Azaleptol

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Azaleptol: 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. Overdose
8. Special instructions
9. Application during pregnancy and lactation
10. Use in childhood
11. In case of impaired renal function
12. For violations of liver function
13. Use in the elderly
14. Drug interactions
15. Analogs
16. Terms and conditions of storage
17. Terms of dispensing from pharmacies
18. Reviews
19. Price in pharmacies

Latin name: Azaleptol

ATX code: N05AN02

Active ingredient: clozapine (Clozapine)

Producer: PJSC "Technologist" (Ukraine)

Description and photo update: 2019-09-07

Azaleptol is an antipsychotic drug that has neuroleptic, muscle relaxant and sedative effects.

Release form and composition

The drug is available in the form of tablets: round, single-layer, with a flat surface and beveled edges, light yellow with a green tint or light yellow, surface marbling is allowed, the core has a homogeneous structure, tablets at a dose of 100 mg have a separating risk (10 pcs. in blisters, in a cardboard box 5 blisters; 50 pcs. in a container, in a cardboard box 1 container; each pack also contains instructions for the use of Azaleptol).

1 tablet contains:

active substance: clozapine - 25 or 100 mg;
auxiliary components: lactose monohydrate, corn starch, potato starch, magnesium stearate, povidone 25.

Pharmacological properties

Pharmacodynamics

Azaleptol is an antipsychotic drug with the active ingredient clozapine.

The mechanism of action of clozapine is associated with blocking dopamine receptors of the central nervous system (CNS), while it exhibits a high blocking efficiency relative to dopamine D ₄ receptors, and has a weak effect on D ₁ -, D ₂ -, D ₃ - and D ₅ receptors … Along with antidopamine, it has anti-alpha-adrenergic, anticholinergic, antihistaminic activity, inhibits the activation reaction, and exhibits antiserotonergic properties.

Clozapine has no cataleptogenic effect.

Azaleptol exhibits a quick and clinically pronounced sedative effect, has a strong antipsychotic effect, including in patients with productive and negative symptoms of schizophrenia who are resistant to other antipsychotic drugs. With continued therapy for 12 months, clinically significant improvement is observed in about 60% of patients.

In addition, there has been an improvement in some aspects of cognitive dysfunction. In contrast to standard antipsychotics, the use of clozapine significantly reduces the risk of suicidal behavior in schizophrenia or schizoaffective disorders. Rarely, severe extrapyramidal reactions occur, including acute dystonia, akathisia, parkinson-like side effects. The drug practically does not cause an increase in prolactin levels, this avoids the development of gynecomastia, amenorrhea, galactorrhea and impotence. It should be noted that these undesirable effects often occur with the use of standard antipsychotics.

Pharmacokinetics

After oral administration, clozapine is almost completely absorbed (90–95%). Simultaneous food intake does not affect the rate and degree of drug absorption. At the first passage, clozapine undergoes moderate metabolism, its bioavailability is 50-60%.

The maximum concentration (C _max) of clozapine in the blood is reached after about 2.1 hours. Plasma protein binding is up to 95%, the volume of distribution is 1.6 l / kg. It passes into breast milk.

Clozapine is almost completely biotransformed, the pharmacological activity of its main metabolite desmethyl clozapine has a less pronounced and shorter duration of action.

Clozapine excretion is biphasic. The half-life (T _1/2) after a single dose of Azaleptol at a dose of 75 mg is approximately 8 hours. T _1/2 against the background of a daily intake of 75 mg for 7 days increases to 14.2 hours. It is excreted mainly in the form of metabolites: through the kidneys - about 50% of the dose taken, through the intestines - 30%.

The pharmacokinetics of clozapine is linear, with an increase in its dose twice a day from 37.5 mg to 75 mg and 150 mg against the background of equilibrium blood concentration, a dose-dependent increase in AUC (area under the plasma concentration-time curve) and C _max is observed …

The pharmacokinetics of clozapine in case of impaired renal and liver function, diseases of the biliary tract has not been established, therefore, patients with these pathologies should be careful. In severe forms of impaired renal and liver function, diseases of the biliary tract, the drug is contraindicated.

