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Synonyms
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Aricept: Restore Cognitive Function in Alzheimer's Disease
Aricept (donepezil hydrochloride) is a centrally acting reversible acetylcholinesterase inhibitor specifically formulated for the treatment of dementia of the Alzheimer’s type. This prescription medication works by increasing acetylcholine concentrations in the cerebral cortex, thereby enhancing cholinergic neurotransmission. Clinical evidence demonstrates its efficacy in improving cognition, function, and global status in patients with mild to moderate Alzheimer’s disease, with some benefits observed in severe cases. Proper administration under medical supervision can help slow symptom progression and maintain functional abilities longer than without pharmacological intervention.
Features
- Active ingredient: Donepezil hydrochloride
- Available in 5 mg and 10 mg film-coated tablets
- Once-daily dosing regimen
- Rapidly absorbed with relative bioavailability of 100%
- Peak plasma concentration reached in 3-4 hours
- Linear pharmacokinetics across 1-10 mg dose range
- Approximately 96% bound to human plasma proteins
- Metabolized primarily by CYP2D6 and CYP3A4 isoenzymes
- Elimination half-life of approximately 70 hours
- Steady-state plasma concentrations reached within 15-21 days
Benefits
- Cognitive Enhancement: Improves memory, attention, reasoning, and language abilities
- Functional Improvement: Helps maintain activities of daily living including dressing, eating, and personal hygiene
- Behavioral Symptom Management: May reduce apathy, depression, and anxiety associated with Alzheimer’s
- Disease Progression Delay: Slows cognitive and functional decline compared to placebo
- Global Clinical Improvement: Demonstrates statistically significant benefits on clinician-rated global assessment scales
- Long-term Maintenance: Sustained therapeutic effects with continuous treatment
Common use
Aricept is primarily indicated for the treatment of dementia associated with Alzheimer’s disease. It is approved for use in mild, moderate, and severe stages of the condition. The medication is typically prescribed when a diagnosis of probable Alzheimer’s disease has been established according to standard diagnostic criteria such as DSM-IV or NINCDS-ADRDA. Clinical trials have demonstrated effectiveness across various cognitive domains including memory, attention, orientation, and praxis. Many clinicians initiate therapy when patients begin experiencing functional impairment in instrumental activities of daily living or when Mini-Mental State Examination (MMSE) scores fall between 10-26 points.
Dosage and direction
The recommended initial dosage for Aricept is 5 mg administered once daily, preferably at bedtime. This dosage should be maintained for at least 4-6 weeks to assess initial tolerability and therapeutic response. After this period, the dose may be increased to 10 mg once daily if well tolerated. The 10 mg dose has shown greater efficacy in clinical trials but may be associated with increased incidence of side effects.
For patients with severe Alzheimer’s disease, the 23 mg tablet formulation may be considered after patients have been on 10 mg daily for at least three months. Administration should occur at the same time each day, with or without food. Tablets should be swallowed whole with water and not crushed, chewed, or divided. Dose titration should be guided by clinical assessment and tolerability.
Precautions
Patients with cardiac conduction abnormalities should use Aricept with caution due to potential vagotonic effects on heart rate. Those with a history of ulcer disease or taking NSAIDs concurrently require monitoring for gastrointestinal bleeding. Pulmonary conditions such as asthma or COPD warrant careful observation due to increased bronchial secretions. Hepatic impairment may necessitate dosage adjustment as donepezil is extensively metabolized by the liver. Renal impairment generally does not require dosage modification. Patients with seizure disorders should be monitored closely as cholinomimetics may potentially lower seizure threshold. Surgical patients may require temporary discontinuation due to potential effects on neuromuscular transmission.
Contraindications
Aricept is contraindicated in patients with known hypersensitivity to donepezil hydrochloride, piperidine derivatives, or any excipients in the formulation. The medication should not be administered to patients with documented severe liver impairment (Child-Pugh Class C). Concurrent use with other cholinomimetic drugs is contraindicated due to additive pharmacological effects. Patients with known genetic deficiencies of CYP2D6 enzyme activity may require alternative treatments. Those with history of allergic dermatitis to transdermal patches should avoid the tablet formulation as cross-reactivity, though rare, may occur.
