Donepezil HCl CAS NO 120011-70-3 Inquire about Donepezil HCl 

Tecoland supplies Donepezil HCl bulk active pharmaceutical ingredient (API) to the pharmaceutical industry. Our Donepezil HCl is manufactured by cGMP compliant facility. Welcome to contact us for further details including current DMF status for the product and up to date regulatory status of the manufacturing facility. We look forward to assisting you with your research and development projects.
What is Donepezil HCl

Donepezil is used to help improve mental function in people with Alzheimer’s disease.

Donepezil does not work the same in all people. Some people taking donepezil have improved mental function, while others may have unchanged or even worsening mental function.

Donepezil is not a cure for Alzheimer’s disease. This condition will progress over time, even in people who take donepezil.

Biochem/physiol Actions

Donepezil hydrochloride is a piperidine containing an organic compound and a non-competitive inhibitor. It is useful in treating Alzheimer′s disease, in which dementia is a prominent symptom. Donepezil is shown to induce cognitive ability and overall body function. It has a half-life of 70 hours.
Donepezil monohydrochloride monohydrate is a centrally acting reversible acetylcholinesterase inhibitor.

Posology and method of administration
For Adults/Elderly:

Treatment is initiated at 5 mg/day (once-a-day dosing).The 5 mg/day dose should be maintained for at least one month in order to allow the earliest clinical responses to treatment to be assessed and to allow steady-state concentrations of donepezil hydrochloride to be achieved. Following a one-month clinical assessment of treatment at 5 mg/day, the dose of donepezil can be increased to 10 mg/day (once-a-day dosing). The maximum recommended daily dose is 10 mg. Doses greater than 10 mg/day have not been studied in clinical trials.

Treatment should be initiated and supervised by a physician experienced in the diagnosis and treatment of Alzheimer’s dementia. Diagnosis should be made according to accepted guidelines (e.g. DSM IV, ICD 10). Therapy with donepezil should only be started if a caregiver is available who will regularly monitor drug intake for the patient. Maintenance treatment can be continued for as long as a therapeutic benefit for the patient exists. Therefore, the clinical benefit of donepezil should be reassessed on a regular basis. Discontinuation should be considered when evidence of a therapeutic effect is no longer present. Individual response to donepezil cannot be predicted.

Upon discontinuation of treatment, a gradual abatement of the beneficial effects of Donepezil is seen.

For Renal Impairment

A similar dose schedule can be followed for patients with renal impairment, as clearance of donepezil hydrochloride is not affected by this condition.

For Hepatic Impairment

Due to possible increased exposure in mild to moderate hepatic impairment, dose escalation should be performed according to individual tolerability. There are no data for patients with severe hepatic impairment.

For Pediatric Population

Donepezil is not recommended for use in children and adolescents below 18 years of age.

Donepezil side effects

Get emergency medical help if you have signs of an allergic reaction: hives; difficult breathing; swelling of your face, lips, tongue, or throat.

Donepezil may cause serious side effects. Call your doctor at once if you have:

  • slow heartbeats;
  • a light-headed feeling, like you might pass out;
  • new or worsening stomach pain, heartburn, nausea, or vomiting;
  • a seizure;
  • painful or difficult urination;
  • new or worsening breathing problems; or
  • signs of stomach bleeding–bloody or tarry stools, coughing up blood or vomit that looks like coffee grounds.

Common side effects of donepezil may include:

  • nausea, vomiting, diarrhea;
  • loss of appetite;
  • muscle pain;
  • sleep problems (insomnia); or
  • feeling tired.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Drug Interactions

Cases of QTc interval prolongation and Torsade de Pointes have been reported for donepezil. Caution is advised when donepezil is used in combination with other medicinal products known to prolong the QTc interval and clinical monitoring (ECG) may be required. Examples include:

  • Class IA antiarrhythmics (e.g. quinidine)
  • Class III antiarrhythmics (e.g. amiodarone, sotalol)
  • Certain antidepressants (e.g. citalopram, escitalopram, amitriptyline)
  • Other antipsychotics (e.g. phenothiazine derivatives, sertindole, pimozide, ziprasidone)
  • Certain antibiotics (e.g. clarithromycin, erythromycin, levofloxacin, moxifloxacin)

Donepezil hydrochloride and/or any of its metabolites do not inhibit the metabolism of theophylline, warfarin, cimetidine or digoxin in humans. The metabolism of donepezil hydrochloride is not affected by concurrent administration of digoxin or cimetidine. In vitro studies have shown that the cytochrome P450 isoenzymes 3A4 and to a minor extent 2D6 are involved in the metabolism of donepezil. Drug interaction studies performed in vitro show that ketoconazole and quinidine, inhibitors of CYP3A4 and 2D6 respectively, inhibit donepezil metabolism. Therefore these and other CYP3A4 inhibitors, such as itraconazole and erythromycin, and CYP2D6 inhibitors, such as fluoxetine could inhibit the metabolism of donepezil. In a study in healthy volunteers, ketoconazole increased mean donepezil concentrations by about 30%. Enzyme inducers, such as rifampicin, phenytoin, carbamazepine and alcohol may reduce the levels of donepezil. Since the magnitude of an inhibiting or inducing effect is unknown, such drug combinations should be used with care.

Donepezil hydrochloride has the potential to interfere with medications having anticholinergic activity. There is also the potential for synergistic activity with concomitant treatment involving medications such as succinylcholine, other neuro-muscular blocking agents or cholinergic agonists or beta blocking agents which have effects on cardiac conduction.

Disclaimer:

Information on this page is provided for general information purposes. You should not make a clinical treatment decision based on information contained in this page without consulting other references including the package insert of the drug, textbooks and where relevant, expert opinion. We cannot be held responsible for any errors you make in administering drugs mentioned on this page, nor for use of any erroneous information contained on this page.