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Medication Description: 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. Practically insoluble in water, difficult to dissolve in alcohol.

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

It has strong neuroleptic activity combined with sedative properties.

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

Characteristic pharmacological features of azaleptin are registered on the electroencephalogram the inhibition of the activation reaction upon electrical stimulation of the midbrain reticular formation, a pronounced central and peripheral anticholinergic effect, peripheral a -adrenolytic effect; the drug does not have a cataleptogenic effect; According to reports, inhibits the release of dopamine presynaptic nerve endings.

It is clinically characterized by a strong antipsychotic action in combination with a sedative component in the absence of extrapyramidal side effects typical of other neuroleptics (which may be due to the central cholinolytic effect of the drug). Does not cause strong general depression, like aminazin and other aliphatic phenothiazines.

Applied with hallucinatory-delusional, catatonic-hebephrenic, catathophaluccinatory states and states of psychomotor agitation in schizophrenia, with manic syndrome in the framework of manic-depressive psychosis, with affective tension and mood disorders, with psychopathies in unwell patients. In some cases, the drug is effective for resistance to treatment with other antipsychotics.

Assign inside (after eating) 2 - 3 times a day. Single dose for adults 50 - 100 - 200 mg; daily dose of 200 to 400 mg; maximum daily dose of 600 mg (0.6 g). For maintenance therapy and outpatients prescribed 25 to 200 mg per day (can be in the form of a single dose taken in the evening). If necessary, enter a solution of azaleptin 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 anticholinergic effect and moderate effect on dopamine receptors, it does not cause extrapyramidal disorders. Nevertheless, in the treatment with azaleptin, muscle weakness, drowsiness, confusion, dry mouth, orthostatic hypotension, tachycardia can be observed. The most serious condition is granulocytopenia (up to agranulocytosis). Therefore, it is necessary to carefully monitor the blood picture.