Azaleptin: instructions for use
- Azaleptin: instructions for use
- Pharmacological action and pharmacokinetics
- Indications for use Azaleptin
- Method of administration and dosing regimen
- Contraindications to the prescription of Azaleptin
- Side effect of Azaleptin
- Application of Azaleptin during pregnancy and lactation
- Use of Azaleptin in Children
- Analogues of Azaleptin
- Prices for Azaleptin
Azaleptin is an antipsychotic drug, neuroleptic, which has central and peripheral anticholinergic antiserotonin, adrenoblokiruyuschee and antihistamine action, has a pronounced soothing and muscular relaxing effect, enhancing the action of analgesics and hypnotics.
It belongs to the group of "atypical" neuroleptics due to the fact that it has a special binding profile with dopamine receptors (high affinity for D4-dopamine receptors and weak blocking of D5-, D2-, D1-, D3-receptors), does not cause general oppression , extrapyramidal disorders and has less influence on the increase of prolactin secretion. Azaleptin is highly effective in the treatment of productive disorders (schizophrenia and manic syndrome), resistant to therapy with other neuroleptics. Reception of this drug should be carried out under the strict supervision of the attending physician, in connection with the expressed 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
Active ingredient of the drug Azaleptin is clozapine, a tricyclic derivative of dibenzodiazepine, similar in chemical structure to tricyclic antidepressants (rispolept, olanzapine and quetiapine) and benzodiazepine tranquilizers. Metabolism of clozapine occurs in the liver to norclozapine (N-desmethylclozapine) and benzodiazepines, which have all the pharmacological properties that the original compound, causing pronounced antipsychotic and anti-anxiety activity of Azaleptin.
The mechanism of the pharmaceutical effect of this drug is based on the different degree of blocking of different subtypes of the CNS receptors: dopamine (with predominance of blocking D 2 and less pronounced effect on D 1 , D 3 , D 4 , D 5 ), muscarinic (M 1, 2, 3, 5), serotonin (5-HT2A, 5-HT1A, 5-HT1C), H1-histamine and α1, α2-adrenoceptors and GABA receptors, and it also has an agonism for M 4 - receptors. In contrast to 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 accounts for a low proportion of extrapyramidal disorders (up to 20%) and the absence of late dyskinesias.
It has a strong antipsychotic, moderate antimanic and tricyclic-like antidepressant activity in combination with pronounced anti-anxiety, sedation and hypnotics.
Indications for use Azaleptin
Indications for the use of Azaleptin are severe acute and chronic forms of schizophrenia, manic conditions, marked psychomotor agitation in psychopathies, behavioral and emotional disorders, sleep disorders and other psychotic conditions (including in child psychiatry), but only in the absence of therapeutic effect when treatment with classical neuroleptics or with their intolerance.
Method of administration and dosing regimen
Azaleptin is available in tablets containing in its composition 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 (more often extrapyramidal or general oppression syndrome) in the treatment of traditional neuroleptics, and in the absence of treatment effectiveness by at least two classical antipsychotics that have been taken in the meditation dosage for a long time but have not improved the subjective and / or the clinical condition of the patient. Also, the use of this drug should be carried out with constant dynamic observation by the attending physician with mandatory monitoring of laboratory parameters of peripheral blood (general and expanded blood test), ECG-examination and other necessary examinations of the patient to avoid side effects of Azaleptin.
The dose of Azaleptin is determined individually - a single dose is from 50 to 200 mg, and the daily dose should not exceed 200 - 400 mg. Tablets are taken orally, after eating once before 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 medial therapeutic dose of 200 to 300 milligrams.
In severe forms of schizophrenia, hallucinatory-delusional, catatonic hallucinatory and catatonic-hebephrenic states and manic-depressive psychosis, the daily dose is increased to 300-600 milligrams.
Supportive therapy and treatment of patients with cerebrovascular disorders, hepatic and / or renal insufficiency and chronic heart failure is prescribed in a daily dose of 25 to 200 milligrams.
To prevent the development of "withdrawal syndrome" Azaleptin in the form of insomnia, hyperactivity, severe headache and catatonia, the dose is reduced gradually over seven to fourteen days.
