Bivalirudin – direct thrombin inhibitor. Mechanism of action and indication in cardiology Review article
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Published:
Mar 31, 2008
Keywords:
bivalirudin, direct thrombin inhibitor, percutaneous coronary intervention
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Abstract
An understanding of mechanisms of physiological hemostasis and limitations of existing antithrombotic drugs have led to development and expanding clinical use of a number of new antithrombotic agents designed to target specific steps in the platelet and coagulation hemostatic pathways. Direct thrombin inhibitors are a new class of anticoagulants that bind directly to thrombin and block its interaction with its substrates. Currently bivalirudin is the only agent for which significant data exist with respect to its use in coronary and peripheral arteries intervention. This is a bivalent synthetic analog of hirudin which binds transiently to thrombin. Its transient thrombinbinding, short half-life, and only partial dependence on renal excretion potentially lower its risk of bleeding as compared with other thrombin inhibitors.
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Postuła , M., & Strzelak , A. (2008). Bivalirudin – direct thrombin inhibitor. Mechanism of action and indication in cardiology. Cardiology in Practice, 2(1), 22-28. Retrieved from https://www.journalsmededu.pl/index.php/kwp/article/view/1695
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References
1. Weitz J.I.: A novel approach to thrombin inhibition. Thrombosis Research 2003, 109: 517-522.
2. Tulinsky A.: Molecular interactions of thrombin. Semin. Thromb. Hemost. 1996, 22:117-24.
3. Stubbs M.T., Oschkinat H., Mayr I. et al.: The interaction of thrombin with fibrinogen. A structural basis for its specificity. Eur. J. Biochem. 1992, 206: 187-95.
4. Robson R., White H., Aylward P et al.: Bivalirudin pharmacokinetics and pharmacodynamics: 4. Effect of renal function, dose, and gender. Clin. Pharmacol. Ther. 2002, 71: 433-439.
5. Bates S.M., Weitz J.I.: The mechanism of action of thrombin inhibitors. J. Invasive Cardiol. 2000, 12 (supl. F): 27-32.
6. Xiao Z., Theroux P.: Platelet activation with unfractionated heparin at therapeutic concentrations and comparisons with a low-molecular-weight heparin and with a direct thrombin inhibitor. Circulation 1998, 97: 251-256.
7. Di Nisio M., Middeldorp S., Buller H.: Direct thrombin inhibitors. N. Engl. J. Med. 2005, 353: 1028-1040.
8. Bittl J.A., Strony J., Brinker J.A., Ahmed W.H., Meckel C.R., Chaitman B.R., Maraganore J., Deutsch E., Adelman B.: Treatment with bivalirudin (Hirulog) as compared with heparin during coronary angioplasty for unstable or postinfarction angina. Hirulog Angioplasty Study Investigators. N Engl. J. Med. 1995 Sep 21, 333(12): 764-769.
9. Bittl J.A., Chaitman B.R. et al.: Bivalirudin versus heparin during coronary angioplasty for unstable or postinfarction angina: Final report reanalysis of the Bivalirudin Angioplasty Study. Am. Heart J. 2001 Dec,142(6): 952-9.
10. Shammas N.W.: Bivalirudin: pharmacology and clinical applications. Cardiovasc. Drug Rev. 2005 Winter, 23(4): 345-60.
11. White H., Hirulog and Early Reperfusion or Occlusion (HERO)-2 Trial Investigators: Thrombin-specific anticoagulation with bivalirudin versus heparin in patients receiving fibrinolytic therapy for acute myocardial infarction: the HERO-2 randomised trial. Lancet 2001 Dec 1, 358(9296): 1855-63.
12. Antman E.M., Anbe D.T. et al. American College of Cardiology, American Heart Association Task Force on Practice Guidelines, Canadian Cardiovascular Society: ACC/AHA guidelines for the management of patients with ST-elevation myocardial infarction: a report of the American College of Cardiology/ American Heart Association Task Force on Practice Guidelines (Committee to Revise the 1999 Guidelines for the Management of Patients with Acute Myocardial Infarction). Circulation 2004 Aug 31, 110(9): e82-292.
