Thrombin's Critical Role
- Thrombin is a critical target in antithrombotic
therapy because it plays key roles in thrombosis,
hemostasis, and inflammation1,2
- The coagulation process is initiated after injury
exposes tissue factor. At this point, a small
amount of thrombin is produced2,3,4
- Thrombin activates platelets at the site of
injury. Thrombin is the most potent physiologic platelet activator2,3,4
- Platelets then participate in the inflammatory
process and in the propagation of coagulation2
- Platelet activation and aggregation promote
production of more thrombin1,2
- Thrombin triggers fibrin formation1,2,3
- The result is an explosive burst of thrombin,
mostly after clot formation3
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Angiomax® (bivalirudin) inhibits both circulating and clot-bound thrombin,
blocking thrombin at a crucial point—the site of massive
thrombin production within a clot or the site of vessel injury3,5,6
Safety Considerations
ANGIOMAX with provisional use of glycoprotein IIb/IIIa inhibitor is indicated for use as an anticoagulant in patients undergoing percutaneous coronary intervention (PCI), and in patients with or at risk for heparin-induced thrombocytopenia and thrombosis syndrome (HIT/HITTS) undergoing PCI. ANGIOMAX is intended for use with aspirin and has been studied only in patients receiving concomitant aspirin. ANGIOMAX is contraindicated in patients with active major bleeding or hypersensitivity to ANGIOMAX or its components. The most common (
10%) adverse events for ANGIOMAX were back pain, pain, nausea, headache, and hypotension. An unexplained fall in blood pressure or hematocrit, or any unexplained symptom, should lead to serious consideration of a hemorrhagic event and cessation of ANGIOMAX administration. Please see complete
prescribing information.
1Coughlin SR. Thrombin signalling and protease-activated receptors. Nature. 2000;407:258-264.
2Monroe DM, Hoffman M, Roberts HR. Platelets and thrombin generation. Arterioscler Thromb Vasc Biol. 2002;22:1381-1389.
3Brummel KE, Paradis SG, Butenas S, Mann KG. Thrombin functions during tissue factor-induced blood coagulation. Blood. 2002;100:148-152.
4Mann KG. Thrombin formation. Chest. 2003;124:4S-10S.
5ANGIOMAX® (bivalirudin) Prescribing Information, The Medicines Company, Parsippany, NJ, December 6, 2005.
6Weitz JI, Crowther M. Direct thrombin inhibitors. Thromb Res. 2002;106:V275-V284.