Alzepil

Alzepil – the selection inhibitor of acetylcholinesterase of a brain applied to treatment of Alzheimer's disease.

Form of release and structure

Dosage form – tablets, film coated: round, convex from two parties, almost white or white color, on one of the parties an engraving of "E381" (a tablet of 5 mg) or "E382" (a tablet of 10 mg), almost inodorous (on 14 таб. in the blister, in a cardboard pack 2 or 4 blisters).

Contains in 1 tablet of Alzepil:

• Active agent: donepezil a hydrochloride – 5 or 10 mg (5,21 and 10,42 mg of donepezil of a hydrochloride of monohydrate respectively);
• Auxiliary components: hydroxypropyl cellulose low-replaced (L-HPC B1), titanium dioxide, a gipromelloz, magnesium stearate, cellulose microcrystallic, a macrogoal 400, опадрай Y-1-7000 white.

Indications to use

Alzepil – drug for symptomatic therapy of dementia of altsgeymerovsky type of any severity.

Contraindications

Absolute:

• Age up to 18 years;
• Period of pregnancy and lactation;
• Hypersensitivity to components of drug or other derivatives of piperidine.

Relative (Alzepil take with caution):

• Bronchial asthma;
• Chronic obstructive pulmonary disease;
• Disturbances of a heart rhythm;
• Peptic ulcer of a stomach and 12-perstny gut;
• Surgical interventions using the general anesthesia;
• Simultaneous use of non-steroidal anti-inflammatory drugs, holinoblokator or other inhibitors of cholinesterase.

Route of administration and dosage

Alzepil it is necessary to accept in 1 times a day, before going to bed.

Initial dose – 5 mg. Duration of its reception makes 4 weeks then if necessary the dose is raised to 10 mg/days in 1 reception.

The maintenance therapy can be carried out until the therapeutic effect of drug remains (it should be estimated regularly). If Alzepil ceases to act, it needs to be cancelled.

Patients with abnormal liver functions (regardless of severity) do not need dose adjustment as these states do not exert impact on clearance of donepezil.

Side effects

• From the alimentary system: very often (≥1/10) – diarrhea, nausea; often (≥1/100, <1/10) – dyspepsia, vomiting, gastrointestinal frustration, anorexia; infrequently (≥1/1000, ≤1/100) – stomach ulcer and a 12-perstny gut, bleeding from digestive tract;
• From a nervous system: often – dizziness, increased fatigue, a headache, hallucinations, sleeplessness, muscular spasms, an agressive behavior, excitement, a syncope *; infrequently – convulsive attacks *; seldom (≥1/10 000, ≤1/1000) – extrapyramidal symptoms;
• From an urinary system: often – an urine incontience; seldom – abnormal liver functions (including hepatitis);
• From cardiovascular system: infrequently – bradycardia; seldom – atrioventricular and sinuatrial block;
• Dermatological reactions: often – an itch and rash on skin;
• Other: grippopodobny syndrome, pain of various localization;
• Laboratory researches: infrequently – slight increase of activity of a muscular isoform of a kreatinfosfokinaza in blood serum.

* At patients with faints and convulsive attacks cordial blockade is possible.

Special instructions

There are no data on development of a withdrawal in case of the sharp termination of reception of Alzepil, gradual reduction of therapeutic effect of drug is observed.

In need of carrying out operation under the general anesthesia it is necessary to consider that donepezil can increase expressiveness of neuromuscular blockade which is caused by the depolarizing muscle relaxants.

Alzepil can have vagotonic effect on heart rate (in particular, to cause bradycardia). The probability of such effect is important for patients with a sick sinus syndrome and other disturbances of supraventricular conductivity (for example, atrioventricular or sinuatrial block).

Inhibitors of cholinesterase are, presumably, capable to cause generalized spasms to some extent. However convulsive activity can also be manifestation and a basic disease.

Drug is capable to strengthen secretion of hydrochloric acid in a stomach therefore special observation during treatment is required to patients who have a risk of development of stomach ulcer and a 12-perstny gut.

Though in clinical trials this effect did not meet, it is necessary to consider probability of development of an ischuria.

Alzepil can cause dizziness, fatigue and myotonia, especially at the beginning of therapy and at increase in a dose. Besides, the disease concerning which drug is used can be followed by disturbance of speed of reactions and abilities to concentration of attention. For this reason the question of a possibility of driving and performance of potentially dangerous types of works has to be solved individually with the doctor.

Medicinal interaction

Alzepil it is necessary to apply with care along with CYP3A4 and CYP2D6 inhibitors (for example, quinidine, ketokonazoly, itrakonazoly, erythromycin, fluoxetine) as they suppress donepezil metabolism.

Inductors of isoenzymes, such as ethanol, Phenytoinum, rifampicin and carbamazepine, can promote decrease in concentration of donepezil in a blood plasma. As extent of such action is unknown, it is necessary to apply similar combinations also with care.

Donepezil exerts impact on effects of drugs which have anticholinergic activity.

At simultaneous use of agonists of holinoretseptor, quarternary anticholinergic drugs (for example, a bromide glikopirroniya) atypical changes of arterial pressure and heart rate are possible.

In case of the combined use donepezil can strengthen effect of succinylcholine of bromide and other muscle relaxants, agonists of holinoretseptor, the beta adrenoblockers exerting impact on conductivity of heart.

Terms and storage conditions

To store at a temperature which is not exceeding 30 °C in the place, unavailable to children.

Period of validity – 5 years.