Lacrimin may be available in the countries listed below.
Oxybuprocaine hydrochloride (a derivative of Oxybuprocaine) is reported as an ingredient of Lacrimin in the following countries:
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Amoxapen may be available in the countries listed below.
Amoxicillin is reported as an ingredient of Amoxapen in the following countries:
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Class: Parasympathomimetic (Cholinergic) Agents
VA Class: AU300
Chemical Name: 2,3-Dihydro-5,6-dimethoxy-2-[(1-(phenylmethyl)-4-piperidinyl)methyl]-1H-inden-1-one
Molecular Formula: C24H29NO3
CAS Number: 120014-06-4
Brands: Aricept
Centrally active, reversible acetylcholinesterase inhibitor.1 2 3 7
Palliative treatment of mild to moderate dementia of the Alzheimer’s type (Alzheimer’s disease, presenile or senile dementia).1 2 3 4 6 15
Comparative studies have not been performed to date, but donepezil does not share the hepatotoxic potential of tacrine and may be preferable to tacrine as a first-line treatment because it can be administered once daily and does not require regular monitoring of liver function.5 6
Administer conventional or orally disintegrating tablets orally once daily, usually at bedtime.1 2
Administer with or without food.1 2
Orally disintegrating tablets: Place on tongue and allow to dissolve; follow with water.1
Donepezil hydrochloride orally disintegrating and conventional film-coated tablets are bioequivalent.1
Available as donepezil hydrochloride; dosage expressed in terms of the salt.1
Initially, 5 mg daily.1 6 11
Some data suggest the possibility of additional benefit with higher (10 mg daily) dosage in some patients;1 2 6 12 however, additional benefit with the 10-mg dosage has not been demonstrated in controlled clinical studies.1 2 12 Adverse cholinergic effects are more likely with the 10-mg dosage.1 2
Daily administration of 10 mg should not be considered until patient has received 5 mg daily for 4–6 weeks, since occurrence of adverse effects may be influenced by the rate of increase in dosage.1 2 11
No specific recommendation for dosage adjustment.1
Known hypersensitivity to donepezil or piperidine derivatives or any ingredient in the formulation.1
Potential for exaggerated succinylcholine-type muscle relaxation during anesthesia.1
Cholinesterase inhibitors may produce bradycardia or heart block via vagotonic effects on the sinoatrial or AV nodes.1 May occur in patients with or without known cardiac conduction abnormalities.1 14 Syncope reported in patients receiving donepezil.1
Possible diarrhea, nausea, and vomiting, particularly at dosage of 10 mg daily.1
Potential for increased gastric acid secretion.1
Carefully monitor patients, especially those at increased risk for developing ulcers (e.g., those with history of peptic ulcer disease, those receiving concomitant NSAIA therapy), for symptoms of active or occult GI bleeding.1
Although not reported in clinical studies with donepezil, cholinomimetic agents may cause bladder outflow obstruction.1 14
Use with caution in patients with a history of asthma or obstructive pulmonary disease.1
Cholinomimetic agents may have the potential to cause generalized seizures; however, seizures also may be a manifestation of Alzheimer’s disease.1
Category C.1
Not known whether donepezil is distributed into milk.1 Not indicated for use in nursing women.1
Safety and efficacy not established.1
Dementia of the Alzheimer's type occurs principally in patients >55 years of age.1 The mean age of patients receiving donepezil in clinical studies was 73 years of age.1 No substantial differences in most adverse effects in patients ≥65 years of age relative to those <65 years of age.1
Nausea, diarrhea, insomnia, vomiting, muscle cramp, fatigue, anorexia.1
Metabolized by CYP3A4 and CYP2D6.1 Unlikely to cause clinically important induction or inhibition of CYP3A4 or CYP2D6; not known whether donepezil has any enzyme-induction potential.1
Pharmacokinetic interactions unlikely with drugs highly bound to plasma proteins.1
Unlikely to alter clearance of drugs metabolized by CYP3A4 or CYP2D6.1
Possible pharmacokinetic interaction (altered plasma donepezil concentrations) with CYP2D6 or CYP3A4 inducers or inhibitors.1
Drug | Interaction | Comments |
|---|---|---|
Anticholinergic agents | Possible interference with activity of anticholinergic agents1 | |
Carbamazepine | Possible induction of donepezil metabolism1 | |
Cholinergic agonists (e.g., bethanecol) | Synergistic effect1 | |
Cholinesterase inhibitors | Synergistic effect1 | |
Cimetidine | No clinically important effects observed on pharmacokinetics of either drug with concomitant use1 | |