Indications for use

treatment of schizophrenia, resistant to therapy with standard antipsychotics (resistance or tolerance), or in case of individual intolerance to standard antipsychotics associated with the occurrence of such severe uncontrollable neurological side effects as tardive dyskinesia or the development of extrapyramidal symptoms;
therapy of suicidal behavior in patients with schizophrenia or schizoaffective disorder - in order to long-term reduction of the risk of recurrence of suicidal attempts
treatment of psychotic disorders in patients with Parkinson's disease - in cases where the withdrawal of anticholinergic drugs (including tricyclic antidepressants) or a decrease in the dose of dopaminergic antiparkinsonian drugs does not allow to control psychotic symptoms and / or the appearance of a functionally unacceptable increase in the severity of motor symptoms.

Contraindications

Absolute:

a history of clozapine-induced agranulocytosis;
a history of idiosyncratic or toxic granulocytopenia or agranulocytosis (unless the development of granulocytopenia or agranulocytosis is a consequence of previous chemotherapy);
dysfunction of the bone marrow;
drug intoxication, toxic psychoses (including alcoholic psychosis), coma;
epilepsy uncontrollable;
vascular collapse and / or depression of the central nervous system of any etiology;
myocarditis and other severe heart disorders;
severe renal dysfunction;
paralytic ileus;
progressive liver disease;
liver failure;
acute period of liver disease, which is accompanied by nausea, decreased appetite, or jaundice;
concomitant therapy with depot forms of neuroleptics, drugs that can contribute to the appearance of agranulocytosis;
galactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome;
breast-feeding;
childhood;
hypersensitivity to the components of the drug.

In addition, the use of Azaleptol is contraindicated if it is impossible to regularly monitor the patient's blood counts.

You can not use Azaleptol during pregnancy, except in cases of extreme necessity, when the expected effect of therapy for the mother significantly exceeds the potential threat to the fetus.

Azaleptol, instructions for use: method and dosage

Azaleptol tablets are taken orally.

The minimum effective dose should be used, which the doctor selects individually for each patient.

A prerequisite for starting treatment with Azaleptol is that the indicators of the total number of leukocytes and the absolute number of neutrophils correspond to the standardized normal range of values. The total number of leukocytes in the patient's blood should be 3500 per 1 mm ³ and above (or 3.5 x 10 ⁹ / l), the absolute number of neutrophils - 2000 per 1 mm ³ and above (or 2 x 10 ⁹ / l).

Dose adjustment of Azaleptol is necessary when the patient is on concomitant therapy with benzodiazepines, selective serotonin reuptake inhibitors, or other drugs that interact with clozapine.

Recommended dosage of Azaleptol:

