Alzepil tabs 5mg #28

Alzepil user manual

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Composition

1 tablet may include 5 or 10 mg of donepezil hydrochloride, the active ingredient.
Additional ingredients: low-substituted hydroxypropylcellulose, microcrystalline cellulose, magnesium stearate, white opadrai Y-1-7000.

Form of issue

Alzepil is available in the form of tablets (5 or 10 mg) for 28 or 56 pieces per package.

pharmachologic effect

Anticholinesterase.

Pharmacodynamics and pharmacokinetics

Donepezil is a reversible selective inhibitor of the main type of cholinesterase of the brain - acetylcholinesterase. The inhibition of this enzyme with donepezil occurs 1000 and more times more than the inhibition of butyrylcholinesterase, which is mainly outside the central nervous system.
One-time administration of 5-10 mg of Alzepil provides suppression of cholinesterase activity by 63.6% and 77.3%, respectively (when evaluated in erythrocyte envelopes). The use of the drug helps slow the development of Alzheimer's disease, reduce the severity of cognitive symptoms, and in some cases, restore the daily activity of patients. Alzepil regulates violations in the behavioral sphere, reduces the manifestations of hallucinations, apathy, repeated unreasonable movements, and also facilitates the care of patients.
When administered orally (inward), Plasma Smeh uppezil is observed after 3-4 hours. Absorption of donepezil does not depend on food intake. The AUC of the drug and its plasma concentrations increase in proportion to the dose taken. T1 / 2 equals approximately 70 hours, in connection with which the regular intake of single doses ensures the achievement of an equilibrium state of Alzepil for 14-21 days of treatment. The plasma content in the equilibrium state and the pharmacodynamic activity of donepezil during the day are subject to minor changes.
Binding of the drug to plasma proteins is at the level of 95%. Donepezil, like the products of its metabolism (the main metabolite - 6-O-des-methyldonepezil) can be found in the human body for more than 10 days.
Metabolism donepezil, due to the action of the cytochrome P450 system, occurs in the liver. Excretion in the urine is 57%, with 17% in the form of an unchanged drug, with feces up to 14.5% donepezil.
Plasma concentrations of Alzepil and its metabolic products, when taken with 5 mg of the drug, are distributed in the following order: donepezil - 30%, 6-O-desmethyldipine-11%, 5-0-desmethidonepezil - 7%, donepezil cis-N-oxide 9 %, glucuronic conjugate 5-O-desmethyldonepezil - 3%.
With pathologies of the liver of a mild or moderate nature, there is an increase in the equilibrium plasma concentration of donepezil.

Indications for use

Alzepil is prescribed as a drug of maintenance therapy for Alzheimer's disease (dementia of the Alzheimer's type), located at any stage of its development.

Contraindications

Contraindications to the use of Alzepil are:
    hypersensitivity to donepezil or additional ingredients of drugs (including piperidine derivatives);
    breastfeeding and pregnancy;
    age to 18 years.

Be wary when:

    general anesthesia;
    obstructive chronic lung disease;
    heart rhythm disturbances;
    bronchial asthma;
    parallel reception of holinoblockers, NSAIDs or other holinomimetics;
    peptic ulcer of the gastrointestinal tract.

Side effects

    cold;
    bradycardia;
    painful sensations of different localization;
    sinoatrial blockade;
    fainting;
    AV blockade;
    increased fatigue;
    diarrhea;
    dizziness;
    nausea;
    headache;
    muscle cramps;
    vomiting;
    insomnia;
    dyspepsia;
    hallucinations;
    anorexia;
    increased excitement;
    disorders of the gastrointestinal tract;
    aggressive behavior;
    bleeding GIT;
    convulsive seizures;
    peptic ulcer of the gastrointestinal tract;
    extrapyramidal symptoms;
    urinary incontinence;
    hepatitis;
    skin rash;
    violations of hepatic function;
    itching;
    muscle pain.

