DefinitionThis section has been translated automatically.
Dabigatran is a reversible direct oral thrombin inhibitor. Dabigatran inhibits both free and fibrin-bound thrombin and thrombin-induced platelet aggregation.
The oral drug is administered as an inactive prodrug called "dabigatran etexilate". Dabigatran etexilate is converted into the active dabigatran in the plasma in the liver by esterases. The reaction is independent of CYP450. The maximum plasma concentration is reached 0.5 - 2 hours after ingestion. Dabigatran has a half-life of 11-14 hours.
Pharmacodynamics (Effect)This section has been translated automatically.
Hirudin analogues bind with high affinity to the catalytic centre and the substrate recognition domain of the protease thrombin and thus behave like competitive inhibitors of the enzyme. They strongly prolong thrombin time and moderately prolong aPTT. The drugs are excreted metabolically and renally.
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IndicationThis section has been translated automatically.
Prevention of stroke and systemic embolism in adult patients with non-valvular atrial fibrillation Treatment of adult patients with deep vein thrombosis and/or pulmonary embolism after prior treatment with fractionated or unfractionated heparin for 5 days and prevention of recurrent deep vein thrombosis and/or pulmonary embolism.
Pregnancy/nursing periodThis section has been translated automatically.
Not to be used by pregnant women and nursing mothers. Do not use during the breastfeeding period.
Dosage and method of useThis section has been translated automatically.
According to the technical information. Dabigatran is usually taken in the morning and evening independently of meals.
Undesirable effectsThis section has been translated automatically.
See below for details:
Common (≥ 1/100, < 1/10) ADRs: Anemia, nosebleed, gastrointestinal bleeding, abdominal pain, diarrhea, dyspepsia, nausea. Occasionally ( ≥ 1/1000, < 1/100): thrombocytopenia, drug hypersensitivity, rash, intracranial bleeding, hematoma, hemoptysis, rectal/hemorrhoidal bleeding, gastrointestinal ulcers, gastroesophagitis, vomiting, pathological liver function, dysphagia, skin bleeding. Rare (≥ 1/10.000, < 1/1000): Urticaria, hyperbilirubinaemia, haemarthrosis, urogenital haemorrhage, haematuria.
InteractionsThis section has been translated automatically.
The simultaneous intake of P-glycoprotein inhibitors (e.g. amiodarone, verapamil, quinidine, ketoconazole and clarithromycin) leads to increased dabigatran levels. If P-glycoprotein inducers such as rifampicin, St. John's wort, carbamazepine or phenytoin are taken at the same time, dabigatran levels decrease.
ContraindicationThis section has been translated automatically.
Hypersensitivity to the active substance or any of the other ingredients. Patients with severe renal insufficiency. Acute clinically relevant bleeding. Organ damage that increases the risk of bleeding, spontaneous or pharmacologically induced restriction of hemostasis, impairment of liver function, liver disease, concomitant systemic administration of ketoconazole, ciclosporin, itraconazole or tacrolimus. For further contraindications see Technical Information. There is no approval for children and adolescents.
PreparationsThis section has been translated automatically.
Note(s)This section has been translated automatically.
Since the beginning of 2016, a specific antidote has been available to counteract the effects of dabigatran in an emergency. This is the humanised antibody fragment Idarucizumab.