schizophrenia, resistant to therapy with standard antipsychotics, risk of recurrence of suicidal attempts: initial dose - 12.5 mg (1/2 tablet in a dose of 25 mg) 1-2 times a day, on the second day - 25 mg 1-2 times a day day. If there is good tolerance, the dose is gradually (over 14–21 days) increased by 25–50 mg per day until a daily dose of 300 mg is reached. If necessary, the achieved dose can be increased by 50-100 mg with an interval of 7 days. The range of therapeutic doses varies, the antipsychotic effect in most patients occurs at a daily dose of 300-450 mg, in some cases a lower daily dose may be adequate, while other patients require a higher (up to 600 mg per day). The daily dose is divided into several doses in unequal doses, the largest of which is taken before bedtime. The maximum daily dose is 900 mg. It should be borne in mind that at doses over 450 mg per day, an increase in adverse reactions is possible. The treatment is continued until the maximum therapeutic effect is reached, then the patient is transferred to a maintenance dose, gradually reducing the previous dose to the minimum effective dose of Azaleptol. If the maintenance dose is no more than 200 mg, then it is advisable to take it once a day, in the evening. The duration of the course of treatment is at least 180 days. When planning to discontinue therapy, it is recommended to gradually reduce the daily dose over 7-14 days. If there is a need for a sharp withdrawal of the drug (including those associated with the development of leukopenia), the patient should be carefully monitored due to the increased risk of exacerbation of psychotic symptoms. Besides,against the background of a sharp withdrawal, the appearance of a headache, increased sweating, nausea, vomiting, diarrhea and other symptoms caused by the cholinergic ricochet effect is possible. If the break in taking Azaleptol was more than two days, then treatment should be resumed with a dose of 12.5 mg 1-2 times a day. Increasing the dose to a therapeutically effective dose when restoring therapy in patients with good tolerance can be carried out more quickly than with the initial use of Azaleptol. Caution should be exercised in patients who, prior to interruption of treatment, had respiratory arrest or cardiac arrest while taking the drug. You can take the first dose of clozapine only a day after the complete cessation of previous therapy with oral antipsychotics;diarrhea and other symptoms due to the cholinergic rebound effect. If the break in taking Azaleptol was more than two days, then treatment should be resumed with a dose of 12.5 mg 1-2 times a day. Increasing the dose to a therapeutically effective dose when restoring therapy in patients with good tolerance can be carried out more quickly than with the initial use of Azaleptol. Caution should be exercised in patients who, prior to interruption of treatment, had respiratory arrest or cardiac arrest while taking the drug. You can take the first dose of clozapine only a day after the complete cessation of previous therapy with oral antipsychotics;diarrhea and other symptoms due to the cholinergic rebound effect. If the break in taking Azaleptol was more than two days, then treatment should be resumed with a dose of 12.5 mg 1-2 times a day. Increasing the dose to a therapeutically effective dose when restoring therapy in patients with good tolerance can be carried out more quickly than with the initial use of Azaleptol. Caution should be exercised in patients who, prior to interruption of treatment, had respiratory arrest or cardiac arrest while taking the drug. You can take the first dose of clozapine only a day after the complete cessation of previous therapy with oral antipsychotics;Increasing the dose to a therapeutically effective dose when restoring therapy in patients with good tolerance can be carried out more quickly than with the initial use of Azaleptol. Caution should be exercised in patients who, prior to interruption of treatment, had respiratory arrest or cardiac arrest while taking the drug. You can take the first dose of clozapine only a day after the complete cessation of previous therapy with oral antipsychotics;Increasing the dose to a therapeutically effective dose when restoring therapy in patients with good tolerance can be carried out more quickly than with the initial use of Azaleptol. Caution should be exercised in patients who, prior to interruption of treatment, had respiratory arrest or cardiac arrest while taking the drug. You can take the first dose of clozapine only a day after the complete cessation of previous therapy with oral antipsychotics;You can take the first dose of clozapine only a day after the complete cessation of previous therapy with oral antipsychotics;You can take the first dose of clozapine only a day after the complete cessation of previous therapy with oral antipsychotics;
psychotic disorders in patients with Parkinson's disease: the initial dose is 12.5 mg per day, once in the evening. Then the dose can be increased by 12.5 mg at intervals of 3-4 days with a maximum allowable increase of 2 times in 7 days to 50 mg. The usual effective dose range is 25 to 37.5 mg per day. If taking Azaleptol at a dose of 50 mg per day for 7 days does not achieve the desired clinical response, you can carefully increase the dose by 12.5 mg once every 7 days. During the dose escalation period (7-14 days), blood pressure (BP) must be carefully monitored. If the patient has excessive sedation, orthostatic hypotension or confusion, then it is necessary to limit the dose increase or stop it. Azaleptol should be taken once in the evening. Exceeding a daily dose of 50 mg is indicated only in exceptional cases. The maximum dose is 100 mg per day. After complete remission of psychotic symptoms for at least 14 days, the dose of the neuroleptic can be increased, provided that the increase is based on motor status. If this leads to a relapse of psychotic symptoms, then the dose of Azaleptol can be increased by 12.5 mg every 7 days to the maximum dose and taken 1 or 2 times a day. It is recommended to stop taking the drug by gradually reducing the dose by 12.5 mg for 14 days. Immediate discontinuation of treatment is indicated when a patient is diagnosed with neutropenia or agranulocytosis. In this case, it is necessary to carefully monitor the patient's mental state. After complete remission of psychotic symptoms for at least 14 days, the dose of the neuroleptic can be increased, provided that the increase is based on motor status. If this leads to a relapse of psychotic symptoms, then the dose of Azaleptol can be increased by 12.5 mg every 7 days to the maximum dose and taken 1 or 2 times a day. It is recommended to stop taking the drug by gradually reducing the dose by 12.5 mg for 14 days. Immediate discontinuation of treatment is indicated when a patient is diagnosed with neutropenia or agranulocytosis. In this case, it is necessary to carefully monitor the patient's mental state. After complete remission of psychotic symptoms for at least 14 days, the dose of the neuroleptic can be increased, provided that the increase is based on motor status. If this leads to a relapse of psychotic symptoms, then the dose of Azaleptol can be increased by 12.5 mg every 7 days to the maximum dose and taken 1 or 2 times a day. It is recommended to stop taking the drug by gradually reducing the dose by 12.5 mg for 14 days. Immediate discontinuation of treatment is indicated when a patient is diagnosed with neutropenia or agranulocytosis. In this case, it is necessary to carefully monitor the patient's mental state.5 mg every 7 days up to the maximum dose and take 1 or 2 times a day. It is recommended to stop taking the drug by gradually reducing the dose by 12.5 mg for 14 days. Immediate discontinuation of treatment is indicated when a patient is diagnosed with neutropenia or agranulocytosis. In this case, it is necessary to carefully monitor the patient's mental state.5 mg every 7 days up to the maximum dose and take 1 or 2 times a day. It is recommended to stop taking the drug by gradually reducing the dose by 12.5 mg for 14 days. Immediate discontinuation of treatment is indicated when a patient is diagnosed with neutropenia or agranulocytosis. In this case, it is necessary to carefully monitor the patient's mental state.

