Azaleptin® (Azaleptin®)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceClozapineClozapine
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    • Dosage form: & nbsppills
    Composition:

    1 tablet contains:

    active substance: clozapine (azaleptin) 25 mg or 100 mg;

    Excipients: lactose monohydrate (sugar milk) 0.1010 g and 0.1100 g, potato starch 0.0225 g and 0.0375 g, calcium stearate 0.0015 g and 0.0025 g.

    Description:

    Ploskotsilindricheskie tablets of a greenish-yellow color.

    Pharmacotherapeutic group:Antipsychotic agent (antipsychotic)
    ATX: & nbsp

    N.05.A.H.02   Clozapine

    Pharmacodynamics:

    Antipsychotic agent (neuroleptic), almost does not cause extrapyramidal disorders, increases the effect of hypnotic and analgesic drugs (LS). The antipsychotic effect is due to the blockade of dopamine D2-receptors of the mesolimbic and mesocortical system. Sedative action is due to blockade of adrenoreceptors of the reticular formation of the brainstem; antiemetic effect - blockade of dopamine D2receptors of the trigger zone of the vomiting center; hypothermic action - blockade of dopamine receptors of the hypothalamus.Has peripheral and central m-holinoblokiruyuschee, alpha-adrenergic blocking action. Does not affect the concentration of prolactin in the blood.

    Antipsychotic action is close to that of aliphatic phenothiazines, but without a "sub-melancholic shade" and unpleasant subjective sensations, does not have a cataleptogenic effect, reduces the threshold of convulsive readiness.

    Does not affect the higher intellectual functions, practically does not cause extrapyramidal disorders.

    Pharmacokinetics:

    Well absorbed from the digestive tract. Bioavailability - 27-60%. The maximum concentration in the blood is determined after 2.5 hours (1-6 hours), stable equilibrium concentrations - after 8-10 days and averaged 319 ng / ml (102-771 ng / ml). Relationship with blood plasma proteins 95%. Biological availability is 27-60%. Clozapine quickly distributed in the body and accumulates in the parenchymal organs (lungs, liver, kidneys).

    Metabolized in the liver by an enzyme system CYH1A2, metabolites have little or no activity, are excreted by the kidneys (50%) and bile (35%). Half-life from the body is subject to large fluctuations, after taking a single dose of 75 mg - 8 hours (from 4-12 hours); at reception of 100 mg 2 times a day -12 h (4-66 h).

    Indications:

    Acute and chronic forms of schizophrenia, especially those resistant to therapy with other antipsychotic drugs (neuroleptics) and / or intolerance of their side effects.

    Psychotic disorders in children older than 5 years and adolescents of different etiologies.

    Contraindications:

    - Hypersensitivity to azaleptin or any other components of the drug;

    - granulocytopenia or agranulocytosis in the anamnesis (with the exception of the development of granulocytopenia or agranulocytosis due to previously used chemotherapy);

    - a violation of bone marrow function;

    - alcoholic or other toxic psychosis, drug intoxication, coma;

    - pregnancy and lactation;

    - children's age (up to 5 years).

    Carefully:Decompensated diseases of the cardiovascular system, severe hepatic or renal insufficiency, closed angle glaucoma, prostatic hyperplasia, intestinal atony, epilepsy, intercurrent diseases with febrile syndrome.
    Dosing and Administration:

    Inside, after eating, squeezed a small amount of liquid, 2-3 times a day.

    Single dose for adults 50-200 mg, the initial daily dose is 150-300 mg, the average daily dose is 200-400 mg. The highest daily dose is 600 mg. The dose is selected individually, starting with the appointment of small doses (25 mg) and gradually increasing them by 25-50 mg per day until the therapeutic effect is obtained.

    For mild forms of the disease for maintenance therapy, as well as in patients with hepatic or renal insufficiency, chronic heart failure, with cerebrovascular disorders are prescribed at lower daily doses (20-200 mg).

    It is necessary to take into account the stage-by-stage manifestation of the therapeutic effect: the rapid onset of hypnotic and sedative action; relief of anxiety, psychomotor agitation and aggressiveness (after 3-6 days); antipsychopathic effect (after 1-2 weeks); effect on the symptoms of negativity (after 20-40 days). After reaching a therapeutic effect, they switch to a supportive course.

    Side effects:

    In the first weeks of treatment, azaleptin can cause such changes in the blood picture as granulocytopia, up to agranulocytosis (see below). The appearance of symptoms resembling influenza, a tremendous chill,fever, sore throat, inflammation of the gums and mucous membranes of the mouth, flaccid wounds, boils, exacerbation of chronic or latent foci of infection (tonsillitis, periostitis, etc.) may be a manifestation of the first signs of agranulocytosis.

