Azaleptin - instructions for use, analogues of neuroleptic, reviews and release forms (tablets of 25 mg and 100 mg) of a drug for the treatment of schizophrenia and psychosis in adults, children and pregnancy. Composition and interaction with alcohol

In this article, you can read the instructions for using the drug Azaleptin. There are reviews of visitors to the site - consumers of this medication, as well as the opinions of physicians specialists on the use of neuroleptic Azaleptin in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of Azaleptin in the presence of existing structural analogues.Use for the treatment of schizophrenia, psychosis and sleep disorders in adults, children, as well as during pregnancy and lactation. Composition and interaction of the drug with alcohol.

Azaleptin - antipsychotic agent (neuroleptic), a derivative of dibenzodiazepine. Has a pronounced antipsychotic and sedative effect. Practically does not cause extrapyramidal disorders; in connection with this, clozapine is referred to the group of so-called "atypical" antipsychotics.

The antipsychotic effect is due to the blockade of dopamine D2 receptors in the mesolimbic and mesocortical structures of the brain.

Sedative action is due to blockade of alpha-adrenergic receptors of the reticular formation of the brain stem; antiemetic effect - blockade of dopamine D2 receptors in the trigger zone of the vomiting center; hypothermic action - blockade of dopamine receptors of the hypothalamus. Has peripheral and central m-holinoblokiruyuschee, alpha-adrenergic blocking action. Does not affect the concentration of prolactin in the blood.

Antipsychotic action is close to that of aliphatic phenothiazines, but without a "sub-melancholic shade" and unpleasant subjective sensations,has no cataleptogenic effect, reduces the threshold of convulsive readiness.

Does not affect the higher intellectual functions.

The development of the therapeutic effect is characterized by the gradualness: a rapid onset of hypnotic and sedative action; relief of anxiety, psychomotor agitation and aggressiveness (after 3-6 days); antipsychotic action (after 1-2 weeks); effect on the symptoms of negativity (after 20-40 days).

Composition

Clozapine + excipients.

Pharmacokinetics

When taken orally absorbed from the gastrointestinal tract quickly and almost completely. It is subjected to intensive metabolism at the "first passage" through the liver with the formation of metabolites of low activity or inactive. Metabolized with the participation of the isoenzyme CYP1A2. The distribution is intense and rapid, it penetrates the blood-brain barrier (BBB). Binding to proteins - 95%. It is excreted by the kidneys - 50% and through the intestines - 30%.

Indications

• acute and chronic forms of schizophrenia;
• manic states;
• affective insanity;
• psychomotor agitation in psychopathy;
• emotional and behavioral disorders (including in children);
• sleep disorders.

Forms of release

Tablets 25 mg and 100 mg.

Instructions for use and dosage

Install individually. For oral administration, a single dose of 50-200 mg, daily - 200-400 mg. Treatment usually begins with a dose of 25-50 mg, then gradually increased by 25-50 mg per day to 200-300 mg per day for 7-14 days. The daily dose can be applied once before bedtime or 2-3 times a day after meals. If you cancel treatment, you should gradually reduce the dose within 1-2 weeks. After reaching a therapeutic effect, they switch to a supportive course.

If necessary, clozapine can be administered intramuscularly.

The maximum dose for ingestion is 600 mg per day.

For mild forms of the disease, for maintenance therapy, as well as in patients with hepatic and / or renal insufficiency, chronic heart failure, cerebrovascular disorders are prescribed at lower daily doses (25-200 mg).

Side effect

• drowsiness;
• headache;
• confusion of consciousness;
• extrapyramidal disorders (akinesia, hypokinesia, rigidity of muscles, tremor);
• insomnia;
• restless sleep;
• depression;
• epileptic seizures;
• an increase in the temperature of the central genesis;
• tachycardia;
• arterial hypotension;
• Orthostatic hypotension, accompanied by dizziness;
• arterial hypertension;
• hypersalivation;
• nausea, vomiting;
• dry mouth;
• heartburn;
• increase in body weight;
• increased sweating;
• eosinophilia, granulocytopenia up to agranulocytosis, leukopenia, thrombocytopenia;
• dry mouth;
• constipation;
• disturbances of urination;
• myasthenia gravis;
• decreased potency;
• violation of accommodation.

