Idarubicin (Idarubicinum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

Antineoplastic antibiotics

Included in the formulation
  • Zavedos®
    capsules inwards 
       
  • Idarubicin
    solution in / in 
    FARM STANDART, OJSC     Russia
  • Rubid
    lyophilizate in / in 
    LENS-PHARM, LLC     Russia
    • Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):

    VED

    АТХ:

    L.01.D.B.06   Idarubicin

    Pharmacodynamics:

    Inhibits topoisomerase II, disrupting the synthesis of nucleic acids, has a high rate of penetration into cells due to pronounced lipophilicity. It is embedded in DNA, violating its synthesis.

    Pharmacokinetics:

    After oral administration, up to 39% is absorbed in the gastrointestinal tract. The maximum concentration in the blood plasma is achieved after 3 hours. After intravenous administration penetrates into the nucleated cells of blood and bone marrow.

    The connection with plasma proteins is 97%.

    Metabolism in the liver under the action of ketoreductase to the active metabolite of idarubicinol.

    The half-life is 4-46 hours. Elimination by kidneys in the form of idarubicinol.

    Indications:

    It is used for the treatment of acute non-lymphoblastic and lymphoblastic leukemia, myeloblastic leukemia. It is used as part of complex therapy for lung and breast cancer.

    ICD-10

    II.C30-C39.C34   Malignant neoplasm of bronchi and lungs

    II.C50.C50   Malignant neoplasm of breast

    II.C81-C96.C91.0   Acute lymphoblastic leukemia

    II.C81-C96.C92   Myeloid leukemia [myeloid leukemia]

    II.C81-C96.C94.7   Other specified leukemia

    Contraindications:

    Severe cardiac, hepatic and renal insufficiency, expressed myelosuppression, heart failure, acute and recently transferred myocardial infarction, individual intolerance.

    Carefully:

    Myocarditis, thrombocytopenia, leukopenia, gout, chicken pox, shingles.

    Pregnancy and lactation:

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

    Dosing and Administration:

    Use in children

    In acute lymphoblastic leukemia: 10 mg / m2 daily for 3 days.

    Adults

    Intravenously sprayed (slowly) for 10-15 minutes at 12 mg / m2 daily for 3 days.

    Inside with breast cancer: capsules at a rate of 45 mg / m2 the surface of the body for one day.

    The highest daily dose: 45 mg / m2.

    The highest single dose: 45 mg / m2.

    Side effects:

    Central and peripheral nervous system: fatigue, dizziness, aphasia, convulsions.

    The system of hematopoiesis: anemia, thrombocytopenia, and leukopenia.

    Respiratory system: cough, rapid breathing, interstitial pneumonitis.

    The cardiovascular system: phlebitis, thrombophlebitis, tachycardia, bradycardia, atrioventricular blockade, cardiomyopathy, myocarditis, pericarditis.

    Digestive system: ulcerative stomatitis, anorexia, nausea, rarely - melena, diarrhea, pancreatitis, fatty degeneration of the liver.

    Musculoskeletal system: arthralgia, myalgia.

    Urinary system: nephropathy, cystitis.

    Reproductive system: oligospermia, decreased libido, menstrual irregularities, impotence.

    Dermatological reactions: alopecia, itching.

    Allergic reactions.

    Overdose:

    Arrhythmia, cardiotoxic shock.

    Treatment is symptomatic. Hemotransfusion, dialysis is ineffective.

    Interaction:

    Incompatible with alkaline solutions, as when mixing is the destruction of idarubicin.

    When mixed with heparin idarubicin precipitates.

    Simultaneous use with uricosuric drugs increases the risk of developing nephropathy.

    Special instructions:

    Treatment with idarubicin is carried out under the supervision of a doctor who has experience of antitumor therapy. Monitoring of liver and kidney functions, blood tests.

    Instructions
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