Muscarinic Agonists and Antagonists Flashcards
What G protein receptor is used for M1, M2, and M3?
M1 and M3 - Gq
M2 - Gi
What is the postreceptor mechanism of Gq?
Phospholipase C, IP3, DAG mediated cascade, causes intracellular release of calcium
= muscle contraction
What is the postreceptor mechanism of Gi?
Blocks adenylylcyclase, causing inhibition of cAMP production and activation of K+ channels
= prevention of muscle relaxation
What drugs are muscarinic agonists?
Carbamylcholine (carbachol)
Acetyl-beta-methylcholine (methacholine)
Bethanechol
Pilocarpine
Which muscarinic agonist is not resistant to hydrolysis by AChE?
Acetyl-beta-methylcholine (methacholine)
Slowly hydrolyzed by AChE
Which muscarinic agonists are selective for specific muscarinic receptors?
None! No selective agonists
Which muscarinic agonist is more selective for nicotinic receptors than muscarinic?
Carbamylcholine (carbachol)
Which muscarinic agonist has best potency at M2 receptors (cardiac)?
Acetyl-beta-methylcholine (methacholine)
Which muscarinic agonist has no selectivity for nicotinic receptors?
Bethanechol
Which muscarinic agonist can penetrate the BBB and membranes?
Pilocarpine
What are symptoms of parasympathetic overstimulation?
DUMBBELSS Diarrhea Urination Miosis Bronchoconstriction Bradycardia Emesis Lacrimation Salivation Sweating
What are the clinical uses of carbamylcholine (carbachol)?
Glaucoma (constriction of sphincter and drainage of fluid)
What are the clinical uses of acetyl-beta-methylcholine (methacholine)?
When inhaled, causes bronchoconstriction (challenge test for asthma diagnosis)
What are the clinical uses of bethanechol?
GI disorders: postoperative ileus, congenital megacolon, GERD
Urinary retention
What are the clinical uses of pilocarpine?
Glaucoma (constriction of sphincter and drainage of fluid)
Xerostomia (dry mouth)