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FIU - Muscarinic receptor blockers & agonists
Muscarinic receptor blockers & agonists
17
Pharmacology
Professional
12/30/2011

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Cards

Term
atropine (D/L-hyoscyamine), acts for how long?
Definition
muscarinic receptor blocker, 2 -3 days; tropicamide and phenylephrine preferred as mydriatics
Term
tropicamide mode of action, effect
Definition
shorter-acting cholinergeic antagonist (knocks out parasympathetic NS), mydriatic
Term
phenylephrine mode of action, effect
Definition
alpha adrenergic agonist/sympathomimetic; directly simulates iris dilator muscle - mydriatic
Term
muscarinic receptor blocker uses, overdose effect?
Definition
mydriasis, resuscitation (reduces PNS, takes break off heart), for secretions and bronchoconstriction (atropine - dries and opens airways), antidote for OP poisoning (use atropine - counters cholinergic SLUDGE: Salivation, lacrimation, urination, diaphoresis/hyperhidrosis, GI motility, emesis ALSO micropsia: see objects as smaller); overdose = Central Anticholinergic Syndrome (dry as a bone etc)
Term
Glycopyrrolate, distribution
Definition
muscarinic blocker w/o penetration of BBB/CNS (much weaker than atropine but no mad as a hatter), IV or oral (only 5% absorption)
Term
-tropium mode of action, use, examples with half life
Definition
Inhalative antimuscarinics (counters PNS brochoconstriction and secretion, for COPD/asthma, ex: Ipratropium and Oxitropium (short) and Tiotropium (long)
Term
Darifenacin mode of action, use, advantage
Definition
Selective M3 blocker (M3 receptor mediates detrusor contractility, also involved in bladder and gastrointestinal smooth muscle contraction, saliva production, iris sphincter function).; for urinary incontinence; advantage: won’t cause thirst
Term
Oxybutinin mode of action, use, advantage
Definition
Selective M3 blocker (but M3=M1), urinary incontinence; advantage: won't cause thirst
Term
Tolterodine mode of action, use, interesting fact
Definition
Non-selective muscarinic receptor blocker (uroselectivity not linked to one receptor sub-type; parotid effect down 8x), urinary incontinence
Term
Diphenhydramine
Definition
Benadryl: 1st generation H1 blocker (sedation), alpha blocker, strong anticholinergic effect (muscarinic blocker)
Term
Orphenadrine
Definition
Methylated diphenhydramine: 1st generation H1 blocker, NMDA receptor antagonist, anticholinergic effect (2/3 of atropine, muscarinic blocker)
Term
Benzatropine, mode of action, effect, use
Definition
Atropine derivative, muscarinic blocker, counters ACh/dopamine imbalance due to reduced dopamine, for Parkinson disease
Term
Biperiden, mode of action, use
Definition
Tertiary amine and muscarinic blocker that reduces ACh, for Parkinson
Term
Trihexyphenidyl, mode of action, use
Definition
Tertiary amine and muscarinic blocker that reduces Ach, antiparkinson
Term
Muscarine
Definition
Muscarinic (metabotropic) receptor agonist with less central effect/BBB crossing than ACh
Term
Pilocarpine mode of action, use
Definition
Non-selective M3 agonist, for chornic open-angle and acute angle-closure glaucoma (increased aqueous outflow)
Term
Cevimeline, mode of action, effect, use
Definition
Selective M3 agonist, increased secretion of saliva and tears; for dry mouth and especially for chronic dry eyes/mouth from Sjogren's syndrome
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