Azaleptin: instructions for use

Azaleptin is an antipsychotic drug, a neuroleptic that has a central and peripheral anticholinergic, antiserotonin, adrenoblokiruyuschee and antihistaminic effect, has a pronounced soothing and muscular-relaxing effects, enhancing the effect of painkillers and hypnotic drugs.

It belongs to the group of "atypical" neuroleptics due to the fact that it has a special profile of binding to dopamine receptors (high affinity for D4-dopamine receptors and weak blocking of D5, D2, D1, D3 receptors), does not cause general inhibition , extrapyramidal disorders and has a smaller effect on increasing the secretion of prolactin. Azaleptin is highly effective in treating productive disorders (schizophrenia and manic syndrome) that are resistant to other antipsychotic medications. This drug should be administered under the strict supervision of the attending physician, due to the pronounced possible side effects on the cellular composition of the blood (granulocytopenia), cardiovascular system (myocarditis and progressive cardiomyopathy) and the development of malignant neoplasms.

Pharmacological action and pharmacokinetics

The active ingredient of the drug Azaleptin is clozapine - a tricyclic derivative of dibenzodiazepine, similar in its chemical structure to tricyclic antidepressants (rispoleptom, olanzapine and quetiapine) and benzodiazepine tranquilizers. Clozapine metabolism occurs in the liver to norcozapine (N-desmethylclozapine) and benzodiazepines, which have all the pharmacological properties of the original compound, causing the pronounced antipsychotic and anti-anxiety activity of Azaleptine.

The mechanism of the pharmaceutical action of this drug is based on different degrees of blocking different subtypes of CNS receptors: dopamine (with a predominance of blocking D ₂ and less pronounced effects on D ₁ , D ₃ , D ₄ , D ₅ ), muscarinic (M 1, 2, 3, 5), serotonin (5-HT _2A , 5-HT _1A , 5-HT _1C ), H ₁ - histamine and α _1- , α ₂ -adreno-receptors and GABA receptors, and he also has agonism to M ₄ - receptors. Unlike typical antidepressants, Azaleptin has a simultaneous agonistic effect on D2-dopamine receptors in the mesocortical region of the brain with marked suppression of dopaminergic activity in the mesolimbic pathway, which causes a low proportion of extrapyramidal disorders (up to 20%) and the absence of late dyskinesias.

It has a strong antipsychotic, moderate anti-manic and tricyclic-like anti-depressant activity in combination with pronounced anti-anxiety, sedative and hypnotic effects.

Indications for use Azaleptina

Indications for the use of Azaleptin are severe acute and chronic forms of schizophrenia, manic states, marked psychomotor agitation in psychopathies, behavioral and emotional disorders, sleep disorders and other psychotic states (including in child psychiatry), but only in the absence of a therapeutic effect in treatment with classic neuroleptics or with their intolerance.

Method of application and dosing regimen

Azaleptin is available in tablets containing 100 mg of clozapine and excipients (lactose monohydrate, potato starch and calcium stearate) 50 tablets per pack.

It is prescribed for severe forms of mental disorders, with the development of severe side effects (usually extrapyramidal or general depression syndrome) for treatment with traditional neuroleptics, as well as in the absence of treatment efficacy with at least two classical antipsychotics, which were taken in the average therapeutic dosage for a long time, but did not improve the subjective and / or the clinical condition of the patient. Also, the use of this drug should be carried out with constant dynamic observation of the attending physician with mandatory monitoring of laboratory parameters of peripheral blood (general and detailed blood test), ECG - a study and other necessary examinations of the patient to exclude side effects of Azaleptine.

The dose of Azaleptine is set individually - a single dose ranges from 50 to 200 mg, and the daily dose should not exceed 200 - 400 mg. Tablets are taken orally, after meals once at bedtime or 2-3 times a day.

Treatment begins with 25-50 milligrams with a gradual increase of 25-50 mg per day for seven to fourteen days to a mean therapeutic dose of 200 to 300 milligrams.

In severe forms of schizophrenia, hallucinatory-delusional, catatonic-hallucinatory and catatonic-hebephrenic conditions and manic-depressive psychosis, the daily dose is increased to 300-600 milligrams.

Maintenance therapy and treatment of patients with cerebrovascular disorders, hepatic and / or renal failure and chronic heart failure are prescribed in a daily dose of 25 to 200 milligrams.

For the prevention of the development of Azaleptin withdrawal syndrome in the form of insomnia, hyperactivity, severe headache and catatonia, the dose is gradually reduced over a period of seven to fourteen days.