Contraindications

• granulocytopenia or agranulocytosis in the anamnesis (with the exception of the development of granulocytopenia or agranulocytosis due to previously used chemotherapy);
• oppression of bone marrow hematopoiesis;
• myasthenia gravis;
• comatose conditions;
• toxic psychosis (including alcohol);
• pregnancy;
• lactation period;
• children under 5 years;
• increased sensitivity to clozapine.

Application in pregnancy and lactation

Azaleptin is contraindicated in pregnancy and lactation (breastfeeding).

Use in children

Contraindicated in children under 5 years. The safety and efficacy of clozapine in children and adolescents under the age of 16 years is not established.

special instructions

With caution apply for serious diseases of the cardiovascular system, severe renal and / or hepatic insufficiency, closed-angle glaucoma, with prostatic hyperplasia, intestinal atony, epilepsy, intercurrent diseases with febrile syndrome.

During the treatment period, a systematic control of the peripheral blood pattern is necessary.

When using Azaleptin should be excluded from drinking alcohol.

Impact on the ability to drive vehicles and manage mechanisms

Patients taking clozapine should refrain from potentially dangerous activities associated with the need for concentration and increased speed of psychomotor reactions.

Drug Interactions

With simultaneous use with drugs that exert a depressing effect on the central nervous system (including benzodiazepine derivatives), ethanol-containing drugs, ethanol (alcohol), the severity and frequency of manifestations of the oppressive effect on the central nervous system increases, and the respiratory center is depressed.

At simultaneous application with the means causing arterial hypotension, additive hypotensive effect is possible.

When used simultaneously with agents that cause myelodepression, it is possible to intensify the oppressive effect on bone marrow hematopoiesis; with anticholinergics - it is possible to strengthen the anticholinergic effect.

When used simultaneously with Digoxin or with drugs characterized by high binding to proteins (including heparin, warfarin, phenytoin), it is possible to increase their concentrations in the blood plasma, it is also possible to displace Azaleptin by these means from the sites of its binding to proteins.

With simultaneous application with valproic acid, a change in the concentration of clozapine in the blood plasma is possible, with no clinical manifestations of interaction.

With simultaneous use with carbamazepine, the concentration of clozapine in the blood plasma decreases. Cases of severe pancytopenia and malignant neuroleptic syndrome are described.

With simultaneous application with caffeine, clozapine concentration in the blood plasma increases and it is possible to increase the incidence of side effects.

With simultaneous application of lithium carbonate, myoclonus, convulsions, malignant neuroleptic syndrome, delirium, psychosis are possible.

With simultaneous application with risperidone, an increase in the concentration of Azaleptin in the blood plasma is possible, which is apparently due to a competitive effect on the isoenzyme CYP2D6, which leads to inhibition of clozapine metabolism. With rapid replacement of clozapine with risperidone, dystonia may develop.

Rifampicin can increase the rate of clozapine metabolism by inducing the isoenzymes CYP1A2 and CYP3A.

With simultaneous use with phenytoin, a decrease in the concentration of clozapine in the blood plasma is possible; with fluoxetine, paroxetine, sertraline, fluvoxamine, an increase in the concentration of clozapine in the blood plasma is possible, which in some patients is accompanied by manifestations of toxicity. This effect is particularly pronounced with the simultaneous use of clozapine with fluvoxamine.

With simultaneous use with ciprofloxacin, an increase in the concentration of clozapine in the blood plasma is possible.

Analogues of the drug Azaleptin

Structural analogs for the active substance:

• Azaleprol;
• Clozapine;
• Klozasten;
• Leponeks.

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