Bivalirudin, marketed as Angiomax or Angiox, is a bivalent direct thrombin inhibitor that binds directly to the active site of thrombin, as well as its exosite. It is synthetically created, and is structurally similar to the drug hirudin, which is found in medicinal leeches. It is used in preventing coagulation and formation of blood clots due to the inactivation of the enzyme that catalyzes activation of coagulation factors V, XIII and fibrinogen. Bivalirudin is a reversible direct thrombin inhibitor, as over time, thrombin can cleave the bonds between it and bivalirudin, allowing it to become active again. After injection, bivalirudin enters the blood stream and directly binds to thrombin, preventing its use as an enzyme. This prevents catalyzation of factor V to factor Va, which would form the prothrombinase complex and create more thrombin. It also prevents the catalysis fibrinogen or factor I to fibrin, which then polymerizes to form the blood clot. The lack of useable thrombin also prevents the catalysis of factor XIII to factor XIIIa, which is necessary to crosslink the polymerized fibrin to form a water insoluble clot.

Bivalirudin Action References