Decitabine (Decitabinum)

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

Antimetabolites

Antineoplastic agents

Included in the formulation
  • Dacogen
    concentratelyophilizatesolution d / infusion 
    Johnson & Johnson, LLC     Russia
    • Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):

    VED

    ONLS

    АТХ:

    L.01.B.C   Analogs of pyrimidine

    Pharmacodynamics:

    The preparation is an analogue of the natural nucleoside 2'-deoxycytidine, which is an inhibitor of the enzyme responsible for methylation deoxyribonucleic acid, - methyltransferases deoxyribonucleic acid. Thus, the drug, embedded in deoxyribonucleic acid, leads to hypomethylation of tumor cells, inhibits their division and differentiation, which leads to apoptosis.

    Pharmacokinetics:

    With infusion of 100 mg / m2 for 1 hour, the concentration in the plasma during the infusion increases, then decreases biphasic. The connection with plasma proteins is negligible; the half-life of the terminal phase is 30 minutes. The main pathway of metabolism is deamination with cytidine deaminase, present in the liver, in granulocytes, intestinal epithelium, blood plasma. Eliminated by the kidneys in the form of metabolites, slightly - unchanged.

    Indications:

    Myelodysplastic syndrome.

    ICD-10

    II.D37-D48.D46   Myelodysplastic syndromes

    Contraindications:

    Pregnancy and breastfeeding, hypersensitivity.

    Carefully:

    Diseases of the liver and kidneys.

    Pregnancy and lactation:

    Category FDA - Food and Drug Administration (US Food and Drug Administration). Contraindicated in pregnancy and lactation (breastfeeding).

    Decitabine has a teratogenic effect.

    Dosing and Administration:

    The first cycle: the drug is administered intravenously 15 mg / m2 for three hours, repeat every 8 hours, 3 days.

    After 4-6 weeks, the cycles of drug administration are resumed and continue as long as the therapeutic effect remains.

    At the time of taking the drug, blood tests are periodically done and the dose / duration of the cycles is adjusted.

    Side effects:

    On the part of the respiratory organs: pharyngitis, hypoxia, cough, wheezing in the lungs.

    From the nervous system: dizziness, headache, insomnia, hypoesthesia, confusion.

    From the digestive system: diarrhea, vomiting, constipation, nausea, abdominal pain, rash on the mucous membrane of the mouth, dyspepsia, stomatitis, ascites.

    From the cardiovascular system: thrombocytopenia, neutropenia, febrile neutropenia, anemia, and leukopenia.

    From the skin: rash, ecchymosis, erythema, itching, pallor, petechiae, skin lesions, unspecified.

    Other: hyperglycemia, hypomagnesemia, hypoalbuminemia, fever, anorexia, tremor, unspecified pain, lymphadenopathy, cellulitis, lethargy, herpes simplex, pneumonia, hypokalemia, increased blood urea content.

    Overdose:

    Myelosuppression, including prolonged thrombocytopenia and neutropenia. Reversible increase in serum creatinine levels. Treatment is symptomatic.

    Interaction:

    The drug can enhance myelosuppression while taking with other antitumour agents.

    Simultaneous administration with tamoxifen may lead to thrombocytopenia and thromboembolic complications.

    Special instructions:

    During treatment, men and women are recommended to use reliable contraception.

    Before the beginning of the course of the drug, it is necessary to evaluate the function of the liver, as well as to establish the concentration of creatinine in the blood.

    Instructions
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