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cholinoceptor drugs
pharmacology of cholinoceptor drugs
| Question | Answer |
|---|---|
| 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 |