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Azaleptin
Last reviewed: 03.07.2025
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Indications Azaleptin
The indication for the use of Azaleptin is the treatment of chronic, as well as acute forms of schizophrenic syndrome, manic syndromes, as well as manic-depressive psychoses.
In addition, the drug can be used in case of psychomotor agitation or psychotic conditions that develop as a result of overexcitation.
In some cases, it may be prescribed to patients who are resistant to other neuroleptics.
Release form
Available in tablet form. One glass or polymer bottle with a cap contains 50 tablets. One package contains 1 such bottle.
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Pharmacodynamics
Azaleptin has differences from standard neuroleptic drugs. After taking clozapine, there was no development of catalepsy symptoms, as well as suppression of standard behavior provoked by the introduction of apomorphine or amphetamine into the body.
Azaleptin acts as a weak blocker of D1-3, as well as D5 receptors, and in addition to this, it significantly affects receptors of the D4 type. The active substance of the drug has powerful adrenolytic, cholinolytic, and antihistamine properties, and in addition, it suppresses the activation reaction and has moderate antiserotonergic properties.
In clinical testing conditions, Azaleptin has a rapid and pronounced sedative effect, and in addition, a powerful antipsychotic effect. The latter property of the drug is also observed in patients with schizophrenic syndrome who are resistant to treatment with other drugs. In such cases, the drug acts effectively both in the presence of productive schizophrenic symptoms and in manifestations of loss.
After taking the drug, positive dynamics are described in patients with cognitive disorders. Also, in people suffering from schizophrenia and treated with Azaleptin, the frequency of suicide attempts and suicides is significantly reduced (in comparison with patients not taking the drug). Epidemiological data demonstrate that the frequency of such attempts when using clozapine decreased by >7 times compared to patients not treated with Azaleptin.
The drug has virtually no effect on prolactin levels and is generally well tolerated. The use of clozapine has only occasionally led to the development of severe side effects in patients.
Pharmacokinetics
Azaleptin is rapidly absorbed from the intestine. The active substance reaches its maximum concentration after 2.5 hours. Equilibrium concentrations in blood plasma are established by the 8th-10th day of treatment. The bioavailability of clozapine is approximately 27-60%. Its accumulation occurs within the parenchymatous organs (in the lungs, as well as the kidneys and liver). About 95% of the active ingredient is synthesized with protein within the plasma.
Clozapine is metabolized in the liver, producing low-activity or inactive breakdown products.
Excretion is mainly through the kidneys, about 35% is excreted with bile. The half-life lasts within 4-12 hours after a single dose of the drug (75 mg) or 4-66 hours in the case of taking the drug in a dosage of 100 mg 2 times a day.
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Dosing and administration
Azaleptin is taken orally. It is usually taken after meals. The daily dosage is usually divided into 2-3 doses. For maintenance treatment in the amount of no more than 50 mg of the drug, the daily dose is prescribed as a single dose (in the evening). The duration of the treatment course, as well as the dosage, are determined exclusively by the doctor.
For adults, the drug is usually prescribed in a single dose of 50-200 mg. The dose is selected individually, and starts with 25-100 mg, with a gradual increase in the amount until the desired medicinal effect is achieved. The dosage is usually increased over 1-2 weeks (by 25-50 mg per day).
It is allowed to take no more than 600 mg of the medicine per day.
Once the patient's health improves, it is necessary to switch to maintenance doses. On average, the maintenance dose per day is 150-200 mg. Sometimes this figure may be lower - 25-100 mg of the drug.
Patients with a mild form of the pathology, as well as elderly people or people with insufficient weight, as well as in the case of disorders in the functioning of the heart or kidneys and cerebrovascular pathologies - should not be prescribed more than 200 mg per day.
It is necessary to stop taking the medication by gradually reducing the dosage.
Use Azaleptin during pregnancy
Azaleptin is prohibited to be prescribed during pregnancy. When treating with clozapine, women of reproductive age must use reliable contraception.
It is not recommended to take the medicine during the lactation period. It can be prescribed only after consultation with the attending physician, as well as after the cessation of breastfeeding.
Contraindications
Among the main contraindications:
- the medicine is prohibited for patients with hypersensitivity to the active substance or auxiliary elements of the drug;
- should not be used in the treatment of patients with a history of possible changes in blood counts (especially when they are associated with the use of neuroleptic drugs or tricyclics);
- It is prohibited to use it in the treatment of patients suffering from toxic psychoses (including alcoholic ones), severe cardiovascular pathologies (as well as with symptoms of heart failure and circulatory disorders), myasthenia, and in addition, liver or kidney pathologies with dysfunctions in these organs;
- It is contraindicated to take Azaleptin in the presence of epilepsy, glaucoma, prostatic hypertrophy, and also intestinal atony or infections;
- The medicine is also prohibited for use in children.
During treatment with Azaleptin, it is prohibited to drive a car or operate equipment that may pose a potential danger to life and health.
Side effects Azaleptin
In general, patients tolerate Azaleptin well. However, if the drug is taken in a daily dose of more than 450 mg, the likelihood of side effects increases.
