Open AccessBivalirudin: Pharmacology and Clinical Applications
Author(s) -
Shammas Nicolas W.
Publication year - 2005
Publication title -
cardiovascular drug reviews
Language(s) - English
Resource type - Journals
eISSN - 1527-3466
pISSN - 0897-5957
DOI - 10.1111/j.1527-3466.2005.tb00177.x
Subject(s) - bivalirudin , medicine , direct thrombin inhibitor , thrombin , conventional pci , heparin , discovery and development of direct thrombin inhibitors , partial thromboplastin time , anticoagulant , pharmacology , cardiology , percutaneous coronary intervention , myocardial infarction , platelet , warfarin , dabigatran , atrial fibrillation
Bivalirudin (Hirulog®, Angiomax®) is a specific, reversible and direct thrombin inhibitor with a predictable anticoagulant effect. It is cleared by both proteolytic cleavage and renal mechanisms, predominantly glomerular filtration. Bivalirudin inhibits both circulating thrombin and fibrin bound thrombin directly by binding to thrombin catalytic site and anion‐binding exosite I in a concentration‐dependent manner. Bivalirudin prolongs activated partial thromboplastin time, prothrombin time, thrombin time and activated clotting time (ACT). ACT levels with bivalirudin do not correlate with its clinical efficacy. Bivalirudin with a provisional GpIIb/IIIa inhibitor is indicated in elective contemporary percutaneous coronary intervention (PCI). In respect to combined ischemic and hemor‐rhagic endpoints of death, myocardial infarction, unplanned urgent revascularization and major bleeding during PCI (including subgroups of patients with renal impairment and diabetes) bivalirudin is not inferior to unfractioned heparin and planned GpIIb/IIIa inhibitors. In addition, bivalirudin has been consistently shown to have significantly less in‐hospital major bleeding than heparin alone or heparin in combination with‐a GpIIb/IIIa inhibitor. Bivalirudin appears to be also safe and effective during PCI in patients with heparin‐induced thrombocytopenia. Finally, data from PCI studies support the safety and efficacy of bivalirudin, although its direct randomized comparison with unfractionated heparin is lacking.