Alzepil, 10 mg 28 pcs.

A selective and reversible inhibitor of acetylcholinesterase, which is the main predominant type of cholinesterase in the brain. In vitro, donepezil inhibits this enzyme more than 1,000 times stronger than butyrylcholinesterase, an enzyme that is mainly outside the CNS.

A single dose of 5 mg or 10 mg in equilibrium is accompanied by a 63.6% and 77.3% inhibition of cholinesterase activity (assessed in the erythrocyte membrane model), respectively. The ability of donepezil hydrochloride to inhibit erythrocyte cholinesterase activity correlates with changes in ADAS-cog scores, which is a sensitive tool for assessing changes in cognitive function. The ability of donepezil hydrochloride to alter the course of concomitant neurological changes has not been investigated. Thus, donepezil cannot be considered to affect disease progression.

The efficacy of donepezil has been investigated in four placebo-controlled studies, two six-month and two one-year studies.

The six-month clinical trial was analyzed using three efficacy criteria after donepezil was completed. They used the ADAS-Cog scale (a measure of cognitive function); the clinician’s impression of change scale based on interviews and data from caregivers (a measure of overall level of function); and the daily activity subscale of the clinical dementia assessment scale (a measure of the patient’s ability to participate in society, perform household chores, favorite activities, and self-care).

Patients who achieved the criteria below were considered to have responded to treatment.

Response = improvement of at least 4 points on the ADAS-Cog scale, no worsening on the CIBIC scale, no worsening on the Daily Activity subscale of the Clinical Dementia Rating Scale.

*p< 0.05, **p< 0.01

Donepezil hydrochloride caused a dose-dependent, statistically significant increase in the percentage of patients who were found to respond to treatment.

Indications

Attention Deficit and Memory Disorder, Alzheimer’s DiseaseSymptomatic treatment for mild to moderate Alzheimer’s disease

Active ingredient

Donepezil

Composition

1 tablet contains:

Active substance:

donepezil hydrochloride monohydrate – 10.42 mg (corresponding to donepezil hydrochloride – 10 mg)

Auxiliary substances:

Microcrystalline cellulose – 192 mg,

hydroxypropylcellulose low-substituted (L-HPC B1) – 48 mg,

magnesium stearate – 2 mg.

Composition of the film coating:

Opadray Y-1-7000 white (hypromellose – 3.75 mg, titanium dioxide – 1.875 mg, macrogol 400 – 0.375 mg) – 6 mg.

How to take, the dosage

Alzepil is used strictly as prescribed by your doctor!

Interaction

Alzepil and/or its metabolites do not inhibit the metabolism of theophylline, warfarin, cimetidine or digoxin.

Special Instructions

Treatment should be prescribed and administered by a specialist experienced in the management of patients with Alzheimer’s-type dementia. The diagnosis of the disease must be made in accordance with generally accepted criteria (e.g., DSM IV, ICD 10). Treatment can only be given if a person is able to control medication administration. Treatment is given as long as there is a therapeutic effect, which should be evaluated regularly.

Contraindications

• hypersensitivity (including to piperidine derivatives);
• pregnancy (see “Administration during pregnancy and lactation”);
• lactation period (see “Administration during pregnancy and lactation”).
• pregnancy (see “Administration during pregnancy and lactation”);
• children under 18 years of age (due to lack of clinical data).

With caution: chronic obstructive pulmonary disease, bronchial asthma, cardiac arrhythmias, general anesthesia, peptic ulcer, concomitant use of NSAIDs, choline blockers or other cholinesterase inhibitors.

Side effects

Nausea, diarrhea, headache, fainting spells, dizziness, insomnia, fatigue, hallucinations, agitation, aggressive behavior (which ceases after dose reduction or drug withdrawal), vomiting, stomach upset, urinary incontinence, rash, skin itching, muscle cramps, anorexia, colds, pain of different localization, slight increase in serum concentration of muscle cretinine phosphokinase, bradycardia, seizures, gastrointestinal bleeding, gastric and duodenal ulcers, sinoatrial and atrioventricular block, extrapyramidal symptoms, liver function disorders, including hepatitis.

Overdose

Symptoms: cholinergic crisis (severe nausea, vomiting, salivation, sweating, bradycardia, arterial hypotension, respiratory depression, collapse and convulsions). Increased muscle weakness is possible, which may be fatal if respiratory muscles are affected.