Donepezil, a medication used to treat Alzheimer’s disease.
Trade name Aricept.
It has a small benefit in mental function and ability to function in AD.
IT has not been shown to change the progression of Alzheimer’s disease.
Oral agent.
Pregnancy category US: C (Risk not ruled out).
Bioavailability 100%
Protein binding 96%
Elimination half-life 70 hours
Common side effects include: nausea, trouble sleeping, aggression, diarrhea, feeling tired, and muscle cramps.
Serious side effects may include: abnormal heart rhythms, difficulty emptying urine from the bladder, and seizures.
It is a centrally acting reversible acetylcholinesterase inhibitor.
No evidence that donepezil or other similar agents alters the course or progression of Alzheimer’s disease.
6 to 12-month controlled studies have shown modest benefits in cognition or behavior.
The Food and Drug Administration also approved donepezil for treatment of mild, moderate and severe dementia in Alzheimer’s disease.
Adverse effects: nausea, diarrhea, and vomiting, difficulty sleeping, muscle cramps and loss of appetite.
Most side effects occur in patients taking the 23 mg dose compared to 10 mg or lower doses.
Side effects improved with continued use.
The drug is used with caution in people with heart disease, cardiac conduction disturbances, chronic obstructive pulmonary disease, asthma, severe cardiac arrhythmias and sick sinus syndrome.
Associated with an increased risk of gastrointestinal bleeding.
Maybe associated with bradycardia and fainting and should be used with caution in individuals who are predisposed to seizures.
It binds and reversibly inactivates the cholinesterases, thus inhibiting hydrolysis of acetylcholine, and increases acetylcholine concentrations at cholinergic synapses.
Alzheimer’s disease involves a substantial loss of aspects of the cholinergic system and it is generally accepted that the symptoms of Alzheimer’s disease are related to this cholinergic deficit, particularly in the cerebral cortex and other areas of the brain.
The. loss of cholinergic neurons of the central nervous system (CNS) correlates with the severity of cognitive impairment.
Improves sleep apnea and gait in people with mild Alzheimer’s.
A trial in people with mild cognitive impairment reported the drug was superior to placebo in delaying rate of progression to dementia during the initial 18 months of the study, but this was not sustained at 36 months: it is not indicated for prevention of dementia.
It has no effect on ADHD’s symptoms.