Possible side effect
The most common adverse reactions are cholinergic in nature and often dose-dependent. Nausea affects approximately 11% of patients at 5 mg and 24% at 10 mg daily. Diarrhea occurs in approximately 10% and 15% of patients at 5 mg and 10 mg respectively. Insomnia is reported in 6-9% of patients, while fatigue and vomiting affect approximately 5-8%. Muscle cramps occur in approximately 6% of patients, particularly during dose escalation. Other reported effects include anorexia (8-11%), headache (5-7%), dizziness (5-6%), and syncope (2-3%). Bradycardia may develop in approximately 2-3% of patients, particularly those with pre-existing cardiac conduction abnormalities.
Drug interaction
Aricept may potentiate effects of succinylcholine-type muscle relaxants during anesthesia. Concurrent use with anticholinergic medications may reduce therapeutic efficacy. CYP3A4 and CYP2D6 inhibitors such as ketoconazole, quinidine, and paroxetine may increase donepezil concentrations. Beta-blockers may enhance bradycardic effects. Cholinesterase inhibitors used concurrently with NSAIDs may increase risk of gastrointestinal bleeding. Donepezil may interfere with anticholinergic medications used for overactive bladder. The medication may theoretically potentiate effects of cholinergic agonists such as bethanechol.
Missed dose
If a dose is missed, it should be taken as soon as remembered unless it is almost time for the next scheduled dose. In that case, the missed dose should be skipped and the regular dosing schedule resumed. Patients should never take a double dose to make up for a missed one. If multiple doses are missed, consultation with the prescribing physician is recommended as dose re-titration may be necessary. For patients with moderate to severe Alzheimer’s, caregivers should maintain strict adherence through medication management systems.
Overdose
Overdose with Aricept may produce severe cholinergic crisis characterized by nausea, vomiting, salivation, sweating, bradycardia, hypotension, respiratory depression, collapse, and convulsions. Muscle weakness, including respiratory muscle paralysis, may occur. 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. Intravenous atropine sulfate titrated to effect is recommended, with initial doses of 1.0 to 2.0 mg IV with subsequent dosing based on clinical response. General supportive measures should be implemented, including maintaining adequate respiration. It is not known whether donepezil or its metabolites can be removed by dialysis.
Storage
Aricept tablets should be stored at controlled room temperature 20°-25°C (68°-77°F) with excursions permitted between 15°-30°C (59°-86°F). The medication should be kept in its original container with the lid tightly closed to protect from moisture and light. Tablets should not be stored in bathroom cabinets or other areas with high humidity. Keep out of reach of children and pets. Do not use tablets that show signs of discoloration, cracking, or other physical deterioration. Proper disposal of unused medication should follow local regulations, typically through medication take-back programs.
Disclaimer
This information is provided for educational purposes only and does not constitute medical advice. Aricept is a prescription medication that should be used only under the supervision of a qualified healthcare professional. Individual results may vary, and not all patients will experience the same benefits or side effects. The safety and efficacy of Aricept in conditions other than Alzheimer’s disease have not been established. Patients should consult their healthcare provider for personalized medical advice and before making any changes to their treatment regimen. Emergency medical attention should be sought for any suspected overdose or severe adverse reactions.
Reviews
Clinical trials involving over 2,700 patients demonstrate that Aricept produces statistically significant improvement in cognitive function as measured by the Alzheimer’s Disease Assessment Scale (ADAS-cog). Global function assessments using the Clinician’s Interview-Based Impression of Change with caregiver input (CIBIC-plus) show meaningful clinical improvement. Long-term studies suggest that benefits may be maintained for up to 55 weeks in responsive patients. Real-world evidence indicates that approximately 40-60% of patients experience clinically meaningful stabilization or improvement in cognitive symptoms. Caregiver reports frequently note improved engagement in daily activities and reduced behavioral symptoms. However, some studies indicate that benefits may be modest, with average ADAS-cog improvements of 2-3 points compared to placebo over 6 months.
