Azaleptin
Azaleptin: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Special instructions
- 8. Application during pregnancy and lactation
- 9. Use in childhood
- 10. In case of impaired renal function
- 11. For violations of liver function
- 12. Drug interactions
- 13. Analogs
- 14. Terms and conditions of storage
- 15. Terms of dispensing from pharmacies
- 16. Reviews
- 17. Price in pharmacies
Latin name: Azaleptin
ATX code: N05AH02
Active ingredient: clozapine (Clozapine)
Producer: Organika, JSC (Russia)
Description and photo updated: 28.08.
Prices in pharmacies: from 436 rubles.
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Azaleptin is a drug of the group of antipsychotics. Refers to neuroleptics, has sedative properties. Promotes muscle relaxation, enhances the effect of painkillers and hypnotics. It has a peripheral and central anticholinergic effect.
Release form and composition
The drug is available in the form of tablets: flat-cylindrical, greenish-yellow (10 pcs. In blisters and 50 pcs. In dark glass / polymer jars, in a cardboard box 5 packs or 1 can and instructions for the use of Azaleptin).
Composition of 1 tablet:
- active substance: clozapine (azaleptin) - 25 mg or 100 mg;
- excipients: potato starch, calcium stearate, lactose monohydrate (milk sugar).
Pharmacological properties
Pharmacodynamics
Azaleptin is an antipsychotic agent (neuroleptic) that practically does not lead to the development of extrapyramidal disorders. It enhances the action of analgesic and hypnotics.
The main types of pharmacological effectiveness of the drug and the mechanisms of action that determine them:
- Antipsychotic: associated with blockade of dopamine D 2 -receptors of the mesocortical and mesolimbic systems;
- Antiemetic: based on the blockade of dopamine D 2 -receptors of the trigger zone of the vomiting center;
- Sedative: due to blockade of adrenergic receptors of the reticular formation of the brain stem;
- Hypothermic: associated with blockade of dopamine receptors in the hypothalamus.
Clozapine also has a peripheral and central m-anticholinergic, α-adrenergic blocking effect. It does not affect the concentration of prolactin in the blood.
The antipsychotic effect of the drug is close to that of aliphatic phenothiazines, while the development of a submelancholic shade and unpleasant subjective sensations is not noted. Reduces the threshold of convulsive readiness. It has no cataleptogenic effect. It does not influence the higher intellectual functions, practically does not lead to the development of extrapyramidal disorders.
Pharmacokinetics
Clozapine is well absorbed from the gastrointestinal tract. Its bioavailability is in the range of 27-60%. The time to reach the maximum concentration of the substance in the blood is 2.5 hours (from 1 to 6 hours). Average stable equilibrium concentrations - 319 ng / ml (from 102 to 771 ng / ml), they are reached in 8-10 days. Binds to blood plasma proteins at a level of 95%.
In the body, clozapine is distributed quickly, the accumulation of the substance is noted in the parenchymal organs - in the lungs, liver, kidneys.
Clozapine metabolism occurs in the liver by the CYH1A2 enzyme system, the metabolites are inactive or have weak activity, and are excreted by the kidneys and bile (50 and 35%, respectively). The half-life has high variability: after taking a single dose of 75 mg - 8 hours (from 4 to 12 hours); after taking 2 times a day, 100 mg - 12 hours (from 4 to 66 hours).
Indications for use
Azaleptin is used for the following diseases:
- Acute and chronic form of schizophrenia;
- Manic states (classic and atypical mania, unproductive delusions);
- Affective insanity;
- Mental and motor excitement.
Contraindications
- Granulocytopenia;
- History of agranulocytosis;
- Coma;
- Myasthenia gravis;
- Violation of bone marrow hematopoiesis;
- Pregnancy;
- Lactation;
- Hypersensitivity to the drug;
- Children under 5 years of age.
When prescribing Azaleptin, care must be taken in patients with angle-closure glaucoma, decompensated diseases of the cardiovascular system, severe hepatic / renal failure, prostatic hyperplasia, epilepsy, intercurrent diseases with febrile syndrome, intestinal atony.
Azaleptin, instructions for use: method and dosage
A single dose of the drug for adults is from 50 mg to 200 mg, the daily dose is from 200 mg to 400 mg. In most cases, treatment begins with 25-50 mg, gradually increasing the dosage to 200 or 300 mg per day.
