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Aricept

Aricept - General Information

Aricept (Aricept), is a centrally acting reversible acetyl cholinesterase inhibitor. Its main therapeutic use is in the treatment of Alzheimer's disease where it is used to increase cortical acetylcholine. Aricept 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, donepezil's effect may lessen as the disease process advances and fewer cholinergic neurons remain functionally intact. Aricept has been tested in other cognitive disorders including Lewy body dementia and Vascular dementia, but it is not currently approved for these indications. Aricept has also been studied in patients with Mild Cognitive Impairment, schizophrenia, attention deficit disorder, post-coronary bypass cognitive impairment, cognitive impairment associated with multiple sclerosis, and Down syndrome.

 

Pharmacology of Aricept

Aricept is a centrally acting reversible acetyl cholinesterase inhibitor. Its main therapeutic use is in the treatment of Alzheimer's disease where it is used to increase cortical acetylcholine. It is well absorbed in the gut with an oral bioavailability of 100% and easily crosses the blood-brain barrier. Because it has a half life of about 70 hours, it can be taken once a day. Initial dose is 5 mg per day, which can be increased to 10 mg per day after an adjustment period of at least 4 weeks. Aricept is a parasympathomimetic, specifically, a reversible cholinesterase inhibitor. Aricept 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, donepezil's effect may lessen as the disease process advances and fewer cholinergic neurons remain functionally intact. There is no evidence that donepezil alters the course of the underlying dementing process.

 

Aricept for patients

Patient Info
ARICEPT� (donepezil HCl) is indicated for the treatment of symptoms of mild to moderate Alzheimer�s disease.
ARICEPT� (donepezil HCl) is well tolerated but may not be for everyone. Some people may experience nausea, diarrhea, insomnia, vomiting, muscle cramps, fatigue or loss of appetite. In studies, these side effects were usually mild and temporary. Some people taking ARICEPT� (donepezil HCl) may experience fainting. People at risk for ulcers should tell their doctors because their condition may get worse.

 

Aricept Interactions

Drugs that inhibit or Induce CYP 2D6 and CYP 3A4 may affect the concentration on Aricept.

 

Aricept Contraindications

ARICEPT is contraindicated in patients with known hypersensitivity to donepezil hydrochloride or to piperidine derivatives.

 