Possible side effects include:
- organs of the hematopoietic system: development of eosinophilia, granulocytopenia and leukocytosis of unknown origin. In addition, agranulocytosis may develop, which can be prevented by constant monitoring of blood counts (during the first 18 weeks of treatment - every day, and then at long intervals). If agranulocytosis is detected in the patient, it is necessary to stop taking the drug and transfer him to intensive therapy;
- organs of the nervous system: the appearance of headaches or dizziness, a feeling of drowsiness or severe fatigue, extrapyramidal disorders (usually expressed weakly) or disorders of thermoregulation, accommodation, and sweating. In addition, ptyalism or hyperthermia. The appearance of tremor of the limbs, akathisia, rigidity, and in addition to this, a malignant form of neuroleptic syndrome is observed sporadically;
- digestive system organs: the appearance of vomiting or bowel disorders, as well as the development of dry mucous membranes inside the oral cavity. In addition, the development of cholestasis or an increase in the activity of liver transaminases;
- cardiovascular system: development of tachycardia or orthostatic collapse, as well as increased blood pressure or loss of consciousness. In isolated cases, patients develop collapse with respiratory failure, myocarditis, arrhythmia, and changes in ECG parameters;
- Others: urinary retention or, on the contrary, urinary incontinence, development of skin allergies. Sudden death of a patient was observed in isolated cases. Long-term use of the drug may cause weight gain.
Overdose
In case of using Azaleptin in large doses, patients may experience confusion, a state of excitement or drowsiness, development of areflexia or, on the contrary, increased reflexes. In addition, hallucinations or convulsions may appear, tachycardia, mydriasis may develop, temperature may change, blood pressure may decrease, conductivity within the myocardium or heart rhythm may be disrupted. Ptyalism and deterioration of visual acuity may also be observed. In the most severe cases, problems with respiratory processes developed, and in addition, collapse with a comatose state.
There is no specific antidote to eliminate symptoms. In case of overdose, it is necessary to quickly perform gastric lavage and give the patient enterosorbents. It is also necessary to monitor the cardiovascular and respiratory systems. The doctor may prescribe symptomatic therapy.
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Interactions with other drugs
Azaleptin is prohibited to be prescribed to patients being treated with drugs that have a depressing effect on bone marrow function.
The drug cannot be combined with NSAIDs, as well as pyrazolone derivatives, antithyroid and antimalarial drugs, and gold products.
Azaleptin should be taken with caution in combination with antipsychotics, antidepressants, antimicrobial drugs and anticonvulsants, as well as with sulfonylurea derivatives and antidiabetic agents.
When the active ingredient is combined with MAO inhibitors, benzodiazepines, anesthetics, ethanol, antihistamines, and other CNS depressants, the central effect of these drugs is enhanced. Azaleptin should be used with particular caution by people taking (or who have recently taken) benzodiazepines or other psychotropic drugs, because in this case the possibility of developing collapse increases (in this case, respiratory depression may begin and cardiac arrest may occur).
Antihypertensive and anticholinergic drugs, as well as drugs that suppress respiratory function, should be combined with clozapine with caution.
As a result of combining Azaleptin with drugs that significantly bind to plasma proteins, the risk of side effects may increase (due to the displacement of elements from the plasma protein bond, as well as an increase in the plasma concentration of the unbound component).
In combination with drugs that are metabolized mainly through hemoproteins P450 1A2, as well as P450 2D6, the concentration of the active component of Azaleptin in plasma may increase. Tests have not shown an increase in the medicinal effect of clozapine due to the combination with tricyclics, phenothiazines, and antiarrhythmic drugs of category IC (metabolized with the participation of hemoprotein P450 2D6). It is possible that under the influence of clozapine, the concentration of these drugs in plasma increases, therefore, when combining them, it is necessary to monitor the patient's condition and adjust the dosage of phenothiazines and other drugs that are metabolized through hemoprotein P450 2D6, if necessary.
Azaleptin weakens the medicinal effect of levodopa, as well as other dopamine stimulants.
Cimetidine with erythromycin, as well as drugs that suppress serotonin reuptake processes (such as paroxetine and fluvoxamine), when combined with Azaleptin, increase the levels of the latter's active substance in plasma.
In combination with hemoprotein P450 inducers (for example, carbamazepine), the concentration of clozapine in plasma decreases and its medicinal effect is weakened.
As a result of combining Azaleptin with lithium drugs, the risk of developing a malignant form of neuroleptic syndrome increases.
The active substance Azaleptin reduces the severity of the hypertensive effect of norepinephrine, as well as other drugs that have predominantly adrenergic properties, and in addition, significantly reduces the pressor effect of the substance adrenaline.
The absorption of the drug from the intestine is slowed down when combined with gel-like antacids, as well as cholestyramine.
Storage conditions
Azaleptin should be kept in conditions acceptable for most drugs - a dry place, protected from the sun, inaccessible to children. The temperature should remain within 15-30 degrees.
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Shelf life
Azaleptin can be used for a maximum of 3 years after the release of the drug.
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Attention!
To simplify the perception of information, this instruction for use of the drug "Azaleptin" translated and presented in a special form on the basis of the official instructions for medical use of the drug. Before use read the annotation that came directly to medicines.
Description provided for informational purposes and is not a guide to self-healing. The need for this drug, the purpose of the treatment regimen, methods and dose of the drug is determined solely by the attending physician. Self-medication is dangerous for your health.