donepezil hydrochloride


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donepezil hydrochloride

Aricept

Pharmacologic class: Acetylcholinesterase inhibitor

Therapeutic class: Anti-Alzheimer's agent

Pregnancy risk category C

Action

Reversibly inhibits acetylcholinesterase hydrolysis in CNS, leading to increased acetylcholine level and temporary cognitive improvement in patients with Alzheimer's disease

Availability

Tablets: 5 mg, 10 mg, 23 mg

Tablets (orally disintegrating): 5 mg, 10 mg

Indications and dosages

Mild to moderate Alzheimer's disease

Adults: Initially, 5 mg P.O. daily. After 4 to 6 weeks, may increase dosage to 10 mg at bedtime.

Moderate to severe Alzheimer's disease

Adults: Initially, 10 mg P.O. daily. After 3 months, may increase dosage to 23 mg.

Contraindications

• Hypersensitivity to drug or piperidine derivatives

Precautions

Use cautiously in:

• cardiovascular disease, chronic obstructive pulmonary disease (COPD), asthma, or sick sinus syndrome

• patients at risk for developing ulcers, such as those with history of ulcer disease or those concurrently receiving NSAIDs

• pregnant or breastfeeding patients

• children (safety and efficacy not established).

Administration

• Give with or without food.

• For best response, give at bedtime.

Adverse reactions

CNS: headache, dizziness, vertigo, fatigue, depression, aggression, irritability, restlessness, nervousness, paresthesia, insomnia, abnormal dreams, tremor, aphasia, seizures

CV: chest pain, bradycardia, hypertension, hypotension, vasodilation, atrial fibrillation, heart block

EENT: cataracts, blurred vision, eye irritation, sore throat

GI: nausea, vomiting, diarrhea, anorexia, bloating, epigastric pain, fecal incontinence, GI bleeding

GU: urinary frequency, increased libido, bladder outflow obstruction

Metabolic: dehydration

Musculoskeletal: muscle cramps, arthritis, bone fracture

Respiratory: dyspnea, bronchitis

Skin: pruritus, urticaria, bruising, diaphoresis, rash, flushing

Other: toothache, decreased appetite, weight loss, hot flashes, influenza

Interactions

Drug-drug. Anticholinergics: reduced donepezil effects

Anticholinesterases, cholinomimetics: synergistic effects

Carbamazepine, dexamethasone, phenobarbital, phenytoin, rifampin: accelerated donepezil elimination

NSAIDs: increased risk of GI bleeding

Patient monitoring

Watch closely for increased bronchoconstriction in patients with history of asthma or COPD.

• Assess cardiovascular status. Drug may cause bradycardia from increased vagal tone.

• Monitor closely for signs and symptoms of GI ulcers and bleeding, especially if patient takes NSAIDs concurrently.

Patient teaching

• Advise patient to take drug at bedtime with or without food.

• Instruct patient to allow orally disintegrating tablet to dissolve under tongue and then follow with a glass of water.

• Tell patient not to split, crush, or chew 23-mg tablet.

• Inform patient that drug may slow the heart rate, leading to fainting episodes.

Instruct patient to immediately report signs or symptoms of GI ulcers ("coffee-ground" vomitus, black tarry stools, and abdominal pain), or irregular heartbeat.

• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs mentioned above.

donepezil hydrochloride

(dŏ-nĕp′ĭ-zĭl)
A cholinesterase inhibitor that improves cognitive abilities in patients with Alzheimer's dementia. Its most frequent side effects are diarrhea, nausea, and headache.
References in periodicals archive ?
Indian pharmaceutical firm Zydus Cadila (NSE: CADILAHC) has been granted final approval from the US Food and Drug Administration (FDA) to market Donepezil Hydrochloride tablets in the strength of 23 mg, the company said on Friday.
In December 2014, the FDA approved a combination pill for moderate to severe Alzheimers called Namzaric that combines memantine hydrochloride extended-release (Namenda) and donepezil hydrochloride (Aricept).
Ghoneim, "Determination of donepezil hydrochloride in pharmaceutical formulation and human serum by square-wave adsorptive cathodic stripping voltammetry," Chemia Analityczna, vol.
It said in a regulatory filing that Lupin Pharmaceuticals Inc, the US-based subsidiary of the company, has launched Donepezil Hydrochloride tablets in the US after getting nod from the US Food and Drug Administration (USFDA).
Reddy's packaged in single-use vials Repaglinide Tablets USP, 1 mg, 2 mg Caraco Lamotrigine Orally Disintegrating Tablets, Actavis 25 mg, 50 mg, 100 mg, 200 mg Acamprosate Calcium Delayed-Release Glenmark Tablets, 333 mg RepaglinideTablets USP, 0.5 mg Paddock Labs Tretinoin Gel USP (microspheres), 0.1% Spear Pharmaceuticals Tretinoin Gel USP, 0.04% Spear Pharmaceuticals Fenofibric Acid Delayed-Release Anchen Capsules, 45 mg, 135 mg Metformin Hydrochloride Extended-Release Lupin Tablets USP, 500 mg, 1,000 mg Donepezil Hydrochloride Tablets, 23 mg Par Pharmaceutical AUGUST 2013 Bupropion Hydrobromide Extended-Re- Actavis IeaseTablets,174 mg, 522 mg Naproxen and Esomeprazole Magnesium Dr.
Donepezil hydrochloride (Aricept 5mg/tablet) (Pfizer Pharmaceuticals Inc.) and vitamin C (500 mg/tablet) (Government Pharmaceutical Organization) were used as positive control in this study.
Eisai's Aricept (donepezil hydrochloride) is a piperidine derivative that acts centrally as a reversible AChEI.
Yamanishi, "Research and development of donepezil hydrochloride, a new type of acetylcholinesterase inhibitor, " Japanese Journal of Pharmacology, vol.89, no.1, pp.7-20, 2002.
To date the most successful has been donepezil hydrochloride, showing modest improvement in verbal memory.
(1) Furthermore, donepezil hydrochloride (Aricept), a drug commonly used in patients with Alzheimer's disease, has been reported to cause high-grade A-V block as well as symptomatic sinus bradycardia, presumably due to its inhibition of acetylcholinesterase.
The FDA approved Aricept (donepezil hydrochloride) tablets in the 23-mg strength as a once-daily treatment for moderate-to-severe Alzheimer s.