Dabigatran etexilate (Dabigatrani etexilas)

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

Anticoagulants

Included in the formulation
  • Pradaxa®
    capsules inwards 
    Boehringer Ingelheim International GmbH     Germany
  • Pradaxa®
    capsules inwards 
    Boehringer Ingelheim International GmbH     Germany
    • Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):

    VED

    АТХ:

    B.01.A.E.07   Dabigatran etexilate

    Pharmacodynamics:

    The drug is an inactive predecessor of dabigatran. When used internally absorbed in the gastrointestinal tract, then subjected to hydrolysis by esterases in the liver and blood, turning into an active form - dabigatran. The latter is a strong direct competitive thrombin inhibitor. As thrombin (serine protease) converts fibrinogen into a fibrin during the cascade of fibrinogen coagulation, the inhibition of its activity prevents the formation of a thrombus. Dabigatran inhibits free thrombin, thrombin, associated with a fibrin clot, and thrombin-induced platelet aggregation. The inhibition of thrombin activity leads to a decrease coagulation properties of blood.

    Pharmacokinetics:

    Bioavailability - 6-8%. Absorption in the gastrointestinal tract, while with plasma proteins binds 34-35%. On average, the maximum concentration in the blood is observed after 0.5-2 hours after administration. The half-life is 11 hours. It is metabolized in the liver, excreted mainly by the kidneys (85%), and also through the gastrointestinal tract.

    Indications:

    Prevention of stroke, systemic thromboembolism in patients after orthopedic operations; To reduce mortality in patients with atrial fibrillation.

    ICD-10

    IX.I26-I28.I26   Pulmonary embolism

    IX.I30-I52.I48   Atrial fibrillation and flutter

    IX.I60-I69.I63   Cerebral infarction

    IX.I60-I69.I64   Stroke not specified as a hemorrhage or infarction

    IX.I70-I79.I74   Embolism and thrombosis of the arteries

    IX.I80-I89.I82   Embolism and thrombosis of other veins

    Contraindications:

    Chronic diseases of the kidney and / or liver; bleeding of various etiology and localization, as well as the presence of various organ damage resulting from bleeding, including hemorrhagic stroke; hemostasis disorders; simultaneous administration of ketoconazole; age to 18 years; hypersensitivity.

    Carefully:

    At conditions with a high risk of bleeding.

    Pregnancy and lactation:

    Category FDA - C. Data on the use of dabigatran etexilate in pregnancy are absent. The potential risk in humans is unknown.

    In experimental studies, there is no adverse effect on the fertility or postnatal development of newborns.

    Women of reproductive age should use reliable contraceptive methods to rule out the possibility of pregnancy in the treatment of dabigatran etexilate.When a pregnancy occurs, the use of dabigatran etexilate is not recommended, except when the expected benefit of treatment exceeds the possible risk.

    If it is necessary to use dabigatran etexilate during breastfeeding, because of the lack of clinical data, breastfeeding should be discontinued (as a precautionary measure).

    Dosing and Administration:

    The daily dose is 110-300 mg 1-2 times a day. Dosage regimen and duration of reception is determined individually by the attending physician.

    Side effects:

    From the respiratory system: hemoptysis, nosebleeds.

    From the nervous system: intracranial hemorrhage.

    From the hematopoietic / lymphatic system: bleeding, anemia, hematomas, thrombocytopenia.

    From the immune system: hypersensitivity reactions, including hives, rashes and itching, bronchospasm.

    From the musculoskeletal system: hemarthrosis.

    From the digestive system: ulceration of the mucous membrane of the gastrointestinal tract, dysphagia, vomiting, impaired liver function, increased activity of liver transaminases, abdominal pain, hyperbilirubinemia.

    From the side of the urinary system: hematuria.

    Possible hemorrhages and bleeding at the site of injection.

    Overdose:

    Increased risk of bleeding. In case of an overdose, you should cancel the drug and take diuretics to speed up the removal of the drug from the blood.

    Interaction:

    Increased risk of bleeding with concomitant use with the following drugs: inhibitors Pglycoprotein (amiodarone, quinidine, verapamil), heparin and its derivatives, dextran, ticagrelor, fondaparinux sodium, antagonists of the vitamin K, serotonin reuptake inhibitors, rivaroxaban, anticoagulants, non-steroidal anti-inflammatory drugs.

    Special instructions:

    Before carrying out various types of surgical invasive procedures and operations, the drug should be withdrawn at least 24 hours in advance.

    Care should be taken when driving vehicles and controlling mechanisms during the administration of the drug.

    Instructions
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