Novel oral anticoagulants: Pharmacology, coagulation measures, and considerations for reversal

Journal of Thrombosis and Thrombolysis

Volumn 37, Issue 3, 2014, Pages 380-391

  Jackson II, Larry R ^a   Becker, Richard C ^a  

^a DUKE CLINICAL RESEARCH INSTITUTE   (United States)

Author keywords

Coagulation measures; Novel oral anticoagulants; Pharmacology

Indexed keywords

ACTIVATED CARBON; ACTIVATED PROTHROMBIN COMPLEX; ALBUMIN; ANTICOAGULANT AGENT; ANTIVITAMIN K; APIXABAN; BLOOD CLOTTING FACTOR 10A; DABIGATRAN; EDOXABAN; FRESH FROZEN PLASMA; PROTHROMBIN COMPLEX; RECOMBINANT BLOOD CLOTTING FACTOR 7A; RIVAROXABAN; WARFARIN;

ANTICOAGULATION; ARTICLE; ASSAY; BLOOD CLOTTING TIME; CHROMOGENIC ASSAY; COST BENEFIT ANALYSIS; DILUTE RUSSELL VIPER VENOM TIME ASSAY; DILUTE THROMBIN TIME ASSAY; DRUG BIOAVAILABILITY; DRUG DISTRIBUTION; DRUG EXCRETION; DRUG HALF LIFE; DRUG METABOLISM; DRUG PROTEIN BINDING; ECARIN CLOTTING TIME; HEMATOLOGY TEST KIT; HEMODIALYSIS; HUMAN; INTERNATIONAL NORMALIZED RATIO; INTESTINE ABSORPTION; MAXIMUM PLASMA CONCENTRATION; PARTIAL THROMBOPLASTIN TIME; PRIORITY JOURNAL; PROTHROMBIN TIME; RISK BENEFIT ANALYSIS; THROMBIN TIME; TIME TO MAXIMUM PLASMA CONCENTRATION; BLOOD CLOTTING; CHEMICALLY INDUCED; CLINICAL TRIAL (TOPIC); DRUG EFFECTS; HEMORRHAGE; ORAL DRUG ADMINISTRATION; PHYSIOLOGIC MONITORING; PROCEDURES;

ADMINISTRATION, ORAL; ANTICOAGULANTS; BLOOD COAGULATION; CLINICAL TRIALS AS TOPIC; HEMORRHAGE; HUMANS; MONITORING, PHYSIOLOGIC;

EID: 84898538852     PISSN: 09295305     EISSN: 1573742X     Source Type: Journal    
DOI: 10.1007/s11239-013-0958-0     Document Type: Article

References (46)

