What is the use of Donepezil (Aricept)?

From the Guidelines

Donepezil is primarily used to treat symptoms of mild to moderate Alzheimer's disease and other forms of dementia, with high-quality evidence supporting its effectiveness in improving cognitive function and daily living activities in some patients. The medication works by increasing levels of acetylcholine in the brain, a neurotransmitter important for memory and thinking, as shown in studies such as 1.

Key Points to Consider

• Donepezil is a cholinesterase inhibitor, which has been evaluated in 24 studies comparing it to placebo or vitamin E, with most studies focusing on Alzheimer's disease and some on vascular dementia, Parkinson disease dementia, Down syndrome, and mild cognitive impairment 1.
• The standard dosage of donepezil ranges from 5 mg/d to 10 mg/d, with the majority of studies using a 10 mg/d dosage, and the duration of treatment varying from 12 to 156 weeks or even 2 years with interrupted use 1.
• While donepezil does not cure or stop the progression of Alzheimer's disease, it can temporarily improve cognitive function and daily living activities in some patients, with statistically significant treatment effects measured by the ADAS-cog score and CIBIC-plus score in individuals with Alzheimer's disease and vascular dementia 1.
• Common side effects of donepezil include nausea, diarrhea, insomnia, vomiting, muscle cramps, fatigue, and decreased appetite, which are often mild and temporary, and the medication should not be stopped suddenly without consulting a healthcare provider, as this could worsen symptoms.

Clinical Considerations

• Donepezil should be taken regularly as prescribed, even if symptoms don't immediately improve, as benefits may take weeks to become noticeable.
• The medication is contraindicated in patients with a history of hypersensitivity to the drug or piperidine derivatives.
• Healthcare providers should monitor patients for potential side effects and adjust the dosage or discontinue treatment as needed, with consideration of the individual patient's response to treatment and potential benefits and risks.

From the FDA Drug Label

Donepezil 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)

The use of Donepezil (Aricept) is for the treatment of dementia of the Alzheimer’s type, with demonstrated efficacy in patients with mild, moderate, and severe Alzheimer’s Disease 2.

From the Research

Use of Donepezil (Aricept)

• Donepezil is licensed for the treatment of mild-to-moderate Alzheimer's disease (AD) at doses of 5-10 mg/day and has recently been approved in the US for severe AD 3.
• Donepezil is a reversible, noncompetitive, piperidine-type cholinesterase inhibitor, selective for acetylcholinesterase rather than butyrylcholinesterase 4.
• Donepezil 5 and 10 mg/day significantly improved cognition and global clinical function compared with placebo in well-designed short-term trials in patients with mild to moderate Alzheimer's disease 4, 5.
• Donepezil has been shown to provide significant benefits in cognition, global function, and activities of daily living in patients with mild-to-moderate Alzheimer's disease 6, 7.
• Donepezil is generally well tolerated, with the majority of adverse events being mild and transient, and most events being cholinergic in nature, related to the gastrointestinal and nervous systems 4, 7.

Dosage and Efficacy

• Donepezil 10 mg/day significantly delayed the deterioration in activities of daily living (ADL) compared with placebo in a retrospective analysis of one trial 4.
• Donepezil 5 and 10 mg/day significantly improved patients' abilities to perform complex tasks 4.
• A higher dose of donepezil (23 mg/day) has been approved for treatment of patients with moderate to severe AD, particularly for language and visuospatial ability 6.
• Donepezil treatment resulted in statistically significant improvements in cognition and patient activity and social behavior, and was generally well tolerated despite high levels of comorbid illness and concomitant medication use 7.

Safety and Tolerability

• No patients withdrew from the study and there were no serious adverse events or deaths in a 24-week pilot study of donepezil at doses up to 20 mg/day 3.
• Adverse events reported were as expected for donepezil and were all mild to moderate in intensity 3, 7.
• The incidence of serious adverse events was generally similar between donepezil 5 and 10 mg and placebo in short-term trials 4.