cholinergic agonists (direct acting)
Quiz yourself by thinking what should be in
each of the black spaces below before clicking
on it to display the answer.
Help!
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| ACh | endogenous NT (not a good drug because rapidly metabolized); clinical use = produce complete miosis in eye surgery
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| Methacholine | muscarinic selective, slightly longer duration of action; clinical use = bronchial airway hypersensitivity testing (diagnostic tool)
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| Carbachol | carbamic acid derivative of ACh designed for longer duration of action (resists hydrolysis once bound to AChE); used in the eye to target the desired tissue, but not nicotinic/muscarinic selective; clinical use = produce complete miosis in eye surgery
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| Bethanechol | added methyl to carbachol makes bethanechol; long-acting (resists hydrolysis) and selective for muscarinic receptors; bladder and GI hypotonia
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| Pilocarpine | muscarinic agonist, binds AChE but resists hydrolysis (making it longer acting); used for treatment of open-angle glaucoma; natural product; can also be used clinically for Sjorgen’s syndrome
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| Cevimeline | synthetic pilocarpine-like molecule; approved for Sjorgen’s syndrome
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| Oxotremorine | muscarinic selective; long acting (resists AChE hydrolysis); clinical use = experimental model of Parkinson’s disease tremor
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