13. Direct Thrombin Inhibitor Trialists' Collaborative Group. Direct thrombin inhibitors in acute coronary syndromes: principal results of a meta-analysis based on individual patients' data. Lancet 2002 Jan 26, 359(9303): 294-302.
14. Lincoff A.M., Bittl J.A. et al. REPLACE-2 Investigators: Bivalirudin and provisional glycoprotein IIb/IIIa blockade compared with heparin and planned glycoprotein IIb/IIIa blockade during percutaneous coronary intervention: REPLACE-2 randomized trial. JAMA 2003 Feb 19, 289(7): 853-63. (Errata w: JAMA 2003 Apr 2, 289(13): 1638).
15. Lincoff A.M., Bittl J.A. et al. REPLACE-1 Investigators: Comparison of bivalirudin versus heparin during percutaneous coronary intervention (the Randomized Evaluation of PCI Linking Angiomax to Reduced Clinical Events [REPLACE]-1 trial). Am. J. Cardiol. 2004 May 1, 93(9): 1092- 6.
16. Ebrahimi R., Lincoff A.M. et al.: Bivalirudin vs heparin in percutaneous coronary intervention: a pooled analysis. J. Cardiovasc. Pharmacol. Ther. 2005 Dec, 10(4): 209-16.
17. Chew D.P., Lincoff A.M. et al., REPLACE-2 Investigators: Bivalirudin versus heparin and glycoprotein IIb/IIIa inhibition among patients with renal impairment undergoing percutaneous coronary intervention (a subanalysis of the REPLACE-2 trial). Am. J. Cardiol. 2005 Mar 1, 95(5): 581-5.
18. Stone G.W., McLaurin B.T. et al. ACUITY Investigators: Bivalirudin for patients with acute coronary syndromes. N. Engl. J. Med. 2006 Nov 23, 355(21): 2203-16.
19. Waksman R.: ACUITY-PCI: one drug does not fit all. Lancet 2007 Mar 17, 369(9565): 881-2.
20. Dangas G, Lasic Z et al.: Effectiveness of the concomitant use of bivalirudin and drug-eluting stents (from the prospective, multicenter BivAlirudin and Drug-Eluting STents [ADEST] study). Am J Cardiol. 2005 Sep 1, 96(5): 659-63.
21. Rha S.W., Kuchulakanti P.K. et al.: Bivalirudin versus heparin as an antithrombotic agent in patients treated with a sirolimus-eluting stent. Am. J. Cardiol. 2004 Oct 15, 94(8): 1047-50.
22. Mishkel G.J., Moore A.L. et al.: Bivalirudin versus heparin plus glycoprotein IIb/IIIa inhibitors in drug-eluting stent implantations in the absence of acute myocardial infarction: clinical and economic results. J. Invasive Cardiol. 2007 Feb, 19(2): 63-8.
23. Silber S., Albertsson P. et al.: Guidelines for percutaneous coronary interventions. The Task Force for Percutaneous Coronary Interventions of the European Society of Cardiology. Eur. Heart J. 2005 Apr, 26(8): 804-47.
24. Bassand J.P., Hamm C.W. et al.: Guidelines for the diagnosis and treatment of non-ST-segment elevation acute coronary syndromes. The Task Force for the Diagnosis and Treatment of Non-ST-Segment Elevation Acute Coronary Syndromes of the European Society of Cardiology. Eur. Heart J. 2007 Jul, 28(13): 1598-660.
