Gefitinib (Gefitinibum)

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

Antineoplastic agents - inhibitors of protein kinases

Included in the formulation
  • Gefitinib
    pills inwards 
    JODAS EKSPOIM, LLC     Russia
  • Gefitinib-native
    pills inwards 
    NATIVA, LLC     Russia
  • Iressa®
    pills inwards 
    AstraZeneca UK Ltd     United Kingdom
    • Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):

    VED

    ONLS

    АТХ:

    L.01.X.E.02   Gefitinib

    Pharmacodynamics:

    Selective protein tyrosine kinase inhibitor. Irreversibly blocks the receptors of the epidermal growth factor, which leads to the cessation of growth and to regression of the tumor.

    Pharmacokinetics:

    After ingestion, up to 59% is absorbed in the gastrointestinal tract. The maximum concentration in the blood plasma is achieved in 3-7 hours. The connection with plasma proteins is 90%.

    Metabolism in the liver.

    The half-life is 41 hours. Elimination with feces.

    Indications:It is used to treat non-small cell locally advanced or metastatic lung cancer with ineffective chemotherapy with docetaxel and platinum derivatives.

    ICD-10

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

    Contraindications:Hepatic insufficiency, individual intolerance, children under 18 years of age.

    Carefully:Keratitis, interstitial lung disease, cardiovascular failure, hypersensitivity.

    Pregnancy and lactation:

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

    Dosing and Administration:

    Inside, 250 mg once a day, regardless of food intake.

    The highest daily dose: 250 mg.

    The highest single dose: 250 mg.

    Side effects:

    Central and peripheral nervous system: asthenia.

    Hemopoietic system: hypocoagulation.

    Respiratory system: cough, rapid breathing, interstitial pneumonitis.

    Digestive system: anorexia, nausea, diarrhea, rarely - pancreatitis.

    Sense organs: blepharitis, conjunctivitis, corneal erosion.

    urinary system: hematuria, nephropathy, cystitis.

    Dermatological reactions: alopecia, itching, dysplasia of the eyelashes, rarely - toxic epidermal necrolysis.

    Allergic reactions.

    Overdose:

    Increased side effects.

    Treatment is symptomatic.

    Interaction:Inductors of P-glycoprotein (St. John's wort pitted (Hypericum perforatum) and barbiturates) significantly reduce the exposure of gefitinib.

    Special instructions:

    In the treatment it is not recommended to drive vehicles and work with moving mechanisms.

    When used simultaneously with warfarin, continuous monitoring of prothrombin time is required.

    Instructions
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