Treatment of elderly patients, patients with a history of seizures, cardiovascular disorders or renal insufficiency is recommended to start with a single dose of 12.5 mg - on the first day and then increase the dose slowly and slightly, in old age - no more than 25 mg per day.

The use of Azaleptol in patients with hepatic insufficiency should be accompanied by regular monitoring of liver function indicators.

Side effects

Azaleptol side effects are classified as follows: very common -> 10%; often -> 1% and 0.1% and 0.01% and <0.1%; very rarely - <0.01%, including isolated cases; frequency not established - there is no possibility to establish the frequency of occurrence of adverse reactions based on the available data:

from the lymphatic system and the blood system: often - a decrease in the total number of leukocytes, leukopenia, neutropenia; infrequently - agranulocytosis; rarely, lymphopenia; very rarely - anemia, thrombocytopenia, thrombocytosis;
from the side of metabolism: very often - an increase in body weight up to 31%; rarely - impaired glucose tolerance, diabetes mellitus; very rarely - severe hyperglycemia, ketoacidosis, hyperosmolar coma, hypercholesterolemia, hypertriglyceridemia; frequency not established - pseudopheochromocytoma;
on the part of the psyche: often - dysarthria; infrequently - dysfemia; rarely - agitated state, anxiety; very rarely - obsessive-compulsive disorder;
from the nervous system: very often - drowsiness, dizziness; often - extrapyramidal symptoms, headache, epileptic seizures, akathisia, convulsions, muscle stiffness, myoclonic twitching, tremor; infrequently - neuroleptic malignant syndrome (including while taking lithium preparations or other centrally acting drugs); rarely - delirium, confusion; very rarely - tardive dyskinesia against the background of concomitant therapy with other neuroleptics; frequency not established - pleurotonus, cholinergic syndrome of changes in electroencephalography;
on the part of the organ of vision: often - blurred vision;
from the heart: very often - tachycardia (more often at the beginning of treatment); often - a change in the electrocardiogram (conduction disturbance, decrease in the ST segment, inversion and smoothing of the T-wave); rarely - arrhythmias, pericarditis (including pericardial effusion), myocarditis (including with eosinophilia), in some cases fatal; very rarely - cardiomyopathy, cardiac arrest; the frequency has not been established - angina pectoris, myocardial infarction (including fatal);
on the part of the vascular system: often - syncope, orthostatic hypotension, arterial hypertension; rarely - thromboembolism (including fatal), organ necrosis (including intestines), arterial hypotension, circulatory collapse, cardiac or respiratory arrest;
from the respiratory system: rarely - aspiration of food when swallowing; very rarely - respiratory depression or respiratory arrest; frequency not established - nasal congestion, bronchospasm, pneumonia, lower respiratory tract infections (including fatal);
from the urinary system: often - urinary retention, urinary incontinence; very rarely - impaired renal function, interstitial nephritis, renal failure; frequency not established - nocturnal enuresis;
from the gastrointestinal tract: very often - constipation, hypersalivation; often - dry mouth, nausea, vomiting, anorexia; rarely, dysphagia; very rarely - stool retention, intestinal obstruction, enlarged salivary gland, paralytic intestinal obstruction; frequency not established - abdominal discomfort, dyspepsia, diarrhea, heartburn, colitis;
from the hepatobiliary system and pancreas: often - increased liver enzymes; rarely - pancreatitis, cholestatic jaundice, hepatitis; very rarely - fulminant liver necrosis; the frequency has not been established - hepatotoxicity, hepatofibrosis, hepatic steatosis, hepatic necrosis, impaired liver function, liver failure (including fatal), liver cirrhosis;
from the reproductive system: very rarely - dysmenorrhea, changes in ejaculation, impotence, priapism; frequency not established - retrograde ejaculation;
on the part of the immune system: the frequency is not established - leukocytoclastic vasculitis, Quincke's edema;
on the part of the musculoskeletal system: the frequency has not been established - weakness and / or muscle spasms, myalgia, systemic lupus erythematosus;
dermatological reactions: very rarely - skin reactions; frequency not established - pigmentation disorder;
laboratory indicators: rarely - an increase in the level of CPK (creatine phosphokinase); very rarely - hyponatremia, pirouette-type ventricular tachycardia, lengthening of the QT interval;
general disorders: often - fatigue, impaired regulation of body temperature and sweating, increased body temperature.