25. American College of Cardiology, American Heart Association Task Force on Practice Guidelines, American College of Emergency Physicians, Society for Cardiovascular Angiography and Interventions, Society of Thoracic Surgeons, American Association of Cardiovascular and Pulmonary Rehabilitation, Society for Academic Emergency Medicine: ACC/AHA 2007 guidelines for the management of patients with unstable angina/non- ST-Elevation myocardial infarction. A report of the American College of Cardiology/American Heart Association Task Force on Practice Guidelines developed in collaboration with the American College of Emergency Physicians, the Society for Cardiovascular Angiography and Interventions, and the Society of Thoracic Surgeons endorsed by the American Association of Cardiovascular and Pulmonary Rehabilitation and the Society for Academic Emergency Medicine. J. Am. Coll. Cardiol. 2007, 4, 50(7): e1-e157.
26. The Fifth Organization to Assess Strategies in Acute Ischemic Syndromes Investigators, Yusuf S., Mehta S.R., Chrolavicius S., Afzal R., Pogue J., Granger C.B., Budaj A., Peters R.J., Bassand J.P., Wallentin L., Joyner C., Fox K.A.: Comparison of fondaparinux and enoxaparin in acute coronary syndromes. The New England Journal of Medicine 2006, 354: 1464- 1476.
27. 2007 Focused Update of the ACC/AHA/SCAI 2005 Guideline Update for Percutaneous Coronary Intervention A Report of the American College of Cardiology/American Heart Association Task Force on Practice Guidelines: 2007 Writing Group to Review New Evidence and Update the ACC/AHA/SCAI 2005 Guideline Update for Percutaneous Coronary Intervention, Writing on Behalf of the 2005 Writing Committee. Circulation 2008, 117: 261-295.
28. 2007 Focused Update of the ACC/AHA 2004 Guidelines for the Management of Patients With ST-Elevation Myocardial Infarction A Report of the American College of Cardiology/American Heart Association Task Force on Practice Guidelines: Developed in Collaboration With the Canadian Cardiovascular Society Endorsed by the American Academy of Family Physicians: 2007 Writing Group to Review New Evidence and Update the ACC/AHA 2004 Guidelines for the Management of Patients With ST-Elevation Myocardial Infarction, Writing on Behalf of the 2004 Writing Committee. Circulation 2008, 117: 296-329.
29. Murphy G.S., Marymont J.H.: Alternative anticoagulation management strategies for the patient with heparin-induced thrombocytopenia undergoing cardiac surgery. J. Cardiothorac. Vasc. Anesth. 2007 Feb, 21(1): 113-26.
30. Vasquez J.C., Vichiendilokkul A. et al.: Anticoagulation with bivalirudin during cardiopulmonary bypass in cardiac surgery. Ann. Thorac. Surg. 2002 Dec, 74(6): 2177-9.
31. Stratmann G., deSilva A.M. et al.: Reversal of direct thrombin inhibition after cardiopulmonary bypass in a patient with heparin-induced thrombocytopenia. Anesth. Analg. 2004 Jun, 98(6): 1635-9 (table of contents).
32. Davis Z., Anderson R. et al.: Favorable outcome with bivalirudin anticoagulation during cardiopulmonary bypass. Ann. Thorac. Surg. 2003 Jan, 75(1): 264-5.
33. Koster A., Chew D. et al.: Bivalirudin monitored with the ecarin clotting time for anticoagulation during cardiopulmonary bypass. Anesth. Analg. 2003 Feb, 96(2): 383-6 (table of contents).
34. Clayton S.B., Acsell J.R. et al.: Cardiopulmonary bypass with bivalirudin in type II heparin-induced thrombocytopenia. Ann. Thorac. Surg. 2004 Dec, 78(6): 2167-9.
35. Bott J.N., Reddy K., Krick S.: Bivalirudin use in off-pump myocardial revascularization in patients with heparin-induced thrombocytopenia. Ann. Thorac. Surg. 2003 Jul, 76(1): 273-5.
36. Smedira N.G., Dyke C.M. et al.: Anticoagulation with bivalirudin for off-pump coronary artery bypass grafting: the results of the EVOLUTION-OFF study. J. Thorac. Cardiovasc. Surg. 2006 Mar, 131(3): 686-92.