Contraindications to the appointment of Azaleptine

This drug does not apply:

1. during pregnancy and lactation;
2. children under five;
3. with increased individual sensitivity to clozapine or auxiliary components of Azaleptine;
4. with myasthenia gravis;
5. with agranulocytosis or granulocytopenia in history (except for the development of these conditions due to previous chemotherapy);
6. with coma;
7. with drug intoxication, the development of alcohol or other toxic psychosis;
8. with epilepsy and susceptibility to convulsive readiness (including hyperthermic convulsions in children in history).

With caution, Azaleptin is prescribed to patients with cerebrovascular disorders, hepatic and / or renal failure and chronic heart failure, and with the addition of infectious diseases, especially for flu-like SARS, acute respiratory infections with fever, runny nose, cough and / or sore throat.

Side Effects of Azaleptin

Long-term, uncontrolled use of the drug, with non-compliance with the recommended dosages and frequency of administration in patients may occur:

Since the cardiovascular system: arterial and / or orthostatic hypotension with dizziness, tachycardia , arrhythmia. In rare cases - collapse with depression or respiratory arrest, ECG changes, development of cardiomyopathy, myocarditis and pericarditis.
On the part of the digestive system: dry mouth or hypersalivation, vomiting, heartburn, nausea, abdominal discomfort, constipation, increased activity of liver enzymes and cholestasis.
Metabolic disorders: hyperglycemia and weight gain with the formation of obesity, gynecomastia.
On the part of the hematopoietic system: agranulocytosis and granulocytopenia, eosinophilia and leukocytosis of unknown nature (in the first weeks of treatment).
On the part of the central nervous system: drowsiness, severe fatigue, dizziness, severe headache, extrapyramidal symptoms (mild severity), rigidity, tremor, akathisia, or the development of neuroleptic malignant syndrome.
Allergic reactions: skin rash, pigmentation, urticaria , erythema multiforme, photosensitivity and exfoliative dermatitis.

It is also possible disturbance of accommodation, the development of hyperthermia, urination disorders, thermoregulation and sweating.

Use of Azaleptin during pregnancy and lactation

Azaleptin is a highly effective antipsychotic, sedative, hypnotic, anti-anxiety and anti-manic drug that causes changes in peripheral blood, orthostatic and arterial hypotension with cerebrovascular disorders and a tendency to the development and progression of myocarditis, pericarditis and cardiomyopathies. It actively penetrates the feto-placental barrier and does not exclude the possibility of its teratogenic effect on the fetus with the development of feto - and embryopathies, especially when taking the drug in the first trimester of pregnancy.

When nazaleptina is prescribed while breastfeeding, the child may experience a decrease in sucking activity, anxiety or sleep disturbances, seizures or functional disorders of the cardiovascular system in the form of arrhythmias, tachycardia and hypotension.

Azaleptin use in children

Azaleptine is contraindicated for use in children under five years of age. It is used in child psychiatry for acute and chronic schizophrenia, marked behavioral and emotional disorders, sleep disorders and manic-depressive syndromes in adolescence, with a risk of suicide, persistent aggressiveness and hostility. Due to the possible risk of side effects, the lack of complete safety and effectiveness of clozapine in children and adolescents (under 16), it should be taken under the supervision of adults (parents or medical staff).

Drug interactions Azaleptine while taking with other drugs:

1. With ethanol and ethanol-containing drugs, MAO inhibitors and drugs that have a pronounced inhibitory effect on the CNS, there is an increase in severity and an increase in the manifestations of CNS suppression.
2. With drugs of the benzodiazepine group or with prior therapy with benzodiazepines, the risk of arterial orthostatic hypotension development and collaptoid states with depression and respiratory depression increases.
3. With carbamazepine, chloramphenicol, co-trimoxazole, sulfonamides, penicillinamine, pyrazole analgesics and other drugs that cause myelodepression, the oppressive action of the backbone brain is enhanced.
4. With lithium preparations, there is an increased risk of epiphriscues, neuroleptic malignant syndrome, confusion and dyskinesias.
5. With digoxin, heparin, phenytoin, or with other drugs that are characterized by high protein binding - an increase in plasma concentrations of these drugs is possible.
6. With erythromycin and cimetidine - an increase in the concentration of Azaleptin in the blood.
7. With phenytoin and carbamazepine - there is a decrease in the concentration of Azaleptin in the blood.

Analogs Azaleptina

Analogues of Azaleptin are Azaleprol, Leponex, Clozapine, Clozasten. Azoleptin is also available in pellets for children.

Prices for Azaleptin

Azaleptin 25mg 50 tablets - from 450r.

Azaleptin 100mg 50 tablets - from 1200r.