Nootropic profile
Donepezil
A reversible acetylcholinesterase inhibitor (marketed as Aricept) that is FDA-approved for Alzheimer's disease and is one of the most widely prescribed cognitive enhancers globally.
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What is Donepezil?
Donepezil (marketed as Aricept by Eisai and Pfizer) is a centrally-acting, reversible acetylcholinesterase inhibitor that is one of the most extensively studied and widely prescribed medications for cognitive impairment.
What it does for you
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How to take it
- Alzheimer's starting dose: 5 mg once daily at bedtime, taken for 4-6 weeks before considering dose escalation to allow tolerability assessment
- Alzheimer's maintenance dose: 10 mg once daily at bedtime; a 23 mg extended-release formulation is available for patients with moderate-to-severe...
- Off-label cognitive enhancement: Lower doses of 2.5-5 mg have been explored in research settings for cognitive enhancement in non-demented individuals,...
- Timing and administration: Typically taken at bedtime due to cholinergic side effects (nausea, vivid dreams); can be taken with or without food; tablet and...
- Long half-life: The elimination half-life of approximately 70 hours means steady-state is reached in about 2-3 weeks, and effects persist for days after...
Watch out for
- Common side effects: Gastrointestinal effects are most frequent, including nausea (11%), diarrhoea (10%), and vomiting, typically occurring during dose...
- Vivid dreams and insomnia: Cholinergic enhancement can cause vivid dreams, nightmares, and sleep disturbances, which is why bedtime administration is...
- Cardiovascular effects: Can cause bradycardia, particularly in patients with underlying cardiac conduction abnormalities; ECG monitoring may be warranted in...
- Cholinergic crisis risk: Overdose can produce cholinergic crisis characterised by severe nausea, vomiting, salivation, sweating, bradycardia, hypotension,...
- Drug interactions: Metabolised primarily by CYP2D6 and CYP3A4; interacts with strong inhibitors (ketoconazole, paroxetine) and inducers (rifampicin,...
The science, if you're curious.
- Selectively and reversibly inhibits acetylcholinesterase (AChE) in the central nervous system, preventing the hydrolysis of acetylcholine and increasing its...
- Demonstrates approximately 1,000-fold selectivity for AChE over butyrylcholinesterase (BuChE), resulting in fewer peripheral cholinergic side effects...
- Chronic treatment leads to upregulation of nicotinic acetylcholine receptors (particularly alpha-7 nAChR), which are involved in attention, working memory,...
- Independent of cholinesterase inhibition, Donepezil has been shown to protect neurons against glutamate-mediated excitotoxicity, oxidative stress, and...
Where to find it
- Rogers et al. (1998): "Donepezil improves cognition and global function in Alzheimer disease: a 15-week, double-blind, placebo-controlled study" in Neurology, one of the pivotal trials leading to FDA approval
- Yesavage et al. (2002): "Donepezil and flight simulator performance: effects on retention of complex skills" in Neurology, demonstrating cognitive enhancement in healthy older adults
- Birks and Harvey (2018): Cochrane systematic review "Donepezil for dementia due to Alzheimer's disease" providing comprehensive meta-analysis of efficacy and safety data
- FDA prescribing information: Complete prescribing information for Aricept (donepezil hydrochloride) including pharmacokinetics, clinical trial data, and safety warnings
- Sharma (2019): "Cholinesterase inhibitors as Alzheimer's therapeutics" in Molecular Medicine Reports, reviewing the mechanisms and clinical evidence for donepezil and related agents
Frequently asked
A reversible acetylcholinesterase inhibitor (marketed as Aricept) that is FDA-approved for Alzheimer's disease and is one of the most widely prescribed cognitive enhancers globally.
The main benefits people report from Donepezil are: Cognitive Enhancement, Focus, Longevity, Memory, Mood.
Alzheimer's starting dose: 5 mg once daily at bedtime, taken for 4-6 weeks before considering dose escalation to allow tolerability assessmentAlzheimer's maintenance dose: 10 mg once daily at bedtime; a 23 mg extended-release formulation is available for patients with moderate-to-severe......
Common side effects: Gastrointestinal effects are most frequent, including nausea (11%), diarrhoea (10%), and vomiting, typically occurring during dose...Vivid dreams and insomnia: Cholinergic enhancement can cause vivid dreams, nightmares, and sleep disturbances, which is why bedtime administration...
Selectively and reversibly inhibits acetylcholinesterase (AChE) in the central nervous system, preventing the hydrolysis of acetylcholine and increasing its...Demonstrates approximately 1,000-fold selectivity for AChE over butyrylcholinesterase (BuChE), resulting in fewer peripheral cholinergic side...
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