Alzepil, instructions for use

Alzepil tablets are for oral administration. Preferred time of reception - evening (before bedtime).
Typically, therapy starts with a one-time daily dosage of 5 mg, which should be taken for at least 4 weeks, in order to achieve equilibrium concentrations and determine the early clinical effectiveness of treatment.
In the future, consistent with the therapeutic effect, it is possible to increase the daily dosage to 10 mg, which is the maximum allowable dose of 24 hours.
Supportive treatment is continued until the therapeutic effect of Alzepil is maintained, which must be regularly assessed.
With pathologies of the kidneys and liver of mild and moderate severity, daily dosage adjustment is not performed.

Overdose

When an overdose of Alzepil observed manifestations of a cholinergic crisis, with symptoms of nausea, salivation, vomiting, hyperhidrosis, bradycardia, respiratory depression, lowering blood pressure, convulsions, collapse. Also, there were cases of increasing myasthenia gravis, which can cause death if the muscles of the respiratory system are affected.
The intended treatment consists of standard methods of preventing further intoxication (calling up vomiting, flushing the gastrointestinal tract, prescribing sorbents). As an antidote, iv administration of 1-2 mg of Atropine is used, with adjustment of its further dosages according to the patient's condition. The effectiveness of hemodialysis is unknown.

Interaction

The parallel reception donepezil with carbidopa / levodopa for 21 days does not affect the plasma content of these drugs.
Donepezil, like its metabolites, does not affect the metabolic transformations of theophylline, cimetidine, sertraline, warfarin, thioridazine, digoxin and risperidone, and vice versa.
Metabolism donepezil passes with the participation of cytochrome P450 - ZA4, and also - 2D6, albeit to a lesser extent. Inhibitors of these isoenzymes - quinidine, erythromycin, ketoconazole, fluoxetine, itraconazole, accordingly adversely affect the metabolism of donepezil (for example, ketoconazole increased the content of donepezil by 30%).
The combined use with ketoconazole does not affect its pharmacokinetics.
Joint use of phenytoin, rifampicin, ethanol and carbamazepine may lead to a decrease in the plasma level of Alzepil, which requires caution in their use.
The effect of donepezil on anticholinergic drugs has been proven. With parallel use of Alzepil with muscle relaxants, suxamethonium bromide, beta-adrenoblockers and agonists of cholinergic receptors, their effect was observed to increase.
The combined use of quaternary anticholinergic drugs and cholinergic receptor agonists can lead to atypical cases of changes in blood pressure and heart rate.

Storage conditions

The tablets of the preparation can be stored at a temperature of up to 30 ° C.
Shelf life - 5 years.

special instructions

Supporting treatment with Alzepil is advisable until the observed therapeutic effectiveness, and therefore it is necessary to systematically assess the degree of its effect. In the case of a significant drop in the effectiveness of the drug, its administration is canceled, followed by a gradual decrease in its residual effect. The withdrawal syndrome was not observed. It is impossible to predict a personal response to treatment with donepezil.
At the time of general anesthesia with depolarizing muscle relaxants, donepezil can increase the manifestations of neuromuscular blockade.
The vagotonic effect of cholinomimetics on the heart rate (bradycardia) was noted, and therefore caution is required for their use by patients with cardiac pathologies.
Also, caution in taking Alzepil is necessary in the treatment of patients at risk of ulcerative-erosive lesions of the gastrointestinal tract (a history of an ulcer, intake of NSAIDs, etc.).
Presumably, but without evidence in research, cholinomimetics can lead to a delay in urine.
It is believed that the use of cholinesterase inhibitors can contribute to generalized seizures, but this symptomatology is also inherent in Alzheimer's disease itself.
When carrying out treatment, it is better to refrain from performing precise and dangerous works, as well as driving motor vehicles.

Children

Typically, Alzheimer's disease is formed in old age, and therefore research on its impact on children has not been conducted.

With alcohol

When carrying out therapy with Alzepil, alcoholic beverages should be excluded from the diet.

In pregnancy and lactation

Due to the lack of experience in the use of Alzepil during breastfeeding and pregnancy, its appointment in these periods is not recommended.

Reviews about Alzepil

At this time, Alzheimer's disease therapy, unfortunately, boils down to preventing the formation of its further symptoms and some improvement in the general condition of the patient. Judging by the opinions of doctors and relatives of patients undergoing treatment with Alzepil, this drug does a good job of its task and can significantly delay the development of subsequent manifestations of such a serious pathology, which is certainly dementia of the Alzheimer's type.