Azaleptin tablets should be taken after meals 2-3 times a day. In some cases, it is possible to prescribe a daily dose in one dose before bedtime. The maximum permissible oral dose is 600 mg.
The course of treatment is 1-2 weeks, depending on the severity and form of the disease.
For sleep disorders, the drug is prescribed in small quantities (no more than 50 mg).
Side effects
The drug is well tolerated due to its central anticholinergic action and moderate effect on dopamine receptors. But in some cases, Azaleptin tablets can cause the following side effects from the side:
- Central nervous system: headache, drowsiness, less often - confusion, insomnia, depression, extrapyramidal disorders, epilepsy;
- Cardiovascular system: lowering blood pressure, orthostatic hypotension with dizziness, tachycardia, sometimes - arterial hypertension;
- Gastrointestinal tract: increased salivation, vomiting, nausea, heartburn, dry mouth, constipation;
- Metabolism: increased sweating, weight gain;
- Circulatory system: granulocytopenia, eosinophilia, thrombocytopenia, leukopenia;
- Other systems: violation of accommodation, problems with urination, decreased potency, myasthenia gravis.
Overdose
An overdose of Azaleptin may be accompanied by respiratory depression, drowsiness, anxiety, epileptic seizures, tachycardia, hypotension, collapse, coma. Overdose treatment includes the appointment of sorbents, maintenance of heart and respiratory function, symptomatic therapy. Hemodialysis or peritoneal dialysis in case of poisoning does not give the desired effect.
special instructions
The development of granulocytopenia requires immediate discontinuation of the drug.
During the use of this drug, the use of alcoholic beverages should be excluded.
Influence on the ability to drive vehicles and complex mechanisms
During the period of treatment, care must be taken when driving vehicles and working with complex mechanisms that require increased concentration of attention.
Application during pregnancy and lactation
Azaleptin is contraindicated during pregnancy / lactation.
Pediatric use
Azaleptin is not prescribed for patients under 5 years of age.
With impaired renal function
In severe renal failure, Azaleptin should be used under medical supervision.
For violations of liver function
In severe hepatic impairment, Azaleptin should be used under medical supervision.
Drug interactions
- Tricyclic antidepressants, antipsychotic drugs, drugs that damage blood cells (pyrazolone-containing, non-steroidal anti-inflammatory drugs), antidepressants, carbamazepine, gold drugs, thyreostatics and antimalarial drugs: combined use is contraindicated;
- Antiepileptic drugs, anticoagulants, antimicrobial and hypoglycemic drugs (sulfonylurea derivatives): combined use requires caution;
- Preparations with hypnotics, hypotensive and sedative effects, agents for general anesthesia, narcotic analgesics, monoamine oxidase inhibitors, ethanol: their effect is enhanced;
- Gel antacids, cholestyramine: absorption of clozapine from the intestine is impaired;
- Levodopa and other stimulants of dopamine release: their effect is weakened;
- Benzodiazepines: impaired consciousness, excessive lowering of blood pressure, depression / cessation of breathing may occur;
- Lithium preparations: their neurotoxicity increases (manifests itself in the form of delirium, seizures, extrapyramidal disorders);
- Pentetrazole: the risk of seizures increases;
- Myelotoxic drugs: the manifestations of Azaleptin's hematotoxicity are enhanced.
Analogs
Azaleptin analogs are: Azaleprol, Clozapine, Clozapine-Pharmaplant, Clozasten, Leponex.
Storage conditions and periods
The drug should be stored in a dry place protected from exposure to sunlight at a temperature not exceeding 30 ° C.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Azaleptin
In many reviews of Azaleptin, the drug is evaluated positively. Patients indicate that it is good for insomnia.
However, there is a significant number of responses about poor drug tolerance. Concomitant side effects are described, which are most often manifested in the form of addiction, weight gain, weakness, slurred speech, a feeling of fatigue, dullness of memory, and sleep disturbance after discontinuation of therapy.
Price for Azaleptin in pharmacies
The approximate price of Azaleptin per pack of 50 tablets: in a dosage of 25 mg - 389-1350 rubles, in a dosage of 100 mg - 1122-1618 rubles.
Azaleptin: prices in online pharmacies
|
Drug name Price Pharmacy |
|
Azaleptin 25 mg tablets 50 pcs. 436 r Buy |
|
Azaleptin 100 mg tablets 50 pcs. 1289 RUB Buy |
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
