Ibrutinib (Ibrutinib)

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
  • Imbruwick
    capsules inwards 
    Johnson & Johnson, 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.X.E.27   Ibrutinib

    Pharmacodynamics:

    Covalently binds to the cysteine ​​residue (Cys 481) of the Bruton tyrosine kinase active site. This blocks the metabolic pathways, which depend on the signaling activity of antigenic B-cell receptors. As a result, the division and uncontrolled spread of B cells ceases, the development of the tumor slows down due to the death of malignant cells.

    Pharmacokinetics:

    After ingestion with food up to 59% is absorbed in the gastrointestinal tract. The maximum concentration in the blood plasma is achieved in 1-2 hours. The connection with plasma proteins is 97.3%.

    Metabolism in the liver with the participation of CYP3A4 enzymes to the dihydrodiol metabolite, whose activity is 15 times lower than ibrotinib.

    The half-life is 4-6 hours.

    Elimination with feces (over 90%) and kidneys (less than 10%).

    Indications:

    It is used to treat chronic lymphocytic leukemia and T-cell lymphomas.

    ICD-10

    II.C81-C96.C84.5   Other and unspecified T-cell lymphomas

    II.C81-C96.C91.1   Chronic lymphocytic leukemia

    Contraindications:

    Severe renal and hepatic impairment, age under 18, pregnancy and lactation, individual intolerance.

    Carefully:

    The need for anticoagulants, in addition to antagonists of vitamin K, including warfarin, hypersensitivity.

    Pregnancy and lactation:

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

    Dosing and Administration:

    Inside, with meals, 420-560 mg once a day.

    The highest daily dose: 560 mg.

    The highest single dose: 560 mg.

    Side effects:

    Central and peripheral nervous system: headache, transient impairment of cerebral circulation, rarely - ischemic stroke.

    Respiratory system: dyspnea, cough, pneumothorax, dysphonia.

    Hemopoietic system: neutropenia, thrombocytopenia.

    Blood coagulation system: nasal bleeding, thromboembolic complications, gastrointestinal bleeding.

    The cardiovascular system: increased blood pressure, myocardial infarction, rarely - ventricular tachycardia.

    Digestive system: abdominal pain, dyspeptic disorders, diarrhea, stomatitis.

    Musculoskeletal system: myalgia, ossalgia.

    Dermatological reactions: alopecia, depigmentation of hair, dry skin, nail damage, exfoliative rash.

    Sense organs: decreased visual acuity.

    urinary system: proteinuria.

    Allergic reactions.

    Overdose:

    Increased side effects.

    Treatment is symptomatic.

    Interaction:

    Inductors CYP3A4 (carbamazepine, rifampicin, phenytoin) reduce the concentration of the drug in the blood plasma.

    Special instructions:

    Monitoring of the blood count, including coagulograms, every 2 weeks during the first two months of treatment, then monthly and according to clinical indications.

    It is not recommended to drink the drug with grapefruit juice.

    During treatment, patients need to use reliable contraceptive methods. If the drug is dizzy, you should stop driving the car and work with moving mechanisms.

    Instructions
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