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13 Cards in this Set
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- Back
- 3rd side (hint)
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* Acetyl ester of beta-methylcholine
* Used clinically as a diagnostic agent for bronchospasms (asthma) * Is sufficiently stable in the body (unlike ACh) * Although racemic mixture is used, activity resides in the (S)-enantiomer |
Methacholine Chloride (Provocholine)
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Direct Acting Cholinergic Agonists
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Carbachol Chloride (Miostat)
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* Carbamyl ester of choline (carbamate)
* Possesses both muscarinic & nicotinic activity (local effect) * Rate of hydrolysis is slower & duration of action is longer * used topically for glaucoma & eye surgery |
Direct Acting Cholinergic Agonists
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Bethanechol Chloride (Urecholine)
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* beta-methyl group & carbamate
* mostly muscarinic activity due to beta-methyl group * very slow rate of hydrolysis, DOA: 1-6 hrs * MOA: Stimulates cholinergic receptors in the smooth muscle of the urinary bladder & GIT * Used primarily to treat or prevent post-surgical urinary retention & atony of muscles in GIT |
Direct Acting Cholinergic Agonists
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* HCl salt of alkaloid from Pilocarpus jaborandi or P.microphyllus
* MOA: Directly stimulates cholinergic receptors in the eye causing: - miosis (constriction of pupil) - spasm of accommodation - lowering of intraocular pressure * used primarily as 0.5% solution in treatment of glaucoma * systemic effects: copius sweating, salivation, & gastric secretion |
Pilocarpine HCl (Pilocar)
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Direct Acting Cholinergic Agonists
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Physostigmine (Eserine)
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* alkaloid isolated from Physostigma venenosum
* MOA: inhibits AChE (Ki 10e-8 M) * Monosubstituted carbamate * Uses: - treatment of glaucoma - in ER, physostigmine salicylate has been used to treat overdoses of anticholinergics (e.g. atropine, tricyclic antidepressants) - investigational in Alzheimer's disease |
Reversible Inhibitor
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Neostigmine bromide (Prostigmin)
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* dimethylcarbamate group meta to trimethylammonium group
* dimethylcarbamate enzyme is more resistant to hydrolysis - longer DOA than physostigmine * MOA: inhibit AChE (Ki 10e-7 M) * inhibition of AChE by neostigmine unaffected by pH * Uses: - primarily to prevent post-surgical atony of muscles - myasthenia gravis (skeletal muscle) - ptosis: dropping of eyelid - diplopia: double vision - weakness of jaw muscles & proximal muscles |
Reversible Inhibitor
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Pyridostigmine bromide (Mestinon)
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* disubstituted carbamate
* fairly long DOA (3-6 hrs) * used primarily in treatment of myasthenia gravis * 1/5th as toxic as neostigmine |
Reversible Inhibitor
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Edrophonium chloride (Tensilon)
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* short DOA (minutes)
* used primarily as diagnostic agent for MG * in ER, reversal of curare overdose - used as IM, IV administration * pharmacological challenge with Tensilon transitory but dramatic improvement in muscle function |
Reversible Inhibitor
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Ambenonium chloride (Mytelase)
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* used in treatment of MG for patients that do not respond to neostigmine or pyridostigmine
* derivative of oxalic acid * long DOA |
Reversible Inhibitor
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Demecarium bromide (Humorsol)
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* very lipophilic
* used in treatment of wide angle glaucoma * very long acting (~2 days) * is a potent -> produce lot of cholinergic effect |
Reversible Inhibitor
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Tacrine HCl (Cognex)
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* tetrahydroacridine ring
* MOA: centrally-acting AChE inhibitor * Uses: first drug approved for treatment of AD * limited use (hepatotoxic) * not selective for AChE or BuChE |
Reversible Inhibitor
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Donepezil HCl (Aricept)
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* used in treatment of AD & dementia
* MOA: centrally acting, reversible inhibitor of AChE - selectivity for AChE (500-1200X) more than for BuChE - greater affinity for AChE in brain than in periphery - longer DOA - no potential hepatotoxicity |
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Rivastimine (Exelon)
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* aryl carbamate -> long DOA
* centrally acting AChE inhibitor (10 hr) - psuedo - irreversible inhibitor * used in treatment of AD |
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