1. Zehnder J, Katzung SM, Trevor A (2009) Basic and clinical pharmacology, 11th edn. McGraw-Hill Medical, New York
2. Kamali F, Wynne H (2010) Pharmacogenetics of warfarin. Annu Rev Med 61:63-75
3. Sanderson S, Emery J, Higgins J (2005) CYP2C9 gene variants, drug dose, and bleeding risk in warfarin-treated patients: a Hu-GEnet systematic review and meta-analysis. Genet Med 7:97-104 (Pubitemid 40261834)
4. Connolly SJ, Ezekowitz MD, Yusuf S et al (2009) Dabigatran versus warfarin in patients with atrial fibrillation. N Engl J Med 361:1139-1151
5. Blech S, Ebner T, Ludwig-Schwellinger E, Stangier J, Roth W (2008) The metabolism and disposition of the oral direct thrombin inhibitor, dabigatran, in humans. Drug Metab Dispos 36:386-399 (Pubitemid 351185753)
6. Schulman S, Kearon C, Kakkar AK et al (2009) Dabigatran versus warfarin in the treatment of acute venous thromboembolism. N Engl J Med 361:2342-2352
7. Pharm. BI (2011) PRADAXA (dabigatran etexilate): reducing risk of stroke from atrial fibrillation (Afib). Boehringer Ingelheim Pharmaceuticals, Inc, Ridgefield, CT
8. Ordovás Baines JP, Climent Grana E, Jover Botella A, Valero Garcia I (2009) Pharmacokinetics and pharmacodynamics of the new oral anticoagulants dabigatran and rivaroxaban. Farm Hosp 33:125-133
9. Hankey GJ, Eikelboom JW (2011) Dabigatran etexilate: a new oral thrombin inhibitor. Circulation 123:1436-1450
10. Patel MR, Mahaffey KW, Garg J et al (2011) Rivaroxaban versus warfarin in nonvalvular atrial fibrillation. N Engl J Med 365: 883-891
11. AG BSP (2011) Xarelto: summary of product characteristics. Bayer Pharma AG, Berlin
12. Kubitza D, Becka M, Voith B, Zuehlsdorf M, Wensing G (2005) Safety, pharmacodynamics, and pharmacokinetics of single doses of BAY 59-7939, an oral, direct factor Xa inhibitor. Clin Pharmacol Ther 78:412-421 (Pubitemid 41393676)
13. Fareed J, Thethi I, Hoppensteadt D (2012) Old versus new oral anticoagulants: focus on pharmacology. Annu Rev Pharmacol Toxicol 52:79-99
14. Granger CB, Alexander JH, McMurray JJ et al (2011) Apixaban versus warfarin in patients with atrial fibrillation. N Engl J Med 365:981-992
15. Carreiro J, Ansell J (2008) Apixaban, an oral direct Factor Xa inhibitor: awaiting the verdict. Expert Opin Investig Drugs 17: 1937-1945
16. Zafar MU, Vorchheimer DA, Gaztanaga J et al (2007) Antithrombotic effects of factor Xa inhibition with DU-176b: phase-I study of an oral, direct factor Xa inhibitor using an ex-vivo flow chamber. Thromb Haemost 98:883-888 (Pubitemid 47555083)
17. Favaloro EJ, Lippi G (2012) The new oral anticoagulants and the future of haemostasis laboratory testing. Biochemia medica : casopis Hrvatskoga drustva medicinskih biokemicara / HDMB 22:329-341
18. Ng VL (2009) Prothrombin time and partial thromboplastin time assay considerations. Clin Lab Med 29:253-263
19. Bates SM, Weitz JI (2005) Coagulation assays. Circulation 112:e53-e60
20. Miyares MA, Davis K (2012) Newer oral anticoagulants: a review of laboratory monitoring options and reversal agents in the hemorrhagic patient. Am J Health Syst Pharm 69:1473-1484
21. Tripodi A, van den Besselaar A (2009) Laboratory monitoring of anticoagulation: where do we stand? Semin Thromb Hemost 35:34-41
22. Asmis LM, Alberio L, Angelillo-Scherrer A et al (2012) Rivaroxaban: quantification by anti-FXa assay and influence on coagulation tests: a study in 9 Swiss laboratories. Thromb Res 129:492-498
23. Becker RC, Yang H, Barrett Y et al (2011) Chromogenic laboratory assays to measure the factor Xa-inhibiting properties of apixaban-an oral, direct and selective factor Xa inhibitor. J Thromb Thrombolysis 32:183-187
24. Castellone DD, Van Cott EM (2010) Laboratory monitoring of new anticoagulants. Am J Hematol 85:185-187
25. Colomina MJ, Diez Lobo A, Garutti I, Gomez-Luque A, Llau JV, Pita E (2012) Perioperative use of prothrombin complex concentrates. Minerva Anestesiol 78:358-368
26. Dentali F, Marchesi C, Pierfranceschi MG et al (2011) Safety of prothrombin complex concentrates for rapid anticoagulation reversal of vitamin K antagonists: a meta-analysis. Thromb Haemost 106:429-438
27. Hsia CC, Chin-Yee IH, McAlister VC (2008) Use of recombinant activated factor VII in patients without hemophilia: a meta-analysis of randomized control trials. Ann Surg 248:61-68
