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Direct Thrombin Inhibitors
This section covers the role of thrombin in coagulation, and discusses the use of direct thrombin inhibitors as anticoagulants
In this section:
The role of thrombin in coagulation
Thrombin plays a key role in coagulation.1 During the propagation phase, activated Factor X converts large amounts of prothrombin to thrombin, initiating a ‘thrombin burst’
PL, phospholipid
The direct thrombin inhibitor dabigatran and its approved indications
- Dabigatran is a competitive, reversible direct thrombin inhibitor3
- It inhibits free thrombin, fibrin-bound thrombin and thrombin-induced platelet aggregation
- Inhibition of thrombin prevents the conversion of fibrinogen to fibrin and thus clot formation
- Dabigatran is orally administered as the prodrug dabigatran etexilate, which is converted to the active form in plasma and in the liver
- Dabigatran is approved in Europe in adults for:3
- Prevention of VTE in patients undergoing elective hip or knee replacement surgery
- Treatment of DVT and PE and prevention of recurrent DVT and PE (following initial parenteral anticoagulation for at least 5 days)
- Prevention of stroke and systemic embolism in patients with NVAF with ≥1 risk factors
References
- Hoffman M, Monroe DM. Coagulation 2006: a modern view of hemostasis. Hematol Oncol Clin North Am 2007;21:1–11. Return to content
- Mann KG, Brummel K, Butenas S. What is all that thrombin for? J Thromb Haemost 2003;1:1504–1514. Return to content
- Boehringer Ingelheim International GmbH. Pradaxa® (dabigatran etexilate) Summary of Product Characteristics. 2018. Available at: http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/000829/WC500041059.pdf [accessed 22 August 2018]. Boehringer Ingelheim International GmbH. Pradaxa® (dabigatran etexilate) Summary of Product Characteristics. 2018. Available at: http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/000829/WC500041059.pdf [accessed 22 August 2018]. Return to content
