Afatinib (Afatinibum)

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

Antineoplastic agents - inhibitors of protein kinases

Included in the formulation
  • Giotrif®
    pills inwards 
    Boehringer Ingelheim International GmbH     Germany
    • АТХ:

    L.01.X.E   Protein kinase inhibitors

    L.01.X.E.13   Afatinib

    Pharmacodynamics:

    Selective tyrosine kinase inhibitor (epidermal growth factor receptor with mutation). Irreversibly blocks the receptors of the epidermal growth factor, which leads to the cessation of growth and to regression of the tumor.

    Pharmacokinetics:

    After oral administration, the maximum concentration of the drug is achieved in 3-5 hours. It binds to blood plasma proteins in 95%.

    Half-Elimination (half-life) of the drug is 37 hours. Elimination with feces (85.4%) and with urine (4.3%).

    Indications:

    It is used as a monotherapy for the treatment of metastatic non-small cell lung cancer with the mutation of the epidermal growth factor receptor (EGFR).

    ICD-10

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

    Contraindications:

    Liver failure.

    Individual intolerance.

    Carefully:

    Keratitis, interstitial lung disease, cardiovascular failure.

    Pregnancy and lactation:Pregnancy and lactation: recommendations for Food and Drug Administration (US Food and Drug Administration) - Category D. Not applicable to pregnant and lactating women.
    Dosing and Administration:

    It is ingested 40 mg once a day.

    The highest daily dose: 50 mg.

    The highest single dose: 50 mg.

    Treatment stops when the disease progresses or displays high toxicity of the drug.

    Side effects:

    Central and peripheral nervous system: rapid fatigue, general weakness, violation of taste sensitivity.

    Hematopoietic system: anemia, leukopenia.

    Cardiovascular system: development of cardiovascular insufficiency.

    Respiratory system: rhinorrhea, nosebleeds, dyspnea, cough, distress syndrome.

    Organs of the senses: conjunctivitis, "dry eye syndrome".

    Musculoskeletal system: back pain, muscle spasms.

    Digestive system: diarrhea.

    Skin: rash, acne, dry skin, abnormal nail changes.

    Metabolism: decreased appetite, weight loss, dehydration.

    Allergic reactions.

    Overdose:

    Not described.

    Treatment is symptomatic.

    Interaction:

    Application immediately after meals significantly reduces the exposure of the drug - up to 50%. It is recommended that apathinib on an empty stomach.

    P-glycoprotein inducers: Hypericum perforatum (Hypericum perforatum) and barbiturates significantly reduce the exposure of apatinib
    Special instructions:

    Monitoring of the functional activity of the liver.

    Taking the drug is recommended to combine with the prevention of diarrhea, especially in the first 6 weeks of therapy. With the onset of diarrhea, treatment is immediately performed until the liquid stool is absent for 12 hours. In severe cases, apathinib treatment is interrupted prior to normalization of the stool.

    Instructions
    Up