pharmacopeia
GET
/api/v1/drug/donepezil
2D structure
2-[(1-benzylpiperidin-4-yl)methyl]-5,6-dimethoxy-2,3-dihydroinden-1-one
SMILES COC1=C(C=C2C(=C1)CC(C2=O)CC3CCN(CC3)CC4=CC=CC=C4)OC
InChIKey ADEBPBSSDYVVLD-UHFFFAOYSA-N

Mechanism of action

Sourced from openFDA

Current theories on the pathogenesis of the cognitive signs and symptoms of Alzheimer's disease attribute some of them to a deficiency of cholinergic neurotransmission. Donepezil hydrochloride is postulated to exert its therapeutic effect by enhancing cholinergic function.

Cholinesterase

Indications

Sourced from openFDA
  • Donepezil hydrochloride tablet is an acetylcholinesterase inhibitor indicated for the treatment of dementia of the Alzheimer's type. Efficacy has been demonstrated in patients with mild, moderate, and severe Alzheimer's Disease ( 1 ).ICD-10: G30.9

Contraindications

Sourced from openFDA
  • Known hypersensitivity to donepezil hydrochloride or to piperidine derivatives ( 4 ) Donepezil hydrochloride is contraindicated in patients with known hypersensitivity to donepezil hydrochloride or to piperidine derivatives.contraindicated

Dosage & administration

Sourced from openFDA

Mild to Moderate Alzheimer's Disease: 5 mg to 10 mg once daily ( 2.1 ) Moderate to Severe Alzheimer's Disease: 10 mg to 23 mg once daily ( 2.2 ) 2.1 Dosing in Mild to Moderate Alzheimer’s Disease The recommended starting dosage of donepezil hydrochloride tablet is 5 mg administered once per day in the evening, just prior to retiring. The maximum recommended dosage of donepezil hydrochloride tablets in patients with mild to moderate Alzheimer's disease is 10 mg per day. A dose of 10 mg should not be administered until patients have been on a daily dose of 5 mg for 4 to 6 weeks. 2.2 Dosing in Moderate to Severe Alzheimer’s Disease The recommended starting dosage of donepezil hydrochloride tablet is 5 mg administered once per day in the evening, just prior to retiring. The maximum recommended dosage of donepezil hydrochloride tablets in patients with moderate to severe Alzheimer's disease is 23 mg per day. A dose of 10 mg should not be administered until patients have been on a daily dose of 5 mg for 4 to 6 weeks. A dose of 23 mg per day should not be administered until patients have been on a daily dose of 10 mg for at least 3 months. 2.3 Administration Information Donepezil hydrochloride tablets should be taken in the evening, just prior to retiring. Donepezil hydrochloride tablets can be taken with or without food. The donepezil hydrochloride 23 mg tablet should not be split, crushed, or chewed.

Warnings & precautions

Sourced from openFDA

Cholinesterase inhibitors are likely to exaggerate succinylcholine-type muscle relaxation during anesthesia ( 5.1 ) Cholinesterase inhibitors may have vagotonic effects on the sinoatrial and atrioventricular nodes manifesting as bradycardia or heart block ( 5.2 ) Donepezil hydrochloride can cause vomiting. Patients should be observed closely at initiation of treatment and after dose increases ( 5.3 ) Patients should be monitored closely for symptoms of active or occult gastrointestinal (GI) bleeding, especially those at increased risk for developing ulcers ( 5.4 ) The use of donepezil hydrochloride in a dose of 23 mg once daily is associated with weight loss ( 5.5 ) Cholinomimetics may cause bladder outflow obstructions ( 5.6 ) Cholinomimetics are believed to have some potential to cause generalized convulsions ( 5.7 ) Cholinesterase inhibitors should be prescribed with care to patients with a history of asthma or obstructive pulmonary disease ( 5.8 ) 5.1 Anesthesia Donepezil hydrochloride, as a cholinesterase inhibitor, is likely to exaggerate succinylcholine-type muscle relaxation during anesthesia. 5.2 Cardiovascular Conditions Because of their pharmacological action, cholinesterase inhibitors may have vagotonic effects on the sinoatrial and atrioventricular nodes. This effect may manifest as bradycardia or heart block in patients both with and without known underlying cardiac conduction abnormalities. Syncopal episodes have been reported in association with the use of donepezil hydrochloride.

Adverse reactions

Sourced from openFDA

Most common adverse reactions in clinical studies of donepezil hydrochloride are nausea, diarrhea, insomnia, vomiting, muscle cramps, fatigue, and anorexia ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Lupin Pharmaceuticals, Inc. at 1-800-399-2561 or FDA at 1-800-FDA-1088 or www.fda.gov/ medwatch . The following serious adverse reactions are described below and elsewhere in the labeling: Cardiovascular Conditions [ see Warnings and Precautions ( 5.2 ) ]. Nausea and Vomiting [ see Warnings and Precautions ( 5.3 ) ]. Peptic Ulcer Disease and GI Bleeding [ see Warnings and Precautions ( 5.4 ) ]. Weight Loss [ see Warnings and Precautions ( 5.5 ) ]. Genitourinary Conditions [ see Warnings and Precautions ( 5.6 ) ]. Neurological Conditions: Seizures [ see Warnings and Precautions ( 5.7 ) ]. Pulmonary Conditions [ see Warnings and Precautions ( 5.8 ) ]. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. Donepezil hydrochloride has been administered to over 1,700 individuals during clinical trials worldwide. Approximately 1200 of these patients have been treated for at least 3 months and more than 1,000 patients have been treated for at least 6 months. Controlled and uncontrolled trials in the United States included approximately 900 patients.

