donepezil hydrochloride

do·nep·e·zil hydrochloride (d-np-zl)

n.

An acetylcholinesterase inhibitor drug used to treat dementia caused by Alzheimer's disease.

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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

Tablets (orally disintegrating): 5 mg, 10 mg

⊘Indications and dosages

➣ Mild to moderate Alzheimer's disease

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

➣ Severe Alzheimer's disease

Adults: 10 mg P.O. daily

Contraindications

• Hypersensitivity to drug or piperidine derivatives
• Pregnancy or breastfeeding

Precautions

Use cautiously in:
• cardiovascular disease, chronic obstructive pulmonary disease (COPD)
• history of ulcers, GI bleeding, or sick sinus syndrome
• concurrent use of nonsteroidal anti-inflammatory drugs (NSAIDs).

Administration

• Give with or without food.
• For best response, give at bedtime.

Route	Onset	Peak	Duration
P.O.	Unknown	3-4 hr	Unknown

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

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

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

GU: urinary frequency, increased libido

Hepatic: hepatotoxicity

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

Drug-herbs. Jaborandi tree, pill-bearing spurge: increased risk of drug toxicity

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.
• 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), irregular heart beat, unusual tiredness, or yellowing of skin or eyes.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs and herbs mentioned above.