the product in the database has an inactive status
indications:
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 preparation contains lactose.
Action:
A specific and reversible inhibitor of acetylcholinesterase - 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 (measured in the erythrocyte membrane) at steady state by 63.6% and 77.3% respectively. Inhibition of acetylcholinesterase (AChE) in red blood cells is correlated with changes in the ADAS-cog scale - a sensitive scale measuring selected elements of cognitive activity. The ability of donepezil to change the course of the neuropathological base 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 It is about 70 hours. Steady state is achieved within 3 weeks after the start of therapy. 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; it is excreted in the urine (approximately 57%) and faeces (approximately 14.5%).
Contraindications:
Hypersensitivity to donepezil hydrochloride, piperidine derivatives or any of the excipients.
Precautions:
The drug is not recommended for use in children and adolescents. Donepezil hydrochloride, as a cholinesterase inhibitor, may increase muscle relaxation caused by succinylcholine derivatives during anesthesia. Particularly cautiously use in patients with sinus node syndrome, with supraventricular conduction disorders, such as sinoatrial block or atrioventricular block (risk of bradycardia); in patients with bronchial asthma or obstructive pulmonary disease; in patients with an increased risk of peptic ulcer disease (patients with a history of ulcer or receiving NSAIDs, these patients should be monitored for peptic ulcer disease). Cholinomimetics can cause obstruction of the bladder outlet. Fainting and convulsions may occur during treatment; in these patients, the possibility of blocking the heart or sinus arrest should be considered. Cholinomimetics may exacerbate or induce extrapyramidal symptoms. The simultaneous administration of donepezil with other acetylcholinesterase inhibitors, agonists or cholinergic antagonists should be avoided. Due to the lactose content, the drug should not be used in patients with rare hereditary galactose intolerance, Lapp lactase deficiency or malabsorption of glucose-galactose.
Pregnancy and lactation:
There are no data on the use of donepezil in pregnant women; medicine should not be used during pregnancy unless it is necessary. The drug should not be used during breast-feeding.
Side effects:
Very often: diarrhea, nausea; Headache. Common: colds; anorexia; hallucinations, psychomotor agitation, aggressive behavior (receding after dose reduction or discontinuation of treatment); fainting, dizziness, insomnia; vomiting; stomach disorders; 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; sinoatrial block, atrioventricular block; abnormal liver function, including hepatitis (in the case of unexplained liver dysfunction discontinuation of the drug should be considered).
Dosage:
Orally. Adults: the starting dose is 5 mg in one daily dose; this dose should be used for at least one month. After a clinical evaluation of the monthly treatment with the initial dose, the dose can be increased to 10 mg / day. The maximum recommended daily dose is 10 mg.No dosage adjustment is necessary for patients with renal insufficiency. Due to the increased drug exposure in patients with mild to moderate hepatic impairment, the dose should be increased according to individual tolerability; no data on the use of the drug in patients with severe hepatic impairment. The product should be taken in the evening, just before bedtime.
(C)