Overdose

Symptoms

Symptoms of an Azaleptol overdose include: pupil dilation, shortness of breath, drowsiness, increased salivation, fluctuations in body temperature, depression or impaired breathing, agitation, areflexia, hallucinations, confusion, delirium, increased reflexes, extrapyramidal symptoms, convulsions, respiratory failure, aspiration pneumonia tachycardia, arterial hypotension, arrhythmia, lethargy, coma, collapse.

It should be borne in mind that taking 400 mg of clozapine in adults who have not previously taken the drug can be life-threatening. In young children, a dose of 50 to 200 mg can cause marked sedation, coma, but without death.

Treatment

Within six hours after the use of Azaleptol, it is necessary to carry out several gastric lavages, followed by the intake of activated carbon, electrocardiography. In the future, the appointment of cardiorespiratory intensive therapy, constant monitoring of the patient's condition, control of acid-base balance and electrolytes is shown.

In the presence of oliguria or anuria, hemodialysis or peritoneal dialysis is performed, but the high degree of clozapine binding to proteins will not significantly increase the rate of drug withdrawal. There is no specific antidote.

In the case of an anticholinergic effect, physostigmine, neostigmine, pyridostigmine are used, for the relief of seizures, diazepam or phenytoin is slowly injected intravenously, for arrhythmia, digitalis, potassium preparations or potassium bicarbonate are prescribed, depending on the symptoms. Do not use quinidine or procainamide. In case of arterial hypotension, an infusion of albumin or plasma substitutes is indicated. The most effective stimulants are dopamine or angiotensin.

It is contraindicated to use long-acting barbiturates, epinephrine and other beta-sympathomimetics, which can increase vasodilation.

The patient's condition should be monitored for 5 days due to a possible delay in the development of reactions.

special instructions

Due to the fact that agranulocytosis and granulocytopenia are among the most dangerous and severe side effects of Azaleptol and can pose a threat to the patient's life, the prescription of the drug should be made in strict accordance with the clinical indications for use.

In order to reduce the incidence of agranulocytosis and the mortality rate associated with its development, treatment should be accompanied by monitoring the number of leukocytes and the absolute number of neutrophils, which starts 1.5 weeks before the start of treatment.

It is recommended to count the total number of leukocytes and the absolute number of neutrophils during the first 18 weeks of treatment once a week, then once every 4 weeks throughout the entire treatment period. These blood counts should be monitored for another 4 weeks after the complete withdrawal of the drug.

During the appointment of Azaleptol, the doctor should inform the patient and those caring for him about the need to immediately contact a medical facility in case of the development of any infectious disease for a blood test with counting the number of leukocytes. You should be aware that flu-like conditions, including fever and sore throat, can be signs of neutropenia.

In case of interruption of a course of therapy that lasted more than 18 weeks for a period of 1/2 to 4 weeks for a reason not related to hematological parameters, weekly monitoring of the number of leukocytes for 6 weeks is indicated additionally. If there are no deviations from the norm, then a blood test can be carried out 1 time in 4 weeks. If the treatment was interrupted for 4 weeks or more, then within 18 weeks after the resumption of taking the pills, it is necessary to conduct a blood test weekly and re-titrate the dose of Azaleptol.

If, during the first 18 weeks of treatment, there is a decrease in the number of leukocytes and the absolute number of neutrophils compared to the standardized normal range of values, then hematological tests should be performed at least 2 times a week.

Repeated determination of the number of leukocytes and leukocyte formula should be carried out in the case of a significant decrease in the number of leukocytes compared to the initial level.

