Direct thrombin inhibitors in cardiovascular disease

Nature Reviews Cardiology

Volumn 9, Issue 7, 2012, Pages 402-414

  Arsenault, Kyle A ^a   Hirsh, Jack ^b   Whitlock, Richard P ^b   Eikelboom, John W ^b  

^a MCMASTER UNIVERSITY   (Canada)

^b MCMASTER UNIVERSITY   (Canada)

Author keywords

[No Author keywords available]

Indexed keywords

ABCIXIMAB; ACETYLSALICYLIC ACID; ARGATROBAN; CLOPIDOGREL; DABIGATRAN ETEXILATE; DESULFATOHIRUDIN; ENOXAPARIN; EPTIFIBATIDE; FIBRINOGEN RECEPTOR ANTAGONIST; HEPARIN; HIRULOG; LEPIRUDIN; THIENOPYRIDINE DERIVATIVE; THROMBIN; TIROFIBAN; WARFARIN; XIMELAGATRAN;

ACUTE CORONARY SYNDROME; BLEEDING; BLOOD CLOTTING TIME; BRAIN ISCHEMIA; CARDIOVASCULAR DISEASE; CORONARY ARTERY DISEASE; DRUG EFFICACY; DRUG ELIMINATION; DRUG MEGADOSE; DRUG SAFETY; EMBOLISM; ENZYME ACTIVE SITE; GASTROINTESTINAL HEMORRHAGE; HEART ATRIUM FIBRILLATION; HEPARIN INDUCED THROMBOCYTOPENIA; HUMAN; INTENTION TO TREAT ANALYSIS; LIVER TOXICITY; LOW DRUG DOSE; NON INSULIN DEPENDENT DIABETES MELLITUS; NON ST SEGMENT ELEVATION ACUTE CORONARY SYNDROME; NON ST SEGMENT ELEVATION MYOCARDIAL INFARCTION; PARTIAL THROMBOPLASTIN TIME; PRIORITY JOURNAL; RANDOMIZED CONTROLLED TRIAL (TOPIC); REVASCULARIZATION; REVIEW; ST SEGMENT ELEVATION MYOCARDIAL INFARCTION; STROKE; VENOUS THROMBOEMBOLISM;

ADMINISTRATION, ORAL; ANIMALS; ANTITHROMBINS; BLOOD COAGULATION; CARDIOVASCULAR DISEASES; EVIDENCE-BASED MEDICINE; HEMORRHAGE; HUMANS; INFUSIONS, PARENTERAL; RISK ASSESSMENT; RISK FACTORS; TREATMENT OUTCOME;

EID: 84862865912     PISSN: 17595002     EISSN: 17595010     Source Type: Journal    
DOI: 10.1038/nrcardio.2012.61     Document Type: Review

References (76)

1. th ed: American College of Chest Physicians evidence-based clinical practice guidelines. Chest 141 (2 Suppl.), e24S-e43S (2012).
2. Lee, C. J. & Ansell, J. E. Direct thrombin inhibitors. Br. J. Clin. Pharmacol. 72, 581-592 (2011).
3. Eriksson, B. I. et al. Prevention of thromboembolism with use of recombinant hirudin: results of a double-blind, multicenter trial comparing the efficacy of desirudin (Revasc) with that of unfractionated heparin in patients having total hip replacement. J. Bone Joint Surg. Am. 79, 326-333 (1997).
4. Eriksson, B. I. et al. A comparison of recombinant hirudin with a low-molecular-weight heparin to prevent thromboembolic complications after total hip replacement. N. Engl. J. Med. 337, 1329-1335 (1997).
5. Greinacher, A. & Warkentin, T. E. The direct thrombin inhibitor hirudin. Thromb. Haemost. 99, 819-829 (2008).
6. Warkentin, T. E., Greinacher, A. & Koster, A. Bivalirudin. Thromb. Haemost. 99, 830-839 (2008).
7. nd Thrombin-specific inhibition by and slow cleave of hirulog-1. Biochem. J. 283, 737-743 (1992).
8. White, H. D. Pharmacological and clinical profile of bivalirudin in the treatment of patients with acute coronary syndrome. Expert Opin. Drug Metab. Toxicol. 5, 529-538 (2009).
9. Koster, A. et al. An assessment of different filter systems for extracorporeal elimination of bivalirudin: an in vitro study. Anesth. Analg. 96, 1316-1319 (2003).
10. Jeske, W. P., Fareed, J., Hoppensteadt, D. A., Lewis, B. & Walenga, J. M. Pharmacology of argatroban. Expert Rev. Hematol. 3, 527-539 (2010).
11. Hursting, M. J. et al. Novastan (brand of argatroban): a small-molecule, direct thrombin inhibitor. Semin. Thromb. Hemost. 23, 503-516 (1997).
12. Sciulli, T. M. & Mauro, V. F. Pharmacology and clinical use of bivalirudin. Ann. Pharmacother. 36, 1028-1041 (2002).
13. Hirsh, J. Heparin. N. Engl. J. Med. 324, 1565-1574 (1993).
14. Hirsh, J., Anand, S. S., Halperin, J. L. & Fuster, V. Guide to anticoagulant therapy: heparin. A statement for healthcare professionals from the American Heart Association. Circulation 103, 2994-3018 (2001).
15. Walenga, J. M. et al. Argatroban therapy does not generate antibodies that alter its anticoagulant activity in patients with heparin-induced thrombocytopenia. Thromb. Res. 105, 401-405 (2002).
16. Shantsila, E., Lip, G. Y. & Chong, B. H. Heparin-induced thrombocytopenia: a contemporary clinical approach to diagnosis and management. Chest 135, 1651-1664 (2009).
17. Bittl, J. A. et al. Treatment with bivalirudin (hirulog) as compared with heparin during coronary angioplasty for unstable or postinfarction angina. N. Engl. J. Med. 333, 764-769 (1995).
18. Bittl, J. A. et al. Bivalirudin versus heparin during coronary angioplasty for unstable or postinfarction angina: final report reanalysis of the Bivalirudin Angioplasty Study. Am. Heart J. 142, 952-959 (2001).
19. Lincoff, A. M. et al. Bivalirudin with planned or provisional abciximab versus low-dose heparin and abciximab during percutaneous coronary revascularization: results of the Comparison of Abciximab Complications with Hirulog for Ischemic Events Trial (CACHET). Am. Heart J. 143, 847-853 (2002).
20. Lincoff, A. M. et al. 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. 93, 1092-1096 (2004).
21. Lincoff, A. M. et al. 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 289, 853-863 (2003).
22. Lincoff, A. M. et al. Long-term efficacy of bivalirudin and provisional glycoprotein IIb/IIIa blockade vs heparin and planned glycoprotein IIb/IIIa blockade during percutaneous coronary intervention: REPLACE-2 randomized trial. JAMA 292, 696-703 (2004).
23. Cohen, D. J. et al. Economic evaluation of bivalirudin with provisional glycoprotein IIb/IIIa inhibition versus heparin with routine glycoprotein IIb/IIIa inhibition for percutaneous coronary intervention: results from the REPLACE-2 trial. J. Am. Coll. Cardiol. 44, 1792-1800 (2004).
24. Kastrati, A. et al. Bivalirudin versus unfractionated heparin during percutaneous coronary intervention. N. Engl. J. Med. 359, 688-696 (2008).
25. Parodi, G. et al. Comparison of bivalirudin and unfractionated heparin plus protamine in patients with coronary heart disease undergoing percutaneous coronary intervention (from the Antithrombotic Regimens aNd Outcome [ARNO] trial). Am. J. Cardiol. 105, 1053-1059 (2010).
26. Tavano, D. et al. Comparison of bivalirudin monotherapy versus unfractionated heparin plus tirofiban in patients with diabetes mellitus undergoing elective percutaneous coronary intervention. Am. J. Cardiol. 104, 1222-1228 (2009).
27. Kastrati, A. et al. Abciximab and heparin versus bivalirudin for non-ST-elevation myocardial infarction. N. Engl. J. Med. 365, 1980-1989 (2011).
28. Ebrahimi, R. et al. Bivalirudin vs heparin in percutaneous coronary intervention: a pooled analysis. J. Cardiovasc. Pharmacol. Therapeut. 10, 209-216 (2005).
29. Chew, D. P. et al. Bivalirudin provides increasing benefit with decreasing renal function: a meta-analysis of randomized trials. Am. J. Cardiol. 92, 919-923 (2003).
30. Stone, G. W. et al. Bivalirudin for patients with acute coronary syndromes. N. Engl. J. Med. 355, 2203-2216 (2006).
31. Stone, G. W. et al. Antithrombotic strategies in patients with acute coronary syndromes undergoing early invasive management: one-year results from the ACUITY trial. JAMA 298, 2497-2506 (2007).
32. Pinto, D. S. et al. Economic evaluation of bivalirudin with or without glycoprotein IIb/IIIa inhibition versus heparin with routine glycoprotein IIb/IIIa inhibition for early invasive management of acute coronary syndromes. J. Am. Coll. Cardiol. 52, 1758-1768 (2008).
33. Stone, G. W. et al. Bivalirudin during primary PCI in acute myocardial infarction. N. Engl. J. Med. 358, 2218-2230 (2008).
34. Mehran, R. et al. Bivalirudin in patients undergoing primary angioplasty for acute myocardial infarction (HORIZONS-AMI): 1-year results of a randomised controlled trial. Lancet 374, 1149-1159 (2009).
35. Stone, G. W. et al. Heparin plus a glycoprotein IIb/IIIa inhibitor versus bivalirudin monotherapy and paclitaxel-eluting stents versus bare-metal stents in acute myocardial infarction (HORIZONS-AMI): final 3-year results from a multicentre, randomised controlled trial. Lancet 377, 2193-2204 (2011).
36. Witzenbichler, B. et al. Impact of diabetes mellitus on the safety and effectiveness of bivalirudin in patients with acute myocardial infarction undergoing primary angioplasty: analysis from the HORIZONS-AMI (Harmonizing Outcomes with RevasculariZatiON and Stents in Acute Myocardial Infarction) trial. JACC Cardiovasc. Interv. 4, 760-768 (2011).
37. Cortese, B. et al. Comparison of prolonged bivalirudin infusion versus intraprocedural in preventing myocardial damage after percutaneous coronary intervention in patients with angina pectoris. Am. J. Cardiol. 104, 1063-1068 (2009).
38. Cortese, B. et al. Effect of prolonged bivalirudin infection on ST-segment resolution following percutaneous coronary intervention (from the PROBI VIRI 2 study). Am. J. Cardiol. 108, 1220-1224 (2011).
39. Dangas, G. D. et al. Effect of switching antithrombin agents for primary angioplasty in acute myocardial infarction: the HORIZONS-SWITCH analysis. J. Am. Coll. Cardiol. 57, 2309-2316 (2011).
40. Koutouzis, M. et al. Unfractionated heparin administration in patients treated with bivalirudin during primary percutaneous coronary intervention is associated lower mortality and target lesion thrombosis: a report from the Swedish Coronary Angiography and Angioplasty Registry (SCAAR). Heart 97, 1484-1488 (2011).
41. Kessler, D. P., Kroch, E. & Hlatky, M. A. The effect of bivalirudin on costs and outcomes of treatment of ST-segment elevation myocardial infarction. Am. Heart J. 162, 494-500.e2 (2011).
42. Lee, M. S. et al. Comparison of bivalirudin versus heparin plus glycoprotein IIb/IIIa inhibitors in patients undergoing an invasive strategy: a meta-analysis of randomized clinical trials. Int. J. Cardiol. 152, 369-374 (2011).
43. De Luca, G., Cassetti, E., Verdoia, M. & Marino, P. Bivalirudin as compared to unfractionated heparin among patients undergoing coronary angioplasty: a meta-analysis of randomized trials. Thromb. Haemost. 102, 428-436 (2009).
44. Lewis, B. E. et al. Argatroban anticoagulant therapy in patients with heparin-induced thrombocytopenia. Circulation 103, 1838-1843 (2001).
45. Lewis, B. E. et al. Argatroban anticoagulation in patients with heparin-induced thrombocytopenia. Arch. Intern. Med. 163, 1849-1856 (2003).
46. Lewis, B. E. et al. Argatroban anticoagulation during percutaneous coronary intervention in patients with heparin-induced thrombocytopenia. Catheter. Cardiovasc. Interv. 57, 177-184 (2002).
47. Hirahara, T. et al. Prospective randomized study of argatroban versus heparin anticoagulation therapy after percutaneous coronary intervention for acute myocardial infarction [Japanese]. J. Cardiol. 44, 47-52 (2004).
48. Rössig, L. et al. Argatroban for elective percutaneous coronary intervention: the ARG-E04 multi-center study. Int. J. Cardiol. 148, 214-219 (2011).
49. LaMonte, M. P. et al. Argatroban anticoagulation in patients with acute ischemic stroke (ARGIS-1): a randomized, placebo-controlled safety study. Stroke 35, 1677-1682 (2004).
50. Hankey, G. J. & Eikelboom, J. W. Dabigatran etexilate: a new oral thrombin inhibitor. Circulation 123, 1436-1450 (2011).
51. Testa, L. et al. The direct thrombin inhibitor ximelagatran/melagatran: A systematic review on clinical applications and an evidence based assessment of risk benefit profile. Expert Opin. Drug Saf. 6, 397-406 (2007).
52. Eriksson, B. I., Quinlan, D. J. & Eikelboom, J. W. Novel oral factor Xa and thrombin inhibitors in the management of thromboembolism. Annu. Rev. Med. 62, 41-57 (2011).
53. Stangier, J., Rathgen, K., Stähle, H., Gansser, D. & Roth, W. The pharmacokinetics, pharmacodynamics and tolerability of dabigatran etexilate, a new oral direct thrombin inhibitor, in healthy male subjects. Br. J. Clin. Pharmacol. 64, 292-303 (2007).
54. van Ryn, J. et al. Dabigatran etexilate-a novel, reversible, oral direct thrombin inhibitor: Interpretation of coagulation assays and reversal of anticoagulant activity. Thromb. Haemost. 103, 1116-1127 (2010).
55. The European Agency for the Evaluation of Medicinal Products: Committee for Proprietary Medicinal Products. Points to consider on clinical investigation of medicinal products for prophylaxis of intra and post-operative venous thromboembolic risk. Guideline CPMP/EWP/707/98 [online], http://www.ema.europa. eu/docs/en-GB/document-library/Scientific-guideline/2009/09/WC500003304.pdf (2000).
56. Eriksson, B. I. et al. Dabigatran etexilate versus enoxaparin for prevention of venous thromboembolism after total hip replacement: a randomised, double-blind, non-inferiority trial. Lancet 370, 949-956 (2007).
57. Eriksson, B. I. et al. Oral dabigatran versus enoxaparin for thromboprophylaxis after primary total hip arthroplasty (RE-NOVATE II): a randomised, double-blind, non-inferiority trial. Thromb. Haemost. 105, 721-729 (2011).
58. Eriksson, B. I. et al. Oral dabigatran etexilate vs. subcutaneous enoxaparin for the prevention of venous thromboembolism after total knee replacement: the RE-MODEL randomized trial. J. Thromb. Haemost. 5, 2178-2185 (2007).
59. RE-MOBILIZE Writing Committee. Oral thrombin inhibitor dabigatran etexilate vs North American enoxaparin regimen for prevention of venous thromboembolism after knee arthroplasty surgery. J. Arthroplasty 24, 1-9 (2009).
60. Friedman, R. J. et al. Dabigatran versus enoxaparin for prevention of venous thromboembolism after hip or knee arthroplasty: a pooled analysis of three trials. Thromb. Res. 126, 175-182 (2010).
61. Schulman, S. et al. Dabigatran versus warfarin in the treatment of acute venous thromboembolism. N. Engl. J. Med. 361, 2342-2352 (2009).
62. rd American Society of Hematology Annual Meeting and Exposition (2011).
63. rd Congress of the International Society on Thrombosis and Haemostasis (2011).
64. rd Congress of the International Society on Thrombosis and Haemostasis (2011).
65. EINSTEIN Investigators. Oral rivaroxaban for symptomatic venous thromboembolism. N. Engl. J. Med. 363, 2499-2510 (2010).
66. Connolly, S. J. et al. Dabigatran versus warfarin in patients with atrial fibrillation. N. Engl. J. Med. 361, 1139-1151 (2009).
67. Connolly, S. J. et al. Newly identified events in the RE-LY trial. N. Engl. J. Med. 363, 1875-1876 (2010).
68. Hurlen, M., Abdelnoor, M., Smith, P., Erikssen, J. & Arnesen, H. Warfarin, aspirin or both after myocardial infarction. N. Engl. J. Med. 347, 969-974 (2002).
69. Lip, G. Y. & Lane, D. A. Does warfarin for stroke thromboprophylaxis protect against MI in atrial fibrillation patients? Am. J. Med. 123, 785-789 (2010).
70. Granger, C. B. et al. Apixaban versus warfarin in patients with atrial fibrillation. N. Engl. J. Med. 365, 981-992 (2011).
71. Patel, M. R. et al. Rivaroxaban versus warfarin in nonvalvular atrial fibrillation. N. Engl. J. Med. 365, 883-891 (2011).
72. Eikelboom, J. W. et al. Risk of bleeding with 2 doses of dabigatran compared with warfarin in older and younger patients with atrial fibrillation: an analysis of the Randomized Evaluation of Long-Term Anticoagulant Therapy (RE-LY) trial. Circulation 123, 2363-2372 (2011).
73. Shah, S. V. & Gage, B. F. Cost-effectiveness of dabigatran for stroke prophylaxis in atrial fibrillation. Circulation 123, 2562-2570 (2011).
74. Oldgren, J. et al. Dabigatran vs. placebo in patients with acute coronary syndromes on dual antiplatelet therapy: a randomized, double-blind, phase II trial. Eur. Heart J. 32, 2781-2789 (2011).
75. Uchino, K. & Hernandez, A. V. Dabigatran association with higher risk of acute coronary events: meta-analysis of noninferiority randomized controlled trials. Arch. Intern. Med. 172, 397-402 (2012).
76. Hohnloser, S. H. et al. Myocardial ischemic events in patients with atrial fibrillation treated with dabigatran or warfarin in the RE-LY (Randomized Evaluation of Long-Term Anticoagulation Therapy) trial. Circulation 125, 669-676 (2012).