Additional information about Aricept

Aricept Indication: For management of symptoms associated with Alzheimer's Disease
Mechanism Of Action: Aricept's proposed mechanism of action involves the increase of the concentration of acetylcholine through reversible inhibition of its hydrolysis by acetylcholinesterase.
Drug Interactions: Amantadine Possible antagonism of action
Amitriptyline Possible antagonism of action
Amoxapine Possible antagonism of action
Atropine Possible antagonism of action
Azatadine Possible antagonism of action
Benztropine Possible antagonism of action
Biperiden Possible antagonism of action
Brompheniramine Possible antagonism of action
Carbinoxamine Possible antagonism of action
Chlorpheniramine Possible antagonism of action
Chlorpromazine Possible antagonism of action
Chlorprothixene Possible antagonism of action
Cimetidine Possible antagonism of action
Clemastine Possible antagonism of action
Clidinium Possible antagonism of action
Clomipramine Possible antagonism of action
Clozapine Possible antagonism of action
Cyclizine Possible antagonism of action
Cyclobenzaprine Possible antagonism of action
Cyproheptadine Possible antagonism of action
Darifenacin Possible antagonism of action
Desipramine Possible antagonism of action
Dexbrompheniramine Possible antagonism of action
Dicyclomine Possible antagonism of action
Dimenhydrinate Possible antagonism of action
Diphenhydramine Possible antagonism of action
Diphenoxylate Possible antagonism of action
Diphenylpyraline Possible antagonism of action
Disopyramide Possible antagonism of action
Doxepin Possible antagonism of action
Doxylamine Possible antagonism of action
Ethopropazine Possible antagonism of action
Flavoxate Possible antagonism of action
Flupenthixol Possible antagonism of action
Glutethimide Possible antagonism of action
Glycopyrrolate Possible antagonism of action
Hydroxyzine Possible antagonism of action
Hyoscyamine Possible antagonism of action
Imipramine Possible antagonism of action
Isocarboxazid Possible antagonism of action
Loxapine Possible antagonism of action
Maprotiline Possible antagonism of action
Meclizine Possible antagonism of action
Meperidine Possible antagonism of action
Mesoridazine Possible antagonism of action
Methdilazine Possible antagonism of action
Mirtazapine Possible antagonism of action
Moclobemide Possible antagonism of action
Nortriptyline Possible antagonism of action
Olanzapine Possible antagonism of action
Orphenadrine Possible antagonism of action
Oxybutynin Possible antagonism of action
Perphenazine Possible antagonism of action
Phenelzine Possible antagonism of action
Pimozide Possible antagonism of action
Procainamide Possible antagonism of action
Prochlorperazine Possible antagonism of action
Procyclidine Possible antagonism of action
Promazine Possible antagonism of action
Promethazine Possible antagonism of action
Propantheline Possible antagonism of action
Protriptyline Possible antagonism of action
Quetiapine Possible antagonism of action
Quinidine Possible antagonism of action
Quinidine barbiturate Possible antagonism of action
Risperidone Possible antagonism of action
Scopolamine Possible antagonism of action
Sertraline Possible antagonism of action
Thioridazine Possible antagonism of action
Tizanidine Possible antagonism of action
Tolterodine Possible antagonism of action
Tranylcypromine Possible antagonism of action
Trazodone Possible antagonism of action
Trifluoperazine Possible antagonism of action
Triflupromazine Possible antagonism of action
Trihexyphenidyl Possible antagonism of action
Trimeprazine Possible antagonism of action
Trimethobenzamide Possible antagonism of action
Trimipramine Possible antagonism of action
Tripelennamine Possible antagonism of action
Triprolidine Possible antagonism of action
Trospium Possible antagonism of action
Ziprasidone Possible antagonism of action
Acepromazine Possible antagonism of action
Aceprometazine Possible antagonism of action
Alverine Possible antagonism of action
Belladona Possible antagonism of action
Isopropamide Possible antagonism of action
Methotrimeprazine Possible antagonism of action
Methylscopolamine Possible antagonism of action
Molindone Possible antagonism of action
Propericiazine Possible antagonism of action
Phenindamine Possible antagonism of action
Pheniramine Possible antagonism of action
Pipotiazine Possible antagonism of action
Scopolamine Possible antagonism of action
Solifenacin Possible antagonism of action
Thioproperazine Possible antagonism of action
Thiothixene Possible antagonism of action
Trospium Possible antagonism of action
Zuclopenthixol Possible antagonism of action
Food Interactions: Avoid alcohol.
Take without regard to meals.
Generic Name: Donepezil
Synonyms: Not Available
Drug Category: Nootropic Agents; Parasympathomimetics
Drug Type: Small Molecule; Approved
Other Brand Names containing Donepezil: Aricept; Aricept ODT; Eranz;
Absorption: Donepezil is well absorbed with a relative oral bioavailability of 100% and reaches peak plasma concentrations in 3 to 4 hours.
Toxicity (Overdose): Symptoms of overdose include severe nausea, vomiting, salivation, sweating, bradycardia, hypotension, respiratory depression, collapse and convulsions. Increasing muscle weakness is a possibility and may result in death if respiratory muscles are involved.
Protein Binding: 96%
Biotransformation: Donepezil is metabolized by CYP 450 isoenzymes 2D6 and 3A4 in the liver and also undergoes glucuronidation. The main metabolite, 6-O-desmethyl donepezil, has been reported to inhibit AChE to the same extent as donepezil in vitro.
Half Life: 70 hours
Dosage Forms of Aricept: Tablet, orally disintegrating Oral
Tablet Oral
Chemical IUPAC Name: 5,6-dimethoxy-2-[[1-(phenylmethyl)piperidin-4-yl]methyl]-2,3-dihydroinden-1-one
Chemical Formula: C24H29NO3
Donepezil on Wikipedia: http://en.wikipedia.org/wiki/Donepezil
Organisms Affected: Humans and other mammals