Contraindications to the prescription of Azaleptin
This medicine does not apply:
- during pregnancy and lactation;
- in children under five years;
- with increased individual sensitivity to clozapine or ancillary components of Azaleptin;
- with myasthenia gravis;
- with agranulocytosis or granulocytopenia in the anamnesis (except for the development of these conditions due to previously conducted chemotherapy);
- in comatose conditions;
- at intoxication by medicinal preparations, development of alcoholic or other toxic psychoses;
- at an epilepsy and propensity to convulsive readiness (including at a hyperthermal convulsions at children in an anamnesis).
With caution, Azaleptin is prescribed for patients with cerebrovascular disorders, hepatic and / or renal insufficiency and chronic heart failure and when infectious diseases are associated, especially in cases of flu-like ARVI, ARI with fever, runny nose, cough and / or sore throat.
Side effect of Azaleptin
Long-term, uncontrolled use of the drug, with non-compliance with the recommended dosages and the frequency of admission in patients may occur:
From the cardiovascular system: arterial and / or orthostatic hypotension with dizziness, tachycardia , arrhythmia. In rare cases - a collapse with oppression or stopping breathing, changes in the ECG, the development of cardiomyopathies, 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 hematopoiesis system: agranulocytosis and granulocytopenia, eosinophilia and leukocytosis of unknown nature (in the first weeks of treatment).
From the side of the central nervous system: drowsiness, severe fatigue, dizziness, severe headache, extrapyramidal symptoms (mild), rigidity, tremor, akathisia or the development of malignant neuroleptic syndrome.
Allergic reactions: in the form of skin rashes, pigmentation, urticaria , erythema multiforme, photosensitivity and exfoliative dermatitis.
It is also possible to disrupt accommodation, develop hyperthermia, urination disorders, thermoregulation and sweating.
Application of Azaleptin during pregnancy and lactation
Azaleptin is a highly effective antipsychotic, sedative, hypnotic, anti-anxiety and antimanic drug that causes changes in peripheral blood, orthostatic and arterial hypotension with cerebrovascular disorders and a tendency to develop and progress myocarditis, pericarditis and cardiomyopathies. It actively penetrates the feto-placental barrier and the probability 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, is not ruled out.
When prescribing Azaleptin while breastfeeding, the child may experience a decrease in sucking activity, anxiety or sleep disorders, convulsive seizures or functional cardiovascular disorders in the form of arrhythmias, tachycardia, and hypotension.
Use of Azaleptin in Children
Azaleptin is contraindicated for prescription in children up to the age of five. It is used in children's psychiatry for acute and chronic schizophrenia, expressed behavioral and emotional disorders, sleep disorders and manic-depressive syndromes in adolescence, with the risk of suicide, persistent aggression and hostility. In connection with the possible risk of side effects, lack of complete safety and effectiveness of clozapine in children and adolescents (up to 16 years), it should be administered under the supervision of adults (parents or medical personnel).
Azaleptin drug interaction with simultaneous reception with other medicinal products:
- With ethanol and ethanol containing drugs, MAO inhibitors and drugs that have a pronounced oppressive effect on the central nervous system, there is an increase in severity and an increase in the manifestations of CNS suppression.
- With preparations of the benzodiazepine group or with prior therapy with benzodiazepines, the risk of development and progression of arterial and orostatic hypotension, collapoid states with inhibition and stopping of breathing increases.
- With carbamazepine, chloramphenicol, co-trimoxazole, sulfonamides, penicillinamine, pyrazolone analgesics and other drugs that cause myelodepression, the inhibitory effect of the nasal marrow occurs.
- With lithium preparations - increased risk of epicas, malignant neuroleptic syndrome, confusion and dyskinesia.
- With digoxin heparin, phenytoin or with other drugs that are characterized by high binding to proteins - it is possible to increase the concentration of these drugs in blood plasma.
- With erythromycin and cimetidine, an increase in the concentration of Azaleptin in the blood.
- With phenytoin and carbamazepine - there is a decrease in the concentration of Azaleptin in the blood.
Analogues of Azaleptin
Analogues of Azaleptin are Azaleprol, Leponex, Clozapine, Klozasten. Azoleptin is also produced in granules for children.
Prices for Azaleptin
Azaleptin 25mg 50 tablets - from 450r.
Azaleptin 100mg 50 tablets - from 1200r.