Donepezil hydrochloride is a specific reversible inhibitor of acetylcholinesterase, the main cholinesterase in the brain. Administration of the drug in doses of 5-10 mg causes suppression of acetylcholine esterase at steady-state. The inhibition of acetylcholinesterase (AchE) in red blood cells by donepezil hydrochloride is correlated with changes in the ADAS-cog scale, measuring selected elements of cognitive ability. Maximum plasma concentrations are achieved approximately 3-4 hours after oral administration. The food does not affect absorption. Plasma proteins are approximately 95% bound. It is excreted in the urine both in unchanged form and metabolized. T0,5 is about 70 hours.
Contraindications:
Hypersensitivity to the preparation ingredients and piperidine derivatives.
Precautions:
Use with caution in patients with sick sinus syndrome or other supraventricular conduction disorders, such as atrioventricular block or atrio-ventricular block. Caution in people with peptic ulcer disease or taking NSAIDs in patients with a history of asthma or obstructive pulmonary disease. Treatment should be discontinued if symptoms of malignant neuroleptic syndrome occur (elevated body temperature, muscle stiffness, disturbances from the autonomic nervous system, disturbances in consciousness and elevated serum creatine kinase activity). Other symptoms may include myoglobinuria (decomposition of transverse striated muscles) and acute renal failure. Due to the lactose content, patients with rare hereditary galactose intolerance, Lapp lactase deficiency or malabsorption of glucose-galactose should not take this medicine.
Pregnancy and lactation:
There are no data on the use of donepezil in pregnant women. Should be used during pregnancy only in case of undoubted necessity. Women taking donepezil should not breastfeed.
Side effects:
Very common: diarrhea, nausea, headaches. Common: common cold, anorexia, hallucinations, agitation, aggravation (regress after dose reduction or discontinuation of treatment), fainting, dizziness, insomnia, vomiting, stomach upset, rash, pruritus, muscle cramps, urinary incontinence, fatigue, pain. Uncommon: epileptic seizures, bradycardia, gastrointestinal bleeding, gastric and duodenal ulcers, slight increase in plasma creatine kinase concentration. Rare: extrapyramidal symptoms, sinoatrial block, atrioventricular block, liver dysfunction, including hepatitis. Very rare: a neuroleptic malignant syndrome.
Dosage:
Orally, in the evening, immediately before going to bed. Adults / elderly patients: initially, at least for 1 month 5 mg once a day. The dose can then be increased to 10 mg a day. The maximum daily dose is 10 mg. There is no need to change the dosage in patients with renal impairment. In the case of liver dysfunction, the dose should be adjusted individually.
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