Index of drugs

Symptomatic treatment of mild to moderately severe dementia in Alzheimer's disease in adult patients.

1 tabl powl. contains 5 mg or 10 mg donepezil hydrochloride. The preparation contains lactose.

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 T_0,5 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.

Hypersensitivity to the active substance, piperidine derivatives or to any of the excipients.

The use of the preparation in patients with severe dementia in Alzheimer's disease, other types of dementia or other types of memory impairment (eg age-related cognitive impairment) has not been studied. The preparation will probably potentiate muscle relaxation caused by succinylcholine derivatives during anesthesia. Cholinesterase inhibitors may exert vagotonic effects on heart rate (eg bradycardia). The above effects may be particularly important in patients with a sick sinus syndrome or supraventricular conduction disorders, such as a sinoatrial or atrioventricular block. There were cases of syncope and seizures. When testing such patients, consideration should be given to the possibility of blocking the heart or sinus arrest. Patients with an increased risk of developing peptic ulcers, eg with a history of peptic ulcer disease or receiving NSAIDs, should be monitored for signs of peptic ulcer disease. Although this was not observed in clinical trials of donepezil hydrochloride, cholinomimetics may cause obstruction of the bladder outlet. Cholinomimetics are considered a possible cause of generalized seizures. However, the occurrence of seizures may also be a symptom of Alzheimer's disease. Cholinomimetics may exacerbate or induce extrapyramidal symptoms. Very rare occurrences of neuroleptic malignant syndrome (NMS) have been reported in connection with donepezil, particularly in patients receiving concomitant antipsychotics. If a patient develops symptoms and symptoms suggestive of NMS or unexplained high fever without other clinical symptoms, treatment should be discontinued. Caution should be exercised when prescribing cholinesterase inhibitors to patients with a history of asthma or obstructive pulmonary disease. Do not administer concomitantly with other acetylcholinesterase inhibitors, cholinergic agonists or antagonists. There are no data on the use of the drug in patients with severe hepatic impairment. The product contains lactose - should not be used in patients with rare hereditary galactose intolerance, Lapp lactase deficiency or malabsorption of glucose-galactose. It must not be used in children under 18 years of age.

The use of the drug during pregnancy is contraindicated, except when it is necessary. Women taking donepezil should not breastfeed

Very common: diarrhea, nausea, headache.Common: cold, anorexia, hallucinations, agitation, unusual dreams and nightmares, fainting, dizziness, insomnia, vomiting, stomach disorders, rash, pruritus, muscle cramps, urinary incontinence, fatigue, pain, accidents. Uncommon: convulsions, bradycardia, gastrointestinal haemorrhage, peptic ulcer of the stomach and duodenum, slight increase in muscle creatine kinase activity in the serum. Rare: extrapyramidal symptoms, sinoatrial block, atrioventricular block, liver dysfunction, including hepatitis. Very rare: a neuroleptic malignant syndrome. 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. In case of unexplained liver dysfunction, discontinuation should be considered.

Orally. Adults: the starting dose is 5 mg daily (administered once daily), in the evening, just before bedtime. Administration of a 5 mg daily dose should be continued for at least 1 month, allowing the earliest clinical assessment of treatment efficacy and reaching a steady-state concentration of donepezil hydrochloride. After a clinical review of the treatment for one month, a dose of 5 mg per day can be increased to 10 mg per day (administered once a day). The maximum recommended daily dose is 10 mg. Doses above 10 mg per day have not been evaluated in clinical trials. Treatment should be carried out by a doctor who has experience in the diagnosis and treatment of dementia in Alzheimer's disease. The diagnosis should be made in accordance with the approved guidelines (eg according to DSM IV, ICD 10). Donepezil should only be treated if a carer is available to ensure regular monitoring of the patient's use of the medicine. Maintenance treatment can be continued as long as the beneficial effects for the patient are maintained. Therefore, a regular assessment of the clinical benefit of donepezil is required. When there is no longer any indication of therapeutic effect, discontinuation of the drug should be considered. An individual response to donepezil can not be predicted. After discontinuation of treatment, a gradual decrease in the beneficial effects of treatment with the preparation was observed. In patients with renal insufficiency, a similar dosage regimen may be used as in patients with normal renal function. In patients with mild to moderate hepatic insufficiency, the dose should be titrated according to individual patient tolerability. There are no data on the use of the drug in patients with severe hepatic impairment.