A specific and reversible inhibitor of acetylcholinesterase - the main enzyme that breaks down acetylcholine in the brain. In patients with Alzheimer's disease, the drug administered in single doses of 5 mg or 10 mg daily inhibits acetylcholine esterase activity by 63.6% and 77.3% respectively. The ability of donepezil to change the underlying underlying disease of neuropathological changes has not been studied. A 6-month clinical trial conducted in Alzheimer's patients, assessing cognitive abilities, functioning in social and family life and the possibility of independent functioning, confirmed the clinical efficacy of donepezil. The maximum concentration of the drug in the blood occurs 3-4 hours after oral administration. Final T0,5 is about 70 h. Food does not affect the absorption of the drug. Donepezil binds to 95% of plasma proteins. Metabolized with the participation of cytochrome P-450. Excreted mainly in the urine, both in unchanged form and in the form of metabolites.
Contraindications:
Hypersensitivity to donepezil hydrochloride, piperidine derivatives or other components of the preparation.
Precautions:
The preparation is not recommended for children and adolescents. Use with caution in patients with a history of bronchial asthma or obstructive pulmonary disease. Donepezil may increase muscle relaxation caused by succinylcholine derivatives during anesthesia. Donepezil may have a vagotonic effect on heart rate (eg bradycardia), which is important in patients with sick sinus syndrome or other supraventricular conduction disorders, i.e. embolic-atrial block or atrioventricular block. Donepezil as a cholinomimetic may inhibit urinary outflow from the bladder or exacerbate or cause extrapyramidal symptoms. There are no data on the use of the preparation in patients with severe hepatic impairment. The use of donepezil in patients with severe dementia in Alzheimer's disease, other types of dementia or other types of memory impairment (e.g., age-related cognitive impairment) has not been studied. Do not use in patients with rare hereditary galactose intolerance, lactase deficiency (Lapp type) or malabsorption of glucose-galactose.
Pregnancy and lactation:
It should not be used during pregnancy unless it is absolutely necessary and should not be used during breastfeeding.
Side effects:
Very often: diarrhea, nausea; headaches. Common: colds; anorexia; hallucinations, agitation, aggressive behavior; fainting, dizziness, insomnia; vomiting, abdominal disorder; rash, pruritus; muscle cramps; urinary incontinence; fatigue, pain; Accidents. Uncommon: convulsions; bradycardia; gastrointestinal haemorrhage, gastric and duodenal ulcer; slight increase in muscle creatine kinase activity. Rarely: extrapyramidal symptoms; block of emboli-vestibular, atrioventricular block; liver problems, including hepatitis. In patients studied for syncope and seizures, the possibility of blocking the heart or sinus arrest should be considered. Hallucinations, agitation and aggressive behavior subsided after dose reduction or discontinuation of treatment.
Dosage:
Orally, once a day, in the evening, just before bedtime. Starting dose: 5 mg daily for at least 1 month, which will allow a clinical assessment of the effectiveness of treatment and achieving a balance of donepezil hydrochloride levels. After the clinical evaluation, the dose can be increased to 10 mg a day. The maximum recommended daily dose is 10 mg. No dosage adjustment is necessary for patients with renal insufficiency. In patients with mild or moderate hepatic impairment, the dose should be increased according to individual patient tolerability. Treatment with donepezil can only be undertaken in cases where regular monitoring of the patient's intake is possible.Maintenance treatment should be continued for as long as the beneficial effect of the preparation is found; Regular clinical evaluation of the medicine's action is necessary. Discontinuation of the drug should be considered when there is no longer any therapeutic effect.
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