Treatment with Azaleptol should be discontinued immediately if the number of leukocytes in the blood is less than 3000 per 1 mm ³, and the absolute number of neutrophils is less than 1500 per 1 mm ³ after 18 weeks of therapy. The patient should be provided with daily follow-up control of the number of leukocytes and leukocyte blood count, careful observation for the presence of symptoms indicating the development of infection, including flu-like symptoms. The analysis of hematological parameters should be continued until they are completely restored. Resuming the use of the drug in this category of patients is contraindicated.

If, after stopping treatment with Azaleptol, the decrease in the number of leukocytes or the absolute number of neutrophils does not stop, consultation with an experienced hematologist is required.

Potential adverse events include leukocytosis and / or eosinophilia of unknown etiology, especially during the first weeks of therapy.

If the number of eosinophils exceeds 3000 mm ³ (or 3 x 10 ⁹ / l), then the treatment must be suspended or canceled, the resumption of taking Azaleptol is indicated only if the number of eosinophils is below 1000 mm ³ (or 1 x 10 ⁹ / l).

With the development of infection, immediate antibiotic therapy is necessary due to the high risk of septic shock.

Treatment of patients with a history of cardiac pathologies or abnormalities in the cardiovascular system identified during a medical examination should be started after consulting a specialist and conducting electrocardiography. Prescribing Azaleptol to this category of patients is possible if the expected benefit from the use of the drug significantly exceeds the existing risks of developing adverse events.

The likelihood of orthostatic hypotension (including syncope), collapse, cardiac arrest and / or respiratory arrest (including death) increases with a rapid increase in the dose of Azaleptol during the titration period and when combined with benzodiazepine or other psychotropic drugs. In patients with Parkinson's disease, during the first weeks of treatment, it is necessary to monitor blood pressure in the supine and standing positions.

If shortness of breath, tachycardia, accompanied by arrhythmia, symptoms of heart failure, myocardial infarction or influenza occurs, especially during the dose selection period, an immediate diagnosis is required to exclude myocarditis. If myocarditis or cardiomyopathy is suspected, immediate withdrawal of Azaleptol and consultation with a cardiologist are required. In the future, resuming the use of the drug in patients who have undergone clozapine-induced myocarditis or cardiomyopathy is not recommended.

In the first three weeks of treatment, a transient increase in body temperature above 38 ° C is possible, in most cases it is benign, but sometimes due to a change in the number of leukocytes. Therefore, with an increase in the patient's body temperature, the patient should be carefully examined to exclude the development of a possible infection, agranulocytosis or neuroleptic malignant syndrome. If the cause of the high temperature is neuroleptic malignant syndrome, then Azaleptol is stopped immediately.

In order to reduce the risk of thromboembolism, patients are advised to maintain physical activity.

Patients with angle-closure glaucoma and an enlarged prostate gland require careful monitoring of the condition.

The anticholinergic properties of Azaleptol can cause varying degrees of severity of intestinal motility disorders. Therefore, patients with a history of colon disease or surgery in the lower abdomen require special attention. Consideration should be given to the effect of concomitant therapy drugs (including antidepressants, antipsychotics, antiparkinsonian drugs) on the occurrence of constipation and possible deterioration of the condition.

Azaleptol can contribute to the development of metabolic disorders that increase the risk of cardiovascular and cerebrovascular pathologies, hyperglycemia, dyslipidemia, and weight gain. With severe hyperglycemia due to the use of an atypical antipsychotic drug, it is necessary to consider the question of possible withdrawal of the drug.

At the beginning of the use of Azaleptol and periodically during the treatment period, it is recommended to conduct clinical monitoring of changes in the patient's body weight, including the assessment of lipids.

If there is a clinically significant increase in the values of functional liver function tests in patients with impaired liver function or symptoms of jaundice are recorded, taking the tablets should be temporarily discontinued. After hepatic function is restored, treatment can be resumed.

Influence on the ability to drive vehicles and complex mechanisms

During the period of use of Azaleptol, patients are contraindicated to engage in potentially hazardous activities, including driving.

Application during pregnancy and lactation

The use of Azaleptol is contraindicated during breastfeeding.

Taking the drug during pregnancy is allowed only in cases where, in the opinion of the doctor, the expected clinical effect for the mother exceeds the potential threat to the fetus.

If it is necessary to stop taking pills during pregnancy, then the dose of Azaleptol should be reduced very slowly.

For women of reproductive age, it is recommended to use reliable contraception.

