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cholinoceptor drugs

pharmacology of cholinoceptor drugs

QuestionAnswer
parasympathetic affects on the eye contract the cirular smooth muscle fibers of the ciliary muscle and iris to produce a spasm of accomodation and an increased outflow of aqueous humor, reducing intraocular pressure: miosis
parasympathetic effects on the cardiovascuar system produce a negative chronotropic effects, decrease conduction velocity through the AV node, produce vasodiliation
parasympathetic effects on GI increase smooth muscle contractions, with increased peristaltic activity and motility, increase salivation and acid secretion
parasympathetic effects on urinary tract increase contraction of the ureter and bladder smooth muscle, increase sphincter relaxation
other effects of parasympathetic drugs bronchoconstriction and increased bronchial secretions, increase secretions of tears and sweat, produce tremor and ataxia
Bethanechol used to stimulate smooth muscle motor activity of the urinary tract to prevent urinary retention; sometimes used to stimulate gastrointestinal smooth muscle for postoperative abdominal distention and gastric atony
bethanechol has low lipid solubility and is poorly absorbed from GI tract, limited distribution to CNS
bethanechol resistant to hydrolysis and has a longer duration of action than ACh (2-3 hours)
pilocarpine used topically for open-angle glaucoma
pilocarpine well absorbed from the Gi tract and enters the CNS
carbachol used for treatment of open angle glaucoma
adverse effects of direct acting cholinoceptor drugs bronchoconstriction, vasodilation, bradycardia and increased acid secretion
contraindications for the use of chlinoceptors peptic ulcers, asthma, cardiac disease
edrophonium has a short duration
Neostigmine, physostigmine, and demecarium these drugs interact with AChE and undergo a two step hydrolysis
neostigmine, physostigmine, and demecarium have direct agonist action at skeletal muscle nicotinic cholinoceptors
neostigmine is poorly absorbed from the GI tract and has negligible distribution into the CNS
physostimine well absorbed after oral administration, and it enters the CNS
echothiophate irreversibly inhibits AChE
ecothiophate poorly absorbed from the GI tract and has negligible distribution into the CNS
adverse effects of indirect acting cholinergic agents muscle weakness, cramps, fasciculations, excessive bronchial secretions, convulsion, coma, and respiratory failure
Created by: swohlers
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