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Description of the medicine: Azaleptin (Azaleptinum)

AZALEPTIN (Azaleptinum). 8-Chloro-11- (4-methyl-1-piperazinyl) - 5H-dibenzo- [b, e] [1, 4] -diazepine.

Synonyms: Alemoxan, Clozapine, Leponex, Alemoxan, Clazaril, Clozapine, Iprox, Lapenax, Leponex, Lepotex.

Greenish-yellow crystalline powder. It is practically insoluble in water, it is hardly soluble in alcohol.

The chemical structure is a tricyclic compound having elements of similarity with tricyclic antidepressants and partially with benzodiazepine tranquilizers.

It has strong antipsychotic activity in combination with sedative properties.

It has a muscle-relaxing effect, potentiates the effect of sleeping pills and analgesics.

The characteristic pharmacological features of azaleptin are the inhibition of the activation reaction recorded on an electroencephalogram during electrical stimulation of the reticular formation of the midbrain, a pronounced central and peripheral anticholinergic effect, peripheral a-adrenolytic effect; the drug does not have a cataleptogenic effect; reportedly inhibits dopamine release by presynaptic nerve endings.

It is clinically characterized by a strong antipsychotic effect in combination with a sedative component in the absence of extrapyramidal side effects characteristic of other antipsychotics (which may be due to the central anticholinergic effect of the drug). It does not cause strong general inhibition, like chlorpromazine and other aliphatic phenothiazines.

It is used for hallucinatory-delusional, catatonic-hebephrenic, catatonic-hallucinatory conditions and states of psychomotor agitation in case of schizophrenia, in case of manic syndrome in the framework of manic-depressive psychosis, in case of affective tension and mood disorders, in case of psychopathy in excited patients. In some cases, the drug is effective for resistance to treatment with other antipsychotics.

Assign inside (after eating) 2 to 3 times a day. Single dose for adults 50 - 100 - 200 mg; a daily dose of 200 to 400 mg; maximum daily dose of 600 mg (0.6 g). For maintenance therapy and outpatients, 25 to 200 mg per day is prescribed (possible as a single dose taken in the evening). If necessary, a solution of azaleptin is administered intramuscularly. In small doses (25 - 50 mg), the drug can be used for sleep disorders of various origins.

Azaleptin is usually well tolerated; due to a pronounced central cholinolytic effect and a moderate effect on dopamine receptors, it does not cause extrapyramidal disorders. Nevertheless, with azaleptin treatment, muscle weakness, drowsiness, confusion, dry mouth, orthostatic hypotension, and tachycardia can be observed. The most serious deposition is granulocytopenia (up to agranulocytosis). Therefore, it is necessary to carefully monitor the blood picture.