Pediatric use

Due to the lack of information on the safety and efficacy of Azaleptol in the treatment of children, the appointment of the drug in this category of patients is contraindicated.

With impaired renal function

It is contraindicated to use Azaleptol tablets for the treatment of patients with severe renal impairment.

For violations of liver function

It is contraindicated to prescribe Azaleptol in case of liver failure, the presence of progressive liver disease, during exacerbations of liver disease, accompanied by decreased appetite, nausea or jaundice.

Use in the elderly

It should be borne in mind that while taking clozapine in patients over the age of 60, especially with a weakened cardiovascular system, the likelihood of orthostatic hypotension and tachycardia increases. In addition, they are more likely to have anticholinergic effects such as urinary retention or constipation.

Drug interactions

monoamine oxidase inhibitors, methadone, narcotic drugs, antihistamines, benzodiazepines, ethanol: they can significantly increase their effect, in some cases their combination with clozapine can be fatal;
psychotropic drugs, including benzodiazepines: special care is required due to the increased risk of developing vascular collapse, sometimes causing cardiac or respiratory arrest;
lithium preparations and other drugs acting on the central nervous system: increase the risk of neuroleptic malignant syndrome;
drugs that have a depressing effect on respiration or have anticholinergic and antihypertensive activity: an additive effect may occur;
norepinephrine and other drugs with a predominant alpha-adrenergic effect: their pressor effect may be weakened;
adrenaline: clozapine eliminates the pressor effect of adrenaline;
antiepileptic drugs, including valproic acid: due to the fact that clozapine is characterized by a decrease in the seizure threshold, it may be necessary to prescribe antiepileptic drugs (especially in patients with a history of epilepsy) or dose adjustment of Azaleptol;
warfarin, digoxin and other substances that bind to plasma proteins to a large extent: an increase in their plasma concentrations is possible due to their displacement from protein complexes in the blood plasma (dose adjustment of substances actively binding to proteins is required);
tricyclic antidepressants, phenothiazines, class 1c antiarrhythmics: an increase in their concentration in blood plasma is possible (a decrease in their dose is required);
cimetidine, erythromycin, azithromycin, fluvoxamine, venlafaxine and other selective serotonin reuptake inhibitors, ciprofloxacin, perazine, oral contraceptives: increase the level of clozapine in blood plasma and the incidence of undesirable effects;
caffeine, ciprofloxacin: the level of clozapine and its main metabolite in blood plasma can increase significantly with daily consumption of coffee and tea or the use of ciprofloxacin in a daily dose of 500 mg;
carbamazepine, rifampicin and other drugs that induce P450 CYP3A4: may lower plasma clozapine levels. This should be taken into account when canceling them after joint therapy;
phenytoin: May cause a decrease in plasma levels of clozapine and a decrease in the effectiveness of a previously effective dose.

When treating with Azaleptol, combinations with drugs that significantly inhibit the function of the bone marrow, depot neuroleptics with long-acting myelosuppressive potential should not be used. It is recommended with caution to prescribe concomitant therapy with drugs that increase the QTc interval or contribute to electrolyte imbalance.

Close monitoring of the level of clozapine concentration in blood plasma is necessary in patients who are simultaneously taking other drugs that have an affinity for cytochrome P450 isoenzymes, including CYP3A4, CYP1A2 or CYP2D6.

It should be borne in mind that the combination of clozapine with protease inhibitors and azole antimycotics can cause clinically significant interactions. In addition, abrupt cessation of smoking in experienced smokers can potentiate an increase in the level of clozapine in blood plasma and cause an increase in the frequency of undesirable effects.

Analogs

Analogs of Azaleptol are: Azaleptin, Azapine, Hedonin, Clozapine, Clozasten, Quetixol, Ketilept, Nantarid, Seroquel, Leponex, etc.

Terms and conditions of storage

Keep out of the reach of children.

Store at temperatures up to 25 ° C.

The shelf life is 3 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Azaleptol

The few reviews about Azaleptol are mostly positive. Most often they are left by caregivers, they report the effectiveness of the drug. In most reviews, the disadvantage of a drug is an impressive list of side effects.

Price for Azaleptol in pharmacies

Due to the lack of the drug in the pharmacy network, the price of Azaleptol has not been established. An analogue of Azaleptin can be purchased for 425-510 rubles. (in a package of 50 tablets of 25 mg) or 1169-1335 rubles. (in a package of 50 tablets of 100 mg).

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!