Index of drugs

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

1 tabl powl. contains 5 mg or 10 mg donepezil hydrochloride; Table. powl. contain lactose. 1 tabl disintegrating in the mouth (ODT) contains 5 mg or 10 mg donepezil hydrochloride; Table. ODT contain lactose, aspartame, maltodextrin.

Selective and reversible acetylcholinesterase inhibitor - the main enzyme that breaks down acetylcholine in the brain. In patients with Alzheimer's disease, the drug administered in therapeutic doses inhibits the enzyme activity in about 64-77%. The inhibition of acetylcholinesterase in red blood cells by donepezil correlates with changes in the ADAS-Cog scale in which selected cognitive aspects are measured. The effect of donepezil on the change in the course of the neuropathological basis has not been studied, therefore, no effect on the progression of the disease can be attributed to the drug. C_maxin the blood occurs 3-4 h after oral administration. The food does not affect absorption. Steady state is achieved within 3 weeks. Donepezil binds to plasma proteins in 95%. It is metabolised in the liver with the participation of cytochrome P450 to many metabolites (one of the metabolites - 6-O-demethyldonepezil is pharmacologically active). The drug is excreted mainly in the urine (57%) and partly in the faeces (15%). T_0,5 is about 70 hours.

Hypersensitivity to donepezil hydrochloride or any of the excipients, as well as hypersensitivity to piperidine derivatives. Pregnancy and breastfeeding. Children.

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. Particularly cautiously use in patients with sinus node syndrome or other supraventricular conduction disorders, i.e. embolic-atrial block or atrioventricular block (the drug may exert a vagotonic effect on the heart rate); in patients with bronchial asthma or obstructive pulmonary disease (the drug works cholinomimetycznie); in patients with an increased risk of peptic ulcer disease (with a history of peptic ulcer disease or taking 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 anesthesia. During treatment, fainting or fits may occur; the possibility of blocking the heart or sinus arrest should be considered. Donepezil as a cholinomimetic can inhibit urinary outflow from the bladder and exacerbate or cause extrapyramidal symptoms. In the event of symptoms of a neuroleptic malignant syndrome (NMS) or a high fever with an unexplained cause, no other clinical symptoms of rheumatism should be stopped with donepezil. In the case of unexplained liver dysfunction, discontinuation of donepezil should be considered. Due to the lactose content, tabl. powl. and tabl. ODT should not be used in patients with hereditary galactose intolerance, Lapp lactase deficiency or malabsorption of glucose-galactose. Due to the content of maltodextrin (glucose), tabl. ODT should not be used in patients with malabsorption of glucose-galactose; Table. ODT may be harmful for patients with phenylketonuria as they contain aspartame (each ODT table contains phenylalanine corresponding to 2.53 mg phenylalanine per single dose).

The use of donepezil during pregnancy is contraindicated. Women using donepezil should not breast-feed.

Very common: diarrhea, nausea, headache. Common: colds, anorexia, hallucinations, agitation, unusual dreams, 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). A neuroleptic malignant syndrome has also been reported.

Orally. Adults (including the elderly): initially 5 mg once a day for at least a month. After a clinical evaluation of the efficacy of the initial dose, the dose can be increased to 10 mg once a day. The maximum recommended daily dose is 10 mg. Treatment should be initiated and supervised by a physician experienced in the diagnosis and treatment of dementia in Alzheimer's disease. The diagnosis should be made in accordance with the approved guidelines (eg DSM V, ICD 10). Donepezil should only be treated if 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.Special flu patients. No dosage adjustment is necessary for patients with renal insufficiency. Due to the possible increased drug exposure in patients with mild to moderate hepatic insufficiency, the dose should be adjusted to the patient's individual tolerability. There are no data on use in patients with severe hepatic impairment.Way of giving. The preparation should be taken in the evening, at bedtime. Place the ODT tablet on the tongue and wait for it to disintegrate and then swallow; you can drink with water.