37. Dyke C.M., Smedira N.G. et al.: A comparison of bivalirudin to heparin with protamine reversal in patients undergoing cardiac surgery with cardiopulmonary bypass: the EVOLUTION-ON study. J Thorac. Cardiovasc. Surg. 2006 Mar, 131(3): 533-9.
38. Koster A., Dyke C.M. et al.: Bivalirudin during cardiopulmonary bypass in patients with previous or acute heparin-induced thrombocytopenia and heparin antibodies: results of the CHOOSE-ON trial. Ann. Thorac. Surg. 2007 Feb, 83(2):572-7.
2. Tulinsky A.: Molecular interactions of thrombin. Semin. Thromb. Hemost. 1996, 22:117-24.
3. Stubbs M.T., Oschkinat H., Mayr I. et al.: The interaction of thrombin with fibrinogen. A structural basis for its specificity. Eur. J. Biochem. 1992, 206: 187-95.
4. Robson R., White H., Aylward P et al.: Bivalirudin pharmacokinetics and pharmacodynamics: 4. Effect of renal function, dose, and gender. Clin. Pharmacol. Ther. 2002, 71: 433-439.
5. Bates S.M., Weitz J.I.: The mechanism of action of thrombin inhibitors. J. Invasive Cardiol. 2000, 12 (supl. F): 27-32.
6. Xiao Z., Theroux P.: Platelet activation with unfractionated heparin at therapeutic concentrations and comparisons with a low-molecular-weight heparin and with a direct thrombin inhibitor. Circulation 1998, 97: 251-256.
7. Di Nisio M., Middeldorp S., Buller H.: Direct thrombin inhibitors. N. Engl. J. Med. 2005, 353: 1028-1040.
8. Bittl J.A., Strony J., Brinker J.A., Ahmed W.H., Meckel C.R., Chaitman B.R., Maraganore J., Deutsch E., Adelman B.: Treatment with bivalirudin (Hirulog) as compared with heparin during coronary angioplasty for unstable or postinfarction angina. Hirulog Angioplasty Study Investigators. N Engl. J. Med. 1995 Sep 21, 333(12): 764-769.
9. Bittl J.A., Chaitman B.R. et al.: Bivalirudin versus heparin during coronary angioplasty for unstable or postinfarction angina: Final report reanalysis of the Bivalirudin Angioplasty Study. Am. Heart J. 2001 Dec,142(6): 952-9.
10. Shammas N.W.: Bivalirudin: pharmacology and clinical applications. Cardiovasc. Drug Rev. 2005 Winter, 23(4): 345-60.
11. White H., Hirulog and Early Reperfusion or Occlusion (HERO)-2 Trial Investigators: Thrombin-specific anticoagulation with bivalirudin versus heparin in patients receiving fibrinolytic therapy for acute myocardial infarction: the HERO-2 randomised trial. Lancet 2001 Dec 1, 358(9296): 1855-63.
12. Antman E.M., Anbe D.T. et al. American College of Cardiology, American Heart Association Task Force on Practice Guidelines, Canadian Cardiovascular Society: ACC/AHA guidelines for the management of patients with ST-elevation myocardial infarction: a report of the American College of Cardiology/ American Heart Association Task Force on Practice Guidelines (Committee to Revise the 1999 Guidelines for the Management of Patients with Acute Myocardial Infarction). Circulation 2004 Aug 31, 110(9): e82-292.
13. Direct Thrombin Inhibitor Trialists' Collaborative Group. Direct thrombin inhibitors in acute coronary syndromes: principal results of a meta-analysis based on individual patients' data. Lancet 2002 Jan 26, 359(9303): 294-302.