Dexamethasone | Possible induction of donepezil metabolism1 | |
Digoxin | No clinically important effects observed on pharmacokinetics of either drug with concomitant use1 | |
Furosemide | Pharmacokinetic interactions (including protein binding interactions) unlikely1 | |
Ketoconazole | Plasma donepezil concentrations increased by 36% with concomitant use; no change in ketoconazole pharmacokinetics1 Inhibition of donepezil metabolism observed in vitro1 | Clinical importance not known1 |
Neuromuscular blocking agents (e.g., succinylcholine) | Exaggerated muscle relaxation1 | |
Phenobarbital | Possible induction of donepezil metabolism1 | |
Phenytoin | Possible induction of donepezil metabolism1 | |
Quinidine | Inhibition of donepezil metabolism in vitro1 | Clinical importance not known1 |
Rifampin | Possible induction of donepezil metabolism1 | |
Theophylline | Pharmacokinetic interaction unlikely1 | |
Warfarin | Pharmacokinetic interactions (including protein binding interactions) unlikely1 |
Relative oral bioavailability is 100%.1
Orally disintegrating and conventional film-coated tablets are bioequivalent.1
Food does not affect rate or extent of absorption when administered as conventional film-coated tablets.1 Effect of food on donepezil absorption after administration as orally disintegrating tablets has not been studied, but any effects are expected to be minimal; orally disintegrating tablets may be taken without regard to meals.1
Approximately 96% (mainly albumin [75%] and alpha1-acid glycoprotein [21%]).1
Extensively metabolized to 4 major metabolites (2 known to be active) and a number of minor metabolites.1 Is metabolized by CYP2D6 and CYP3A4 and undergoes glucuronidation.1
Eliminated in urine and feces (57 and 15%, respectively, over 10 days, with 28% still unrecovered; about 17% of the dose recovered in urine as unchanged drug).1
About 70 hours.1
In patients with stable alcoholic cirrhosis, clearance appears to be reduced by about 20%.1
In patients with moderate to severe renal impairment (Clcr <22 mL/minute per 1.73 m2), clearance appears to be similar to that in healthy individuals.1
15–30°C.1
Precise mechanism(s) of action in patients with dementia of the Alzheimer’s type not fully elucidated.1 Binds reversibly with and inactivates cholinesterases (e.g., acetylcholinesterase), thus inhibiting hydrolysis of acetylcholine1 3 6 7 10 11 12 15 and resulting in increased acetylcholine concentrations at cholinergic synapses.1 6
Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.1 6
Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs.1
Importance of informing patients of other important precautionary information.1 (See Cautions.)
Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.
Routes | Dosage Forms | Strengths | Brand Names | Manufacturer |
|---|---|---|---|---|
Oral | Tablets, film-coated | 5 mg | Aricept | Eisai, (also promoted by Pfizer) |
10 mg | Aricept | Eisai, (also promoted by Pfizer) | ||
Tablets, orally disintegrating | 5 mg | Aricept ODT | Eisai, (also promoted by Pfizer) | |
10 mg | Aricept ODT | Eisai, (also promoted by Pfizer) |
This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing information was updated 03/2011. Actual costs to patients will vary depending on the use of specific retail or mail-order locations and health insurance copays.
Aricept 10MG Tablets (EISAI): 30/$275.98 or 90/$739.94
Aricept 5MG Tablets (EISAI): 30/$276 or 90/$745.98
This report on medications is for your information only, and is not considered individual patient advice. Because of the changing nature of drug information, please consult your physician or pharmacist about specific clinical use.
The American Society of Health-System Pharmacists, Inc. and Drugs.com represent that the information provided hereunder was formulated with a reasonable standard of care, and in conformity with professional standards in the field. The American Society of Health-System Pharmacists, Inc. and Drugs.com make no representations or warranties, express or implied, including, but not limited to, any implied warranty of merchantability and/or fitness for a particular purpose, with respect to such information and specifically disclaims all such warranties. Users are advised that decisions regarding drug therapy are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and the information is provided for informational purposes only. The entire monograph for a drug should be reviewed for a thorough understanding of the drug's actions, uses and side effects. The American Society of Health-System Pharmacists, Inc. and Drugs.com do not endorse or recommend the use of any drug. The information is not a substitute for medical care.
