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Anticoagulants


title: Anticoagulants tags: #FFICM notebook: 🌑-FFICM


BMJ Chat

Dabigatran is used to prevent thromboembolism, particularly following knee and hip arthroplasty surgery. Dabigatran itself is not absorbed when given orally. However, pro-drug dabigatran etexilate has good oral bioavailability. It is converted to active drug by hydrolysis in the liver. Dabigatran is a potent, synthetic, reversible, non-peptide thrombin inhibitor. The inhibition of thrombin results in decreased formation of fibrin and reduces platelet aggregation. Dabigatran inhibits both free and fibrin-bound forms of thrombin, as well as thrombin induced platelet aggregation. The drug is administered by one daily dose and dose not require regular monitoring of effect. [[Mon11October0521AM_4]]

Heparin binds to an enzyme inhibitor, antithrombin III, this in turn inactivates thrombin and factor Xa. Heparin als activates lipoprotein lipase involved in fat transport and binds to histamine and 5-HT receptors. It is not active orally but administered usually by intravenous and subcutaneous routes. [[Mon11October0521AM_4]]

Warfarin also active orally inhibits the synthesis of vitamin K-dependent clotting factors these are Factors II, VII, IX, and X. [[Mon11October0521AM_4]]

Idarucizumab, a monoclonal antibody fragment that has been developed to reverse the anticoagulant effect of dabigatran. It binds specifically to dabigatran and its metabolites and will not reverse the effects of other anticoagulants. [[Mon11October0521AM_4]]

Flashcard type:basic
What is dabigatran's mechanism of action to act as an anticoagulant? Inhibits thrombin
What does thrombin do to help clotting? Increases fibrin levels, and platelet aggregation
What is heparin's mechanism of action to act as an anticoagulant? Binds to Antithrombin III, which then inactivates thrombin and Factor Xa
What does Antithrombin III enzyme do? Inactivates thrombin and factor Xa
What is warfarins mechanism of action to act as an anticoagulant? Inhibits synthesis of Vit-K dependent clotting factors
Which are the Vitamin K dependent clotting factors? Factors II, VII, IX, and X
What do the clotting factors II, VII, IX, and X have in common? They are the Vitamin K dependent clotting factors
What is the specific reversal agent for dabigatran? Idarucizumab
What is idarucizumab for? Reversal agent for dabigatran