Donepezil
What is Donepezil?
- Donepezil (Aricept) is an acetylcholinesterase inhibitor used for therapy of Alzheimer disease.
What are the uses of this medicine?
- Donepezil Aricept is a prescription medicine to treat mild, moderate, and severe Alzheimer’s disease. Aricept can help with mental function and with doing daily tasks. Aricept does not work the same in all people.
Some people may:
- Seem much better
- Get better in small ways or stay the same
- Get worse over time but slower than expected
- Not change and then get worse as expected
- Aricept does not cure Alzheimer’s disease. All patients with Alzheimer’s disease get worse over time, even if they take Aricept.
How does this medicine work?
- Donepezil (doe nep' e zil) is an acetylcholinesterase inhibitor which acts by inhibition of the metabolism of acetylcholine in the postsynaptic clefts, thus enhancing cholinergic neurotransmission.
- Alzheimer disease is associated with a cholinergic deficiency in the cerebral cortex, and the increase in concentration of acetylcholine with acetylcholinesterase inhibition is associated with improvement in cognitive function in patients with Alzheimer dementia.
- Donepezil has selective activity for acetylcholinesterase in the central nervous system with little effect on the enzyme in peripheral tissue.
Who Should Not Use this medicine ?
This medicine cannot be used in patients who:
- are allergic to any of the ingredients in Aricept or to medicines that contain piperidines.
What drug interactions can this medicine cause?
- Cholinesterase inhibitors have the potential to interfere with the activity of anticholinergic medications.
- A synergistic effect may be expected with concomitant administration of succinylcholine, similar neuromuscular blocking agents, or cholinergic agonists.
Is this medicine FDA approved?
- Donepezil was approved for use in the United States in 1996 and is currently the most commonly used acetylcholinesterase inhibitor used for management of Alzheimer disease.
How should this medicine be used?
Recommended dosage: Dosing in Mild to Moderate Alzheimer’s Disease:
- The recommended starting dosage of Aricept is 5 mg administered once per day in the evening, just prior to retiring.
- The maximum recommended dosage of Aricept in patients with mild to moderate Alzheimer’s disease is 10 mg per day.
- A dose of 10 mg should not be administered until patients have been on a daily dose of 5 mg for 4 to 6 weeks.
Dosing in Moderate to Severe Alzheimer’s Disease:
- The recommended starting dosage of Aricept is 5 mg administered once per day in the evening, just prior to retiring.
- The maximum recommended dosage of Aricept in patients with moderate to severe Alzheimer’s disease is 23 mg per day.
- A dose of 10 mg should not be administered until patients have been on a daily dose of 5 mg for 4 to 6 weeks.
- A dose of 23 mg per day should not be administered until patients have been on a daily dose of 10 mg for at least 3 months.
Administration:
- Take Aricept exactly as prescribed by the doctor. Do not stop Aricept or change the dose yourself. Talk with your doctor first.
- Take Aricept one time each day. Aricept can be taken with or without food.
- Aricept 23 mg tablets should be swallowed whole. Do not split, crush, or chew the tablets.
- Aricept ODT melts on the tongue. You should drink some water after the tablet melts.
- If you miss a dose of Aricept, just wait. Take only the next dose at the usual time. Do not take 2 doses at the same time.
- If Aricept is missed for 7 days or more, talk with your doctor before starting again.
- If you take too much Aricept at one time, call your doctor or poison control center, or go to the emergency room right away.
What are the dosage forms and brand names of this medicine?
This medicine is available in fallowing doasage form:
- As Tablets: 5 mg, 10 mg, and 23 mg
- Orally Disintegrating Tablets (ODT): 5 mg and 10 mg
This medicine is available in fallowing brand namesː
- Aricept
- Aricept ODT
What side effects can this medication cause?
The most common side effects of this medicine include:
Aricept may cause the following serious side effects:
- slow heartbeat and fainting
- more stomach acid
- worsening of lung problems in people with asthma or other lung disease
- seizures
- difficulty passing urine
What special precautions should I follow?
- Aricept, as a cholinesterase inhibitor, is likely to exaggerate succinylcholine-type muscle relaxation during anesthesia.
- Cholinesterase inhibitors may have vagotonic effects on the sinoatrial and atrioventricular nodes manifesting as bradycardia or heart block.
- Aricept can cause vomiting. Patients should be observed closely at initiation of treatment and after dose increases.
- Patients should be monitored closely for symptoms of active or occult gastrointestinal (GI) bleeding, especially those at increased risk for developing ulcers. Therefore, patients should be monitored closely for symptoms of active or occult gastrointestinal bleeding, especially those at increased risk for developing ulcers, e.g., those with a history of ulcer disease or those receiving concurrent nonsteroidal anti-inflammatory drugs (NSAIDs).
- The use of Aricept in a dose of 23 mg once daily is associated with weight loss.
- Cholinomimetics may cause bladder outflow obstructions.
- Cholinomimetics are believed to have some potential to cause generalized convulsions.
- Cholinesterase inhibitors should be prescribed with care to patients with a history of asthma or obstructive pulmonary disease.
What to do in case of emergency/overdose?
Symptoms of overdosage may include:
- severe nausea
- vomiting
- salivation
- sweating
- bradycardia
- hypotension
- respiratory depression
- collapse
- convulsions
- muscle weakness
Treatment of overdosage:
- As in any case of overdose, general supportive measures should be utilized.
- Tertiary anticholinergics such as atropine may be used as an antidote for Aricept overdosage.
- It is not known whether Aricept and/or its metabolites can be removed by dialysis (hemodialysis, peritoneal dialysis, or hemofiltration).
Can this medicine be used in pregnancy?
- There are no adequate data on the developmental risks associated with the use of Aricept in pregnant women.
Can this medicine be used in children?
- The safety and effectiveness in pediatric patients have not been established.
What are the active and inactive ingredients in this medicine?
Active ingredient: donepezil hydrochloride
Inactive ingredients:
- Aricept 5 mg and 10 mg film-coated tablets: lactose monohydrate, cornstarch, microcrystalline cellulose, hydroxypropyl cellulose, and magnesium stearate. The film coating contains talc, polyethylene glycol, hypromellose, and titanium dioxide. Additionally, the 10 mg tablet contains yellow iron oxide (synthetic) as a coloring agent.
- Aricept 23 mg film-coated tablets: ethylcellulose, hydroxypropyl cellulose, lactose monohydrate, magnesium stearate, and methacrylic acid copolymer, Type C. The reddish color film coating includes ferric oxide, hypromellose 2910, polyethylene glycol 8000, talc, and titanium dioxide.
- Aricept ODT 5 mg and 10 mg tablets: carrageenan, mannitol, colloidal silicon dioxide, and polyvinyl alcohol. The 10 mg tablet contains yellow iron oxide (synthetic) as a coloring agent.
Who manufactures and distributes this medicine?
- Distributed by Eisai Inc., Nutley, NJ
What should I know about storage and disposal of this medication?
- Store Aricept at room temperature between 59º to 86ºF (15º to 30ºC).
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Psychoanaleptics: Anti-dementia agents (ATC code N06D and others) | ||||||
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Sigma receptor modulators | ||||||
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See also: Receptor/signaling modulators
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