Donepezil (donepezil HCl)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Donepezil hydrochloride is a centrally active, reversible acetylcholinesterase inhibitor.
Donepezil hydrochloride, a piperidine derivative, is a centrally active, reversible inhibitor of acetylcholinesterase.
Donepezil is an anticholinesterase agent that binds reversibly with and inactivates cholinesterases (e.g., acetylcholinesterase), thus inhibiting hydrolysis of acetylcholine. As a result, the concentration of acetylcholine increases at cholinergic synapses. In vitro data and data in animals indicate that the anticholinesterase activity of donepezil is relatively specific for acetylcholinesterase in the brain compared with butyrylcholinesterase inhibition in peripheral tissues.
A deficiency of acetylcholine caused by selective loss of cholinergic neurons in the cerebral cortex, nucleus basalis, and hippocampus is recognized as one of the early pathophysiologic features of Alzheimer's disease associated with memory loss and cognitive deficits. The deficiency of cholinergic transmission has been associated with the accumulation of beta-amyloid peptide and neurofibrillary tangles that is characteristic of Alzheimer's disease. Because synaptic loss has been shown to correlate with cognitive decline in Alzheimer's disease, enhancement of cholinergic function with an anticholinesterase agent such as donepezil is one of the pharmacologic approaches to treatment.
However, the potential benefits of anticholinesterase agents may theoretically diminish as the disease process advances and fewer cholinergic neurons remain functioning.
USES: Donepezil is used to treat confusion (dementia) related to Alzheimer's disease. It does not cure Alzheimer's disease, but it may improve memory, awareness, and the ability to function. This medication is an enzyme blocker that works by restoring the balance of natural substances (neurotransmitters) in the brain.
Generic name: donepezil HCl
Pronunciation: (doh-NEP-eh-zil)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Donepezil
Indications
The following indications are listed for Donepezil:
- Mild To Moderate Alzheimer's Type Dementia
- Moderate To Severe Alzheimer's Type Dementia
Dosing
The manufacturer of donepezil makes no specific recommendations for dosage adjustment in patients with renal or hepatic impairment.
Donepezil hydrochloride is administered orally as conventional film-coated or orally disintegrating tablets. The 2 formulations are bioequivalent. The drug is administered once daily, usually in the evening at bedtime. Donepezil hydrochloride orally disintegrating tablets should be allowed to dissolve on the tongue and followed with water. The 23-mg conventional film-coated tablet should not be split, crushed, or chewed.
Because food does not affect the rate or extent of absorption of donepezil when administered as conventional film-coated tablets, the drug may be administered with or without food. The effect of food on absorption of donepezil when administered as orally disintegrating tablets has not been studied. However, the manufacturer states that any effects are expected to be minimal, and the orally disintegrating tablets may be taken without regard to meals.
The fixed-combination preparation containing memantine hydrochloride and donepezil hydrochloride (Namzaric(R)) may be used in patients receiving a stable dosage of donepezil hydrochloride 10 mg daily. The fixed-combination capsules may be administered with or without food, and should be swallowed intact (and not divided, chewed, or crushed) or may be opened, sprinkled on applesauce, and swallowed without chewing. The entire contents of each capsule should be consumed; the dose should not be divided.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
There is no enhanced messaging for this drug.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
Known hypersensitivity to donepezil or piperidine derivatives or any ingredient in the formulation.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
Common adverse effects reported with donepezil in clinical studies include nausea, diarrhea, insomnia, vomiting, muscle cramps, fatigue, and anorexia.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
No enhanced messaging available.
Safety and efficacy of donepezil have not been established in pediatric patients. Dementia of the Alzheimer's type occurs principally in patients older than 55 years of age.
There are no adequate data to inform the developmental risks associated with the use of donepezil in pregnant women. Animal reproduction studies did not demonstrate any evidence of developmental toxicity when the drug was administered to pregnant rats and rabbits during the period of organogenesis; however, when the drug was administered at clinically relevant doses during later stages of pregnancy and throughout lactation, increased stillbirths and decreased offspring survival were observed.
It is not known whether donepezil is distributed into human milk or if the drug has any effects on nursing infants or milk production. The known benefits of breast-feeding should be considered along with the mother's need for the drug and any potential adverse effects on the breast-fed infant from the drug or underlying maternal condition.
Population pharmacokinetic analysis indicates that clearance of donepezil decreases with increasing age. Compared with patients who were 65 years of age, clearance of donepezil was decreased by 17% in patients 90 years of age and increased by 33% in patients 40 years of age; however, the manufacturer states that these changes may not be clinically important.
ICD codes
No ICD codes are available for this drug.
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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