AHFS Drug Information. © Copyright, 1959-2011, Selected Revisions May 2006. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.
1. Eisai Inc. Aricept (donepezil hydrochloride) tablets and orally disintegrating tablets prescribing information. Teaneck, NJ; 2005 Mar.
2. Eisai Inc. Aricept product monograph. Teaneck, NJ; 1997 Jan.
3. Bryson HM, Benfield P. Donepezil. Drugs Aging. 1997; 10:234-9. [PubMed 9108896]
4. Mohs RC. Donepezil: a viewpoint. Drugs Aging. 1997; 10:240.
5. Whitehouse PJ. Donepezil: a viewpoint. Drugs Aging. 1997; 10:240-1.
6. American Psychiatric Association. Practice guideline for the treatment of patients with Alzheimer’s disease and other dementias of late life. Am J Psychiatry. 1997; 154:1-39.
7. Caspi A. Donepezil, a novel therapy for Alzheimer’s disease. P&T. 1997; 22(Feb):70-4.
8. Rogers SL, Doody R, Mohs R et al. E2020 produces both clinical global and cognitive test improvement in patients with mild to moderately severe Alzheimer’s disease: results of a 30-week phase III trial. Neurology. 1996; 46:A217. [PubMed 8559362]
9. Doraiswamy PM. Current cholinergic therapy for symptoms of Alzheimer’s disease. Primary Psychiatry. 1996; Nov:56-68.
10. Brufani M, Filocamo L, Lappa S et al. New acetylcholinesterase inhibitors. Drugs Fut. 1997; 22:397-410.
11. Anonymous. Donepezil (Aricept) for Alzheimer’s disease. Med Lett Drugs Ther. 1997; 39:53-4. [PubMed 9187642]
12. Rho JP, Lipson LG. Focus on donepezil: a reversible acetylcholinesterase inhibitor for the treatment of Alzheimer’s disease. Formulary. 1997; 32:677-84.
13. Rogers SL, Friedhoff LT. The efficacy and safety of donepezil in patients with Alzheimer’s disease: results of a US multicentre, randomized, double-blind, placebo-controlled trial. The Donepezil Study Group. Dementia. 1996; 7(Nov-Dec):293-303. [PubMed 8915035]
14. Eisai Inc, Teaneck, NJ: Personal communication.
15. Small GW, Rabins PV, Barry PP et al. Diagnosis and treatment of Alzheimer disease and related disorders: consensus statement of the American Association for Geriatric Psychiatry, the Alzheimer’s Association, and the American Geriatrics Society. JAMA. 1997; 278:1363-71. [IDIS 393115] [PubMed 9343469]
16. Doody RS, Stevens JC, Beck C et al. Practice parameter: management of dementia (an evidence-based review). Report of the quality standards subcommittee of the American Academy of Neurology. Neurology. 2001; 56:1154-66. [IDIS 463599] [PubMed 11342679]
Plusvent Accuhaler may be available in the countries listed below.
Fluticasone propionate (a derivative of Fluticasone) is reported as an ingredient of Plusvent Accuhaler in the following countries:
Salmeterol xinafoate (a derivative of Salmeterol) is reported as an ingredient of Plusvent Accuhaler in the following countries:
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Periodil may be available in the countries listed below.
Chlorhexidine digluconate (a derivative of Chlorhexidine) is reported as an ingredient of Periodil in the following countries:
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Flogoral may be available in the countries listed below.
Benzydamine hydrochloride (a derivative of Benzydamine) is reported as an ingredient of Flogoral in the following countries:
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Metoprolol Teva may be available in the countries listed below.
Metoprolol tartrate (a derivative of Metoprolol) is reported as an ingredient of Metoprolol Teva in the following countries:
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Cyanocobalaminum-Darnitsa may be available in the countries listed below.
Cyanocobalamin is reported as an ingredient of Cyanocobalaminum-Darnitsa in the following countries:
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