Use in specific populations

Sourced from openFDA

Pregnancy: Based on animal data, may cause fetal harm ( 8.1 ) 8.1 Pregnancy Risk Summary There are no adequate data on the developmental risks associated with the use of donepezil hydrochloride in pregnant women. In animal studies, developmental toxicity was not observed when donepezil was administered to pregnant rats and rabbits during organogenesis, but administration to rats during the latter part of pregnancy and throughout lactation resulted in increased stillbirths and decreased offspring survival at clinically relevant doses [ see Data ]. In the U.S. general population, the estimated background risks of major birth defects and miscarriage in clinically recognized pregnancies are 2% to 4% and 15% to 20%, respectively. The background risks of major birth defects and miscarriage for the indicated population are unknown. Data Animal Data: Oral administration of donepezil to pregnant rats and rabbits during the period of organogenesis did not produce any teratogenic effects at doses up to 16 mg/kg/day (approximately 6 times the maximum recommended human dose [MRHD] of 23 mg/day on a mg/m 2 basis) and 10 mg/kg/day (approximately 7 times the MRHD on a mg/m 2 basis), respectively.

Pharmacokinetics

Sourced from openFDA
Metabolism
Pharmacokinetics of donepezil are linear over a dose range of 1 to 10 mg given once daily. The rate and extent of absorption of donepezil hydrochloride tablets are not influenced by food.

Overdosage

Sourced from openFDA

Because strategies for the management of overdose are continually evolving, it is advisable to contact a Poison Control Center to determine the latest recommendations for the management of an overdose of any drug. As in any case of overdose, general supportive measures should be utilized. Overdosage with cholinesterase inhibitors can result in cholinergic crisis characterized by 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. Tertiary anticholinergics such as atropine may be used as an antidote for donepezil hydrochloride overdosage. Intravenous atropine sulfate titrated to effect is recommended: an initial dose of 1.0 to 2.0 mg IV with subsequent doses based upon clinical response. Atypical responses in blood pressure and heart rate have been reported with other cholinomimetics when co-administered with quaternary anticholinergics such as glycopyrrolate.

Approval history

Sourced from openFDA
  • Nov 25, 1996NDANDA020690Eisai Inc
  • Jul 23, 2010NDANDA022568Eisai Inc
  • May 31, 2011ANDAANDA090056Aurobindo
  • May 31, 2011ANDAANDA201001Dr Reddys Labs Ltd
  • May 31, 2011ANDAANDA078662Strides Pharma
  • May 31, 2011ANDAANDA200292Prinston Inc
  • May 31, 2011ANDAANDA090686Torrent Pharms
  • Dec 23, 2014NDANDA206439Abbvie

FAERS reports

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Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
36,381 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Fall3,0718.4%
  2. 2Death2,1255.8%
  3. 3Confusional State1,9895.5%
  4. 4Dizziness1,8235.0%
  5. 5Diarrhoea1,8145.0%
  6. 6Fatigue1,7564.8%
  7. 7Nausea1,6754.6%
  8. 8Drug Ineffective1,6044.4%
  9. 9Hallucination1,5674.3%
  10. 10Asthenia1,5144.2%
  11. 11Somnolence1,3533.7%
  12. 12Vomiting1,3303.7%
  13. 13Decreased Appetite1,2293.4%
  14. 14Drug Interaction1,2233.4%
  15. 15Dyspnoea1,0973.0%

Literature

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Recent PubMed references pinned to Donepezil as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

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The 10 most recently updated of 372 ClinicalTrials.gov registrations naming Donepezil as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Pharmacogenomics

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CPIC-curated drug–gene pairs for Donepezil. Levels describe the strength of curated evidence and guideline status — never a recommendation to test or to adjust therapy.

  • CYP2D6CPIC B/C (provisional)ClinPGx 3FDA label: Informative PGx

Frequently asked questions

How does Donepezil work?
Current theories on the pathogenesis of the cognitive signs and symptoms of Alzheimer's disease attribute some of them to a deficiency of cholinergic neurotransmission. Donepezil hydrochloride is postulated to exert its therapeutic effect by enhancing cholinergic function.
What is Donepezil used for?
According to FDA labeling, Donepezil carries indications including: Donepezil hydrochloride tablet is an acetylcholinesterase inhibitor indicated for the treatment of dementia of the Alzheimer's type. Efficacy has been demonstrated in patients with mild, moderate, and severe Alzheimer's Disease ( 1 ).. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Donepezil?
Donepezil is classified as Anticholinesterases, Cholinesterase Inhibitor, Cholinesterase Inhibitors, Increased Central Nervous System Acetylcholine Activity.
What are the brand names for Donepezil?
Donepezil is marketed under brand names including Adlarity, Aricept, Namzaric.
What are the contraindications for Donepezil?
Donepezil labeling lists contraindications including: Known hypersensitivity to donepezil hydrochloride or to piperidine derivatives ( 4 ) Donepezil hydrochloride is contraindicated in patients with known hypersensitivity to donepezil hydrochloride or to piperidine derivatives.. Always consult the full prescribing information and a clinician.
Note. Data for donepezil is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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