14. Lincoff A.M., Bittl J.A. et al. REPLACE-2 Investigators: Bivalirudin and provisional glycoprotein IIb/IIIa blockade compared with heparin and planned glycoprotein IIb/IIIa blockade during percutaneous coronary intervention: REPLACE-2 randomized trial. JAMA 2003 Feb 19, 289(7): 853-63. (Errata w: JAMA 2003 Apr 2, 289(13): 1638).
15. Lincoff A.M., Bittl J.A. et al. REPLACE-1 Investigators: Comparison of bivalirudin versus heparin during percutaneous coronary intervention (the Randomized Evaluation of PCI Linking Angiomax to Reduced Clinical Events [REPLACE]-1 trial). Am. J. Cardiol. 2004 May 1, 93(9): 1092- 6.
16. Ebrahimi R., Lincoff A.M. et al.: Bivalirudin vs heparin in percutaneous coronary intervention: a pooled analysis. J. Cardiovasc. Pharmacol. Ther. 2005 Dec, 10(4): 209-16.
17. Chew D.P., Lincoff A.M. et al., REPLACE-2 Investigators: Bivalirudin versus heparin and glycoprotein IIb/IIIa inhibition among patients with renal impairment undergoing percutaneous coronary intervention (a subanalysis of the REPLACE-2 trial). Am. J. Cardiol. 2005 Mar 1, 95(5): 581-5.
18. Stone G.W., McLaurin B.T. et al. ACUITY Investigators: Bivalirudin for patients with acute coronary syndromes. N. Engl. J. Med. 2006 Nov 23, 355(21): 2203-16.
19. Waksman R.: ACUITY-PCI: one drug does not fit all. Lancet 2007 Mar 17, 369(9565): 881-2.
20. Dangas G, Lasic Z et al.: Effectiveness of the concomitant use of bivalirudin and drug-eluting stents (from the prospective, multicenter BivAlirudin and Drug-Eluting STents [ADEST] study). Am J Cardiol. 2005 Sep 1, 96(5): 659-63.
21. Rha S.W., Kuchulakanti P.K. et al.: Bivalirudin versus heparin as an antithrombotic agent in patients treated with a sirolimus-eluting stent. Am. J. Cardiol. 2004 Oct 15, 94(8): 1047-50.
22. Mishkel G.J., Moore A.L. et al.: Bivalirudin versus heparin plus glycoprotein IIb/IIIa inhibitors in drug-eluting stent implantations in the absence of acute myocardial infarction: clinical and economic results. J. Invasive Cardiol. 2007 Feb, 19(2): 63-8.
23. Silber S., Albertsson P. et al.: Guidelines for percutaneous coronary interventions. The Task Force for Percutaneous Coronary Interventions of the European Society of Cardiology. Eur. Heart J. 2005 Apr, 26(8): 804-47.
24. Bassand J.P., Hamm C.W. et al.: Guidelines for the diagnosis and treatment of non-ST-segment elevation acute coronary syndromes. The Task Force for the Diagnosis and Treatment of Non-ST-Segment Elevation Acute Coronary Syndromes of the European Society of Cardiology. Eur. Heart J. 2007 Jul, 28(13): 1598-660.
25. American College of Cardiology, American Heart Association Task Force on Practice Guidelines, American College of Emergency Physicians, Society for Cardiovascular Angiography and Interventions, Society of Thoracic Surgeons, American Association of Cardiovascular and Pulmonary Rehabilitation, Society for Academic Emergency Medicine: ACC/AHA 2007 guidelines for the management of patients with unstable angina/non- ST-Elevation myocardial infarction. A report of the American College of Cardiology/American Heart Association Task Force on Practice Guidelines developed in collaboration with the American College of Emergency Physicians, the Society for Cardiovascular Angiography and Interventions, and the Society of Thoracic Surgeons endorsed by the American Association of Cardiovascular and Pulmonary Rehabilitation and the Society for Academic Emergency Medicine. J. Am. Coll. Cardiol. 2007, 4, 50(7): e1-e157.
