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Azaleptin (Clozapinum, Clozapine) - antipsychotic drug containing the active ingredient clozapine. Azaleptin differs from the "classical" neuroleptics. When clozapine not mentioned catalepsy development and oppression stereotyped behavior induced by amphetamine and apomorphine.
Azaleptin has little effect on blocking D1-3 and D5-receptors and pronounced effect on D4-receptors. Clozapine has a strong anticholinergic, adrenolytic and antihistamine effect, inhibits the activation reaction and has a mild effect antiserotoninergichesky.
In the clinical setting Azaleptin is pronounced and rapid sedation and strong antipsychotic action. Antipsychotic effect of clozapine observed, including schizophrenia patients resistant to treatment by other drugs. In such cases, clozapine is effective and productive symptoms of schizophrenia and the symptoms of hair loss.
Described positive changes in patients with some cognitive impairment with clozapine. In patients with schizophrenia receiving Azaleptin, the frequency of suicide attempts and suicide is significantly reduced compared with patients who did not receive clozapine (in epidemiological studies the frequency of suicide attempts when clozapine was reduced by more than 7 times compared with patients not receiving clozapine).
Azaleptin virtually no effect on prolactin levels and are generally well tolerated by patients. Severe side effects of clozapine observed only in rare cases.
Azaleptin well absorbed in the intestine, the peak plasma concentrations of clozapine achieved within 2.5 hours. Equilibrium plasma concentrations are set for 8-10 days of therapy. The bioavailability of the active ingredient of the drug Azaleptin is about 27-60%. Clozapine accumulates in parenchymatous organs (liver, lung, kidney). Almost 95% of clozapine is associated with plasma proteins.
Clozapine is metabolized in the liver with the formation of inactive or low metabolites. Excreted mainly kidneys, about 35% is excreted in the bile. Half-life varies from 4 to 12 hours after a single dose of 75 mg clozapine and from 4 to 66 hours when taking 100 mg twice daily clozapine.
Azaleptin intended for oral administration. It is generally recommended to use Azaleptin after meals. The daily dose is usually divided into 2-3 doses, for the treatment of maintenance doses not exceeding 50 mg of clozapine, the daily dose can be administered at one time in the evening. Duration of therapy and clozapine dose determined by the physician.
Adults usually recommended clozapine assignment in a single dose of 50-200 mg. Dose picked individually, starting with 25-100 mg and gradually increasing to achieve the desired therapeutic effect. The dose is usually increased for 1-2 weeks at 25-50 mg per day.
The maximum daily dose is 600 mg clozapine.
After improvement move on to receive maintenance doses of clozapine. Average daily maintenance dose is 150-200 mg clozapine. In some cases, the maintenance dose may be 25-100 mg of clozapine.
Patients with mild disease, underweight and elderly patients, as well as in violation of the kidney and heart and cerebrovascular diseases, are usually not recommended assignment clozapine 200 mg per day.
When receiving excessive doses Azaleptin patients noted the development of drowsiness, confusion, agitation, areflexia, improve reflexes, seizures, hallucinations, mydriasis, tachycardia, body temperature changes, hypotension, cardiac arrhythmias, conduction disturbances infarction, reduction of visual acuity and increase salivation. In severe cases, respiratory depression was noted development, collapse and coma.
A specific antidote is not known. In case of overdose should be as soon as possible to wash out the stomach and assign patient enterosorbentnye funds. In case of overdose of clozapine is necessary to monitor the functions of the respiratory and cardiovascular systems. By prescription symptomatic treatment.
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