What Is Donepezil?

Donepezil, a hexaoxopyridine oxide, is a second-generation specific reversible central acetylcholinesterase (AChE) inhibitor with little effect on peripheral AChE. By inhibiting AChE activity, this product slows down the decomposition of acetylcholine (ACh) at the synaptic space, thereby increasing the ACh content and improving the cognitive function of patients with Alzheimer's disease (AD). Inhibition of acetylcholinesterase activity is 570 times stronger than that of butyrylcholinesterase, which has a higher selectivity. Oral 10mg / kg can inhibit cholinesterase in the brain, and it has a dose-effect relationship.

Basic Information

Chinese name

Donepezil hydrochloride

Main medicine

Donepezil

Treating symptoms

Long-lasting

It is suitable for the treatment of mild or moderate Alzheimer's dementia symptoms.

Oral: Initially 5 mg / day, taken before bedtime; after 1 month, it can be increased to 10 mg / day according to the specific situation, 3 to 6 months as a course of treatment.

1. Common nausea, vomiting, diarrhea, fatigue, burnout, muscle cramps, lack of appetite, etc. The symptoms are often transient and mild reactions, which can be relieved by continued medication. Laboratory tests showed a slight increase in blood creatine kinase, and no other abnormal values were found.

2. Less common dizziness, headache, mental disorder (illusion, irritability, aggressive behavior), depression, dreaming, lethargy, vision loss, chest pain, arthralgia, stomach pain, gastrointestinal disorders, rash, frequent urination or irregularity.

3. Rare but reported that syncope, bradycardia or arrhythmia, sinoatrial block, atrioventricular block, heart murmur, epilepsy or melena. Few liver damage has been reported.

Sinus syndrome, supraventricular heart conduction disease, gastrointestinal disease active or ulcerative disease, history of asthma or obstructive pulmonary disease, history of epilepsy; use with caution; patients with mild to moderate liver and kidney dysfunction do not need to adjust medication In case of unexplained liver and kidney dysfunction and psychiatric symptoms after administration, reduction or withdrawal should be considered. Overdose may cause cholinergic crisis and can detoxify atropine. There was no rebound from discontinuation of treatment.

Those who are allergic to this product or have a history of allergy to piperidine derivatives, pregnant women are prohibited.

1. Synergistic effect with choline-like drugs, -adrenergic receptor antagonists and neuromuscular blockers.

2. Mutually reduce the efficacy with anticholinergics and should not be combined.

3. When used in combination with CYP3A4 inhibitor and CYP2D6 inhibitor, the blood concentration of this product will increase. Pay attention to possible adverse reactions.

4. Combined with the inducer of cytochrome P450 enzyme system, the blood concentration of this product will decrease, which may reduce the curative effect, so it should be considered to increase the dose as appropriate.

5. Alcohol may reduce the concentration of this product, so the combination of the two should be used with caution.

Note: The above content is only for introduction, the drug use must be carried out by a regular hospital under the guidance of a doctor.