26. The Fifth Organization to Assess Strategies in Acute Ischemic Syndromes Investigators, Yusuf S., Mehta S.R., Chrolavicius S., Afzal R., Pogue J., Granger C.B., Budaj A., Peters R.J., Bassand J.P., Wallentin L., Joyner C., Fox K.A.: Comparison of fondaparinux and enoxaparin in acute coronary syndromes. The New England Journal of Medicine 2006, 354: 1464- 1476.
27. 2007 Focused Update of the ACC/AHA/SCAI 2005 Guideline Update for Percutaneous Coronary Intervention A Report of the American College of Cardiology/American Heart Association Task Force on Practice Guidelines: 2007 Writing Group to Review New Evidence and Update the ACC/AHA/SCAI 2005 Guideline Update for Percutaneous Coronary Intervention, Writing on Behalf of the 2005 Writing Committee. Circulation 2008, 117: 261-295.
28. 2007 Focused Update of the ACC/AHA 2004 Guidelines for the Management of Patients With ST-Elevation Myocardial Infarction A Report of the American College of Cardiology/American Heart Association Task Force on Practice Guidelines: Developed in Collaboration With the Canadian Cardiovascular Society Endorsed by the American Academy of Family Physicians: 2007 Writing Group to Review New Evidence and Update the ACC/AHA 2004 Guidelines for the Management of Patients With ST-Elevation Myocardial Infarction, Writing on Behalf of the 2004 Writing Committee. Circulation 2008, 117: 296-329.
29. Murphy G.S., Marymont J.H.: Alternative anticoagulation management strategies for the patient with heparin-induced thrombocytopenia undergoing cardiac surgery. J. Cardiothorac. Vasc. Anesth. 2007 Feb, 21(1): 113-26.
30. Vasquez J.C., Vichiendilokkul A. et al.: Anticoagulation with bivalirudin during cardiopulmonary bypass in cardiac surgery. Ann. Thorac. Surg. 2002 Dec, 74(6): 2177-9.
31. Stratmann G., deSilva A.M. et al.: Reversal of direct thrombin inhibition after cardiopulmonary bypass in a patient with heparin-induced thrombocytopenia. Anesth. Analg. 2004 Jun, 98(6): 1635-9 (table of contents).
32. Davis Z., Anderson R. et al.: Favorable outcome with bivalirudin anticoagulation during cardiopulmonary bypass. Ann. Thorac. Surg. 2003 Jan, 75(1): 264-5.
33. Koster A., Chew D. et al.: Bivalirudin monitored with the ecarin clotting time for anticoagulation during cardiopulmonary bypass. Anesth. Analg. 2003 Feb, 96(2): 383-6 (table of contents).
34. Clayton S.B., Acsell J.R. et al.: Cardiopulmonary bypass with bivalirudin in type II heparin-induced thrombocytopenia. Ann. Thorac. Surg. 2004 Dec, 78(6): 2167-9.
35. Bott J.N., Reddy K., Krick S.: Bivalirudin use in off-pump myocardial revascularization in patients with heparin-induced thrombocytopenia. Ann. Thorac. Surg. 2003 Jul, 76(1): 273-5.
36. Smedira N.G., Dyke C.M. et al.: Anticoagulation with bivalirudin for off-pump coronary artery bypass grafting: the results of the EVOLUTION-OFF study. J. Thorac. Cardiovasc. Surg. 2006 Mar, 131(3): 686-92.
37. Dyke C.M., Smedira N.G. et al.: A comparison of bivalirudin to heparin with protamine reversal in patients undergoing cardiac surgery with cardiopulmonary bypass: the EVOLUTION-ON study. J Thorac. Cardiovasc. Surg. 2006 Mar, 131(3): 533-9.
38. Koster A., Dyke C.M. et al.: Bivalirudin during cardiopulmonary bypass in patients with previous or acute heparin-induced thrombocytopenia and heparin antibodies: results of the CHOOSE-ON trial. Ann. Thorac. Surg. 2007 Feb, 83(2):572-7.