    From the central nervous system: dizziness, drowsiness, headache, increased central temperature, fainting, akathisia, confusion; rarely: extrapyramidal disorders (akinesia or hypokinesia, muscle rigidity, tremor), insomnia, sleep disturbances, depression, malignant neuroleptic syndrome (seizures, shortness of breath or tachypnea, tachycardia or arrhythmia, fever, unstable blood pressure, increased sweating, involuntary urination , severe muscle stiffness, pallor of the skin, excessive fatigue or weakness), convulsive attacks, late dyskinesia.

    From the genitourinary and urinary system: retention of urine, decreased potency.

    From the side of metabolism: weight gain.

    From the side of the musculoskeletal system: myasthenia gravis.

    From the digestive system: hypersalivation, nausea, vomiting, heartburn, dry mouth.

    On the part of the organs of hematopoiesis: granulocytopenia, up to agranulocytosis (the first signs of agranulocytosis may be symptoms resembling the flu: chills, fever, sore throat, inflammation of the gums and mucous membranes of the oral cavity, slow-healing wounds, furunculosis, exacerbation of chronic or latent foci of infection - tonsillitis, periostitis, pyoderma), leukopenia, thrombocytopenia.

    From the sense organs: violation of accommodation.

    From the side of the cardiovascular system: decrease in blood pressure (including orthostatic hypotension); less often - increased blood pressure, tachycardia, flattening of the T wave on the ECG.

    Other: increased sweating.

    Overdose:

    Symptoms: depression of consciousness of varying severity, anxiety, delirious disorders, development of large epileptic seizures, thermolability, hypothermia, tachycardia, arterial hypotension, heart rhythm disturbances, collapse, intestinal atony, respiratory depression.

    Treatment: gastric lavage with the appointment of sorbents, maintenance of respiratory function and cardiovascular system, control of electrolyte balance and acid-base state; symptomatic treatment.

    For 4 days after the disappearance of the symptoms of poisoning, the patient is monitored because of possible late complications.

    Peritoneal dialysis or hemodialysis ineffective.

    Interaction:

    Increases the effect of sedative and hypnotic drugs, drugs for general anesthesia, narcotic analgesics, monoamine oxidase inhibitors, hypotensive drugs, ethanol.

    Weaken the effect of levodopa and other dopaminimulants.

    Absorption from the intestine worsens with the use of gel-like antacids and colestyramine.

    In combination with benzodiazepines, excessive lowering of blood pressure, impaired consciousness, depression or respiratory arrest may occur.

    Simultaneous administration of drugs Li+ increases neurotoxicity (delirium, seizures, extrapyramidal disorders).

    Pentetrazole increases the risk of seizures.

    Do not use together with tricyclic antidepressants, antipsychotic drugs, drugs that damage blood cells (pyrazolone-containing, non-steroidal anti-inflammatory drugs), antidepressants, carbamazepine, gold preparations, thyreostatics and antimalarial drugs.

    Care should be taken when co-prescribing antiepileptic drugs, anticoagulants, antimicrobial and hypoglycemic drugs (sulfonylurea derivatives).

    Myelotoxic drugs increase the manifestation of hematotoxicity of the drug.

    Special instructions:

    When the phenomena of granulocytopenia develop, treatment should be stopped immediately.

    To eliminate arterial hypotension, which develops with clozapine, only angiotensin or norepinephrine derivatives can be used, but not epinephrine (adrenaline) (the perverse effect of adrenaline).

    When taking clozapine, you should refrain from using ethanol.

    Initially, weekly, and then every 3-4 months, it is necessary to monitor the blood picture.

    Clozapine should be used only under the supervision of a doctor, subject to the following conditions: the content of leukocytes in the peripheral blood is within the norm (number of white blood cells> 3500 / mm3, the hemogram is within the norm); if the total number of leukocytes decreases to a level of 3.0 x 109/ l or the amount of granulocytes below the level of 1.5 x 109/ l, treatment with azaleptin should be interrupted.

    PIn serious changes in the blood picture, all drugs and substances potentially depressing the hematopoietic system.
    Effect on the ability to drive transp. cf. and fur:

    During the treatment period, care must be taken when driving vehicles and engaging in other potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

    Form release / dosage:

    Tablets, 25 mg and 100 mg.

    Packaging:

    5 packages of cellular contour for 10 tablets or 50 tablets in cans of light-protective glass or polymeric, together with instructions for medical use in a cardboard bundle.

    Storage conditions:

    In the dark place at a temperature of not more than 30 FROM.

    Shelf life:

    5 years.

    Do not use after the expiration date stated on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:P N002649 / 01
    Date of registration:26.05.2008/04.10.2016
    Expiration Date:Unlimited
    The owner of the registration certificate:ORGANICS, JSC ORGANICS, JSC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp04.02.2017
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