Clinical and pharmacological group: & nbsp

Antineoplastic agents - inhibitors of protein kinases

Included in the formulation
  • Genfatinib
    pills inwards 
  • Histamel
    capsules inwards 
    VEROPHARM SA     Russia
  • Gleihib®
    pills inwards 
  • Glivec®
    capsules inwards 
    Novartis Pharma AG     Switzerland
  • Iglib®
    capsules inwards 
  • Imagliv®
    pills inwards 
    Sandoz d.     Slovenia
  • Imatib
    capsules inwards 
  • Imatinib
    pills inwards 
    BIOCAD, CJSC     Russia
  • Imatinib
    pills inwards 
  • Imatinib
    capsules inwards 
  • Imatinib
    pills inwards 
  • Imatinib
    pills inwards 
    JODAS EKSPOIM, LLC     Russia
  • Imatinib Medak
    capsules inwards 
    medac GmbH     Germany
  • Imatinib Forsyte
    capsules inwards 
    Forsythe ZAO     Russia
  • Imatinib-Aktavis
    capsules inwards 
  • Imatinib-Alvogen
    pills inwards 
    Alvogen IPKo S.A.L.     Luxembourg
  • Imatinib-Segardis
    capsules inwards 
    SIGARDIS ENG, LLC     Russia
  • Imatinib-Teva
    capsules inwards 
  • Imatinib-TL
    capsules inwards 
  • Imvek
    capsules inwards 
  • Neopax
    capsules inwards 
    KRKA-RUS, LLC     Russia
  • Filachromin®
    capsules inwards 
    NATIVA, LLC     Russia
  • Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):

    ONLS

    VED

    7 nosologies

    АТХ:

    L.01.X.E.01   Imatinib

    Pharmacodynamics:

    Inhibits protein tyrosine kinase (Bcr-Abl tyrosine kinase), an abnormal enzyme produced by the Philadelphia chromosome in chronic myelogenous leukemia. Induces apoptosis of Bcr-Abl-positive tumor cells of gastrointestinal stromal tumors expressing c-Kit mutations, inhibiting their proliferation. It also inhibits platelet tyrosine kinase receptor and stem cell factor receptors.

    Pharmacokinetics:

    After ingestion, up to 98% is absorbed in the gastrointestinal tract. The maximum concentration in the blood plasma is achieved in 2-4 hours. The connection with plasma proteins is 95%. Penetrates into breast milk.

    Metabolism in the liver with the participation of the enzyme CYP3A4 of the cytochrome P450 system to form the main active metabolite - N-demethylated piperazine derivative.

    The half-life is 6-7 days. Elimination with feces and urine.

    Indications:

    It is used for the treatment of myeloleukemia in the stage of acceleration and blast crisis, it is used in the treatment of inoperable patients with metastatic stromal malignant tumors of the gastrointestinal tract.

    II.C81-C96.C92.1   Chronic myeloid leukemia

    Contraindications:

    Pregnancy and lactation, individual intolerance, children under 2 years old.

    Carefully:

    Hepatic failure, renal insufficiency, chronic heart failure.

    Pregnancy and lactation:

    Recommendations for FDA - category D. Contraindicated in pregnancy and lactation.

    Dosing and Administration:

    Inside 1 time per day in remission: 400 mg, with exacerbation - 600 mg. Depending on the effectiveness and tolerability of the drug, an increase in dose is possible: in remission, up to 600 mg per day, with exacerbation, 800 mg per day in two divided doses.

    The highest daily dose: 800 mg.

    The highest single dose: 400 mg.

    Side effects:

    Central and peripheral nervous system: dizziness, headache, insomnia, fainting, hemorrhagic stroke, peripheral neuropathy, drowsiness, migraine, depression, cognitive disorders, confusion, brain edema, convulsions.

    Respiratory system: shortness of breath, cough, rarely - pneumonitis, respiratory failure, dysphonia, pulmonary edema.

    The system of hematopoiesis: anemia, neutropenia, thrombocytopenia, leukopenia, febrile neutropenia, rarely - lymphopenia, coagulopathy.

    The cardiovascular system: lowering of arterial pressure, ventricular dysfunction, myocardial infarction, supraventricular arrhythmia, thrombosis, rarely - stenocardia, myocardial ischemia, cardiomyopathy, atrial fibrillation, hypovolemic shock, pulmonary embolism, vasculitis, bleeding.

    Digestive system: stomatitis / mucositis, abdominal pain, vomiting, diarrhea, constipation, nausea, gastroesophageal reflux disease, esophagitis, colitis, intestinal obstruction, evacuation of gastric contents, rarely - dysphagia, gastrointestinal bleeding, gastritis.

    Musculoskeletal system: myalgia, arthralgia, muscle weakness, rarely - muscle spasms, trismus.

    Dermatological reactions: alopecia, skin rashes, erythrodysesthesia syndrome fingers and toes, hyperpigmentation of the skin, itching, skin peeling, nail damage, rarely - erythema multiforme.

    Sense organs: conjunctivitis, blurred vision, lacrimation, tinnitus.

    Reproductive system: increase of mammary glands, gynecomastia, pain in the nipples, swelling of the scrotum, decreased potency.

    Allergic reactions.

    Overdose:

    Increased side effects.

    Treatment is symptomatic.

    Interaction:

    Inductors of the P450 CYP3A4 isoenzyme slows the metabolism of imatinib and increases its concentration in the plasma.

    Preparations that induce the isoenzyme CYP3A4 (dexamethasone, carbamazepine, rifabutin, phenytoin, phenobarbital, rifampicin, preparations of St. John's wort perfumed), accelerate the metabolism of imatinib and reduce its concentration in the blood plasma.

    Special instructions:

    People of reproductive age are recommended to use reliable methods of contraception during the intake of imatinib and within 3 months after treatment.

    Patients receiving imatinib treatment are prohibited from driving and working with moving mechanisms.

    Instructions
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