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Galantamine |
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## indicationFor the treatment of mild to moderate dementia of the Alzheimer's type. Has also been investigated in patients with mild cognitive impairment who did not meet the diagnostic criteria for Alzheimer's disease.## pharmacologyGalantamine is a parasympathomimetic, specifically, a reversible cholinesterase inhibitor. It is indicated for the treatment of mild to moderate dementia of the Alzheimer's type. 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. Galantamine 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 acetylcholinesterase. If this proposed mechanism of action is correct, Galantamine's effect may lessen as the disease progresses and fewer cholinergic neurons remain functionally intact. There is no evidence that Galantamine alters the course of the underlying dementing process.## mechanism of actionGalantamine is a phenanthrene alkaloid and a reversible, competitive acetylcholinesterase inhibitor. It is not structurally related to other acetylcholinesterase inhibitors. Galantamine's proposed mechanism of action involves the reversible inhibition of acetylcholinesterase, which prevents the hydrolysis of acetycholine, leading to an increased concentration of acetylcholine at cholinergic synapses. Galantamine also binds allosterically with nicotinic acetylcholine receptors and may possibly potentiate the action of agonists (such as acetylcholine) at these receptors.## toxicityLD_{50}=75 mg/kg (rat)
## half life7 hours## route of eliminationGalantamine is metabolized by hepatic cytochrome P450 enzymes, glucuronidated, and excreted unchanged in the urine.## drug interactionsAcepromazine: Possible antagonism of actionAceprometazine: Possible antagonism of actionAlverine: Possible antagonism of actionAmantadine: Possible antagonism of actionAmitriptyline: Possible antagonism of actionAmoxapine: Possible antagonism of actionAtropine: Possible antagonism of actionAzatadine: Possible antagonism of actionBenzatropine: Possible antagonism of actionBiperiden: Possible antagonism of actionBrompheniramine: Possible antagonism of actionCarbinoxamine: Possible antagonism of actionChlorpheniramine: Possible antagonism of actionChlorpromazine: Possible antagonism of actionChlorprothixene: Possible antagonism of actionCimetidine: Possible antagonism of actionClemastine: Possible antagonism of actionClidinium: 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 actionDexbrompheniramine: Possible antagonism of actionDicyclomine: Possible antagonism of actionDimenhydrinate: Possible antagonism of actionDiphenhydramine: Possible antagonism of actionDiphenoxylate: Possible antagonism of actionDiphenylpyraline: Possible antagonism of actionDisopyramide: Possible antagonism of actionDoxepin: Possible antagonism of actionDoxylamine: Possible antagonism of actionEthopropazine: 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 actionIsopropamide: Possible antagonism of actionKetoconazole: Ketoconazole increases the effect and toxicity of galantamineLoxapine: Possible antagonism of actionMaprotiline: Possible antagonism of actionMeclizine: Possible antagonism of actionMeperidine: Possible antagonism of actionMesoridazine: Possible antagonism of actionMethdilazine: Possible antagonism of actionMethotrimeprazine: Possible antagonism of actionMethylscopolamine: Possible antagonism of actionMirtazapine: Possible antagonism of actionMoclobemide: Possible antagonism of actionMolindone: Possible antagonism of actionNortriptyline: Possible antagonism of actionOlanzapine: Possible antagonism of actionOrphenadrine: Possible antagonism of actionOxybutynin: Possible antagonism of actionParoxetine: Paroxetine increases the effect and toxicity of galantaminePerphenazine: Possible antagonism of actionPhenelzine: Possible antagonism of actionPhenindamine: Possible antagonism of actionPimozide: Possible antagonism of actionPipotiazine: Possible antagonism of actionProcainamide: Possible antagonism of actionProchlorperazine: Possible antagonism of actionProcyclidine: Possible antagonism of actionPromazine: Possible antagonism of actionPromethazine: Possible antagonism of actionPropantheline: Possible antagonism of actionPropericiazine: Possible antagonism of actionProtriptyline: Possible antagonism of actionQuetiapine: Possible antagonism of actionQuinidine: Possible antagonism of actionQuinidine barbiturate: Possible antagonism of actionRisperidone: Possible antagonism of actionScopolamine: Possible antagonism of actionSertraline: Possible antagonism of actionSolifenacin: Possible antagonism of actionThioproperazine: Possible antagonism of actionThioridazine: Possible antagonism of actionThiothixene: Possible antagonism of actionTizanidine: Possible antagonism of actionTolterodine: Possible antagonism of actionTranylcypromine: Possible antagonism of actionTrazodone: Possible antagonism of actionTrifluoperazine: Possible antagonism of actionTriflupromazine: Possible antagonism of actionTrihexyphenidyl: Possible antagonism of actionTrimeprazine: Possible antagonism of actionTrimethobenzamide: The therapeutic effects of the anticholinergic, Trimethobenzamide, and/or the acetylcholinesterase inhibitor (central), Galantamine, may be reduced due to antagonism. Monitor therapeutic effects of both agents.Trimipramine: Possible antagonism of actionTripelennamine: Possible antagonism of actionTriprolidine: Possible antagonism of actionTrospium: The therapeutic effects of the anticholinergic, Trospium, and/or the acetylcholinesterase inhibitor (central), Galantamine, may be reduced due to antagonism. Monitor therapeutic effects of both agents.Ziprasidone: Possible antagonism of actionZuclopenthixol: Possible antagonism of action |