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Rivastigmine |
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## indicationFor the treatment of mild to moderate dementia associated with Parkinson's disease or of the Alzheimer's type.## pharmacologyRivastigmine is a parasympathomimetic and a reversible cholinesterase inhibitor. An early pathophysiological feature of Alzheimer's disease that is associated with memory loss and cognitive deficits is a deficiency of acetylcholine as a result of selective loss of cholinergic neurons in the cerebral cortex, nucleus basalis, and hippocampus. Tacrine is postulated to exert its therapeutic effect by enhancing cholinergic function. While the precise mechanism of rivastigmine's action is unknown, it is postulated to exert its therapeutic effect by enhancing cholinergic function. This is accomplished by increasing the concentration of acetylcholine through reversible inhibition of its hydrolysis by cholinesterase. If this proposed mechanism is correct, rivastigmine's effect may lessen as the disease progresses and fewer cholinergic neurons remain functionally intact.## mechanism of actionRivastigmine is a carbamate derivative that is structurally related to physostigmine, but not to donepezil and tacrine. The precise mechanism of rivastigmine has not been fully determined, but it is suggested that rivastigmine binds reversibly with and inactivates chlolinesterase (eg. acetylcholinesterase, butyrylcholinesterase), preventing the hydrolysis of acetycholine, and thus leading to an increased concentration of acetylcholine at cholinergic synapses. The anticholinesterase activity of rivastigmine is relatively specific for brain acetylcholinesterase and butyrylcholinesterase compared with those in peripheral tissues.## biotransformationRivastigmine is rapidly metabolized by cholinesterase-mediated hydrolysis.## half life1.5 hours## route of eliminationRivastigmine is extensively metabolized primarily via cholinesterase-mediated hydrolysis to the decarbamylated metabolite NAP226-90. Renal excretion of the metabolites is the major route of elimination. Less than 1% of the administered dose is excreted in the feces.## drug interactionsAmantadine: Possible antagonism of actionAmitriptyline: Possible antagonism of actionAmoxapine: Possible antagonism of actionAzatadine: Possible antagonism of actionBenzatropine: Possible antagonism of actionBiperiden: Possible antagonism of actionBrompheniramine: Possible antagonism of actionChlorpheniramine: Possible antagonism of actionChlorpromazine: Possible antagonism of actionChlorprothixene: Possible antagonism of actionCimetidine: Possible antagonism of actionClemastine: Possible antagonism of actionClomipramine: Possible antagonism of actionClozapine: Possible antagonism of actionCyclizine: Possible antagonism of actionCyclobenzaprine: Possible antagonism of actionCyproheptadine: Possible antagonism of actionDarifenacin: Possible antagonism of actionDesipramine: Possible antagonism of actionDicyclomine: Possible antagonism of actionDimenhydrinate: Possible antagonism of actionDiphenhydramine: Possible antagonism of actionDisopyramide: Possible antagonism of actionDoxepin: Possible antagonism of actionFlavoxate: Possible antagonism of actionFlupenthixol: Possible antagonism of actionGlutethimide: Possible antagonism of actionGlycopyrrolate: Possible antagonism of actionHydroxyzine: Possible antagonism of actionHyoscyamine: Possible antagonism of actionImipramine: Possible antagonism of actionIsocarboxazid: Possible antagonism of actionLoxapine: Possible antagonism of actionMaprotiline: Possible antagonism of actionMeclizine: Possible antagonism of actionMeperidine: Possible antagonism of actionMesoridazine: Possible antagonism of actionMethotrimeprazine: Possible antagonism of actionMirtazapine: Possible antagonism of actionMoclobemide: Possible antagonism of actionNortriptyline: Possible antagonism of actionOlanzapine: Possible antagonism of actionOrphenadrine: Possible antagonism of actionOxybutynin: Possible antagonism of actionPerphenazine: Possible antagonism of actionPhenelzine: Possible antagonism of actionPimozide: Possible antagonism of actionProcainamide: Possible antagonism of actionProchlorperazine: Possible antagonism of actionPromethazine: Possible antagonism of actionPropericiazine: Possible antagonism of actionQuetiapine: Possible antagonism of actionQuinidine: Possible antagonism of actionThioproperazine: Possible antagonism of actionThioridazine: Possible antagonism of actionTizanidine: Possible antagonism of actionTrazodone: Possible antagonism of actionTrifluoperazine: Possible antagonism of actionTrihexyphenidyl: Possible antagonism of actionTrimethobenzamide: The therapeutic effects of the anticholinergic, Trimethobenzamide, and/or the acetylcholinesterase inhibitor (central), Rivastigmine, may be reduced due to antagonism. Monitor therapeutic effects of both agents.Trospium: The therapeutic effects of the anticholinergic, Trospium, and/or the acetylcholinesterase inhibitor (central), Rivastigmine, may be reduced due to antagonism. Monitor therapeutic effects of both agents. |