28. Hardy JF, Belisle S, Van der Linden P (2008) Efficacy and safety of recombinant activated factor VII to control bleeding in non-hemophiliac patients: a review of 17 randomized controlled trials. Ann Thorac Surg 86:1038-1048
29. Girolami A, Ruzzon E, Tezza F, Scandellari R, Vettore S, Girolami B (2006) Arterial and venous thrombosis in rare congenital bleeding disorders: a critical review. Haemophilia 12: 345-351
30. van Ryn J, Stangier J, Haertter S et al (2010) Dabigatran etexilate-a novel, reversible, oral direct thrombin inhibitor: interpretation of coagulation assays and reversal of anticoagulant activity. Thromb Haemost 103:1116-1127
31. Holbrook A, Schulman S, Witt DM et al (2012) Evidence-based management of anticoagulant therapy: antithrombotic therapy and prevention of thrombosis, 9th ed: American College of Chest Physicians Evidence-Based Clinical Practice Guidelines. Chest 141:e152S-e184S
32. Lubetsky A, Yonath H, Olchovsky D, Loebstein R, Halkin H, Ezra D (2003) Comparison of oral vs intravenous phytonadione (vitamin K1) in patients with excessive anticoagulation: a prospective randomized controlled study. Arch Intern Med 163: 2469-2473 (Pubitemid 37385789)
33. Fredriksson K, Norrving B, Stromblad LG (1992) Emergency reversal of anticoagulation after intracerebral hemorrhage. Stroke 23:972-977
34. Freeman WD, Brott TG, Barrett KM et al (2004) Recombinant factor VIIa for rapid reversal of warfarin anticoagulation in acute intracranial hemorrhage. Mayo Clin Proc 79:1495-1500 (Pubitemid 39578872)
35. Ageno W, Gallus AS, Wittkowsky A, Crowther M, Hylek EM, Palareti G (2012) Oral anticoagulant therapy: antithrombotic Therapy and Prevention of Thrombosis, 9th ed: American College of Chest Physicians Evidence-Based Clinical Practice Guidelines. Chest 141:e44S-e88S
36. Samama MM, Guinet C (2011) Laboratory assessment of new anticoagulants. Clin Chem Lab Med 49:761-772
37. Eerenberg ES, Kamphuisen PW, Sijpkens MK, Meijers JC, Buller HR, Levi M (2011) Reversal of rivaroxaban and dabigatran by prothrombin complex concentrate: a randomized, placebo-controlled, crossover study in healthy subjects. Circulation 124:1573-1579
38. Chan HHW, Atkinson HM, Goncharenko M, Berry LR, Chan AKC (2011) Reversal of dabigatran using recombinant activated factor VII and activated prothrombin complex concentrates in thromboelastography assay. J Thromb Haemost 9:576-577 (Abstracts of the XXIII Congress of the International Society on Thrombosis and Haemostasis, 57th Annual SSC Meeting, 2011)
39. Zhou W, Schwarting S, Illanes S et al (2011) Hemostatic therapy in experimental intracerebral hemorrhage associated with the direct thrombin inhibitor dabigatran. Stroke 42:3594-3599
40. Marlu R, Hodaj E, Paris A, Albaladejo P, Crackowski JL, Pernod G (2012) Effect of non-specific reversal agents on anticoagulant activity of dabigatran and rivaroxaban: a randomised crossover ex vivo study in healthy volunteers. Thromb Haemost 108: 217-224
41. Siegal DM, Crowther MA (2013) Acute management of bleeding in patients on novel oral anticoagulants. Eur Heart J 34:489-498
42. Escolar G, Arellano-Rodrigo E, Reverter JC et al (2012) Reversal of apixaban induced alterations of hemostasis by different coagulation factor concentrates: studies in vitro with circulating human blood. Circulation 126(4):520-521 (Abstract from the Emerging Science Series)
43. Fukuda T, Honda Y, Kamisato C, Morishima Y, Shibano T (2012) Reversal of anticoagulant effects of edoxaban, an oral, direct factor Xa inhibitor, with haemostatic agents. Thromb Haemost 107:253-259
44. Morishima Y, Honda Y, Kamisato C, Furugohri T, Shibano T (2011) Reversal agents for edoxaban, a factor Xa inhibitor: effects of factor VIIa, anti-inhibitor coagulant complex, prothrombin complex concentrate, fresh plasma, and vitamin K. J Thromb Haemost 9:135
45. Lu GP, Luan P, Hollenbach S, Abe K, DeGuzman F, Siu G, Hutchaleelaha A, Inagaki M, Conley PB, Phillips DR, Sinha U (2009) Reconstructed recombinant factor Xa as an antidote to reverse anticoagulation by factor Xa inhibitors. J Thromb Haemost 7:309 (Abstracts of the XXIII Congress of the International Society on Thrombosis and Haemostasis, 57th Annual SSC Meeting, 2011)
46. Van Ryn J, Litzenburger T, Waterman A (2011) CanadaK, Hauel N, Kroe-Barrett R, Singh S, Park J. Dabigatran anticoagