Symptomatic treatment of mild to moderately severe dementia in Alzheimer's disease.
Composition:
1 tabl powl. contains 5 mg or 10 mg donepezil hydrochloride. The drug contains lactose.
Action:
Selective and reversible acetylcholinesterase inhibitor - the main enzyme that breaks down acetylcholine in the brain. In patients with Alzheimer's disease, a single dose of 5 mg or 10 mg daily inhibits acetylcholine esterase activity by 63.6% and 77.3% respectively. The effect of donepezil on the neuropathology of Alzheimer's disease has not been studied, therefore it can not be concluded that the drug has any effect on the course of this disease. 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 It is about 70 hours. The state of balance is achieved in the third week after the start of treatment. The 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, piperidine derivatives or other components of the preparation. Pregnancy.
Precautions:
The drug is not indicated for use in children. The efficacy of donepezil has not been established in patients with severe dementia in Alzheimer's disease, other types of dementia or other types of memory impairment (eg associated with aging). Particularly cautiously use in patients with sinus node syndrome or supraventricular conduction disorders, i.e. sinoatrial or atrioventricular block (the drug may exert a vagotonic effect on the heart rate); in patients with asthma or obstructive pulmonary disease; in patients with an increased risk of peptic ulcer disease (with a history of peptic ulcer disease or NSAIDs - these patients should be monitored for symptoms of peptic ulcer). The preparation of donepezil together with other acetylcholinesterase inhibitors, agonists or cholinergic antagonists should be avoided. Donepezil may increase muscle relaxation caused by succinylcholine derivatives during general anesthesia. Donepezil, as a cholinomimetic, can inhibit the flow of urine from the bladder and exacerbate or cause extrapyramidal symptoms. In the event of signs and symptoms indicative of a neuroleptic malignant syndrome or in the event of high fevers of unknown origin without additional clinical signs of neuroleptic malignant syndrome, further use of donepezil should be discontinued. There are no data on the use of the drug in patients with severe hepatic impairment. The therapeutic benefits of the medicine should be regularly evaluated. The drug contains lactose - should not be used in patients with hereditary galactose intolerance, Lapp lactase deficiency or malabsorption of glucose-galactose.
Pregnancy and lactation:
The use of the drug during pregnancy is contraindicated. There are no clinical data on exposure to donepezil during pregnancy. Women taking donepezil should not breastfeed. There are no data on the excretion of donepezil hydrochloride in human milk, and no studies have been conducted with lactating women.
Side effects:
Common: cold, anorexia, hallucinations, agitation, aggravation, fainting, dizziness, insomnia, diarrhea, vomiting, nausea, stomach upset, rash, pruritus, muscle cramps, urinary incontinence, headache, fatigue, aches and pains. Uncommon: convulsions, bradycardia, gastrointestinal haemorrhage, peptic ulcer of the stomach and duodenum, slight increase in muscle creatine kinase activity. Rare: extrapyramidal symptoms, sinoatrial block, atrioventricular block, liver dysfunction (including hepatitis). Very rare: a neuroleptic malignant syndrome.
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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