGE
- miosis
- bronchoconstriction
- salivation
- lacrimation
- urination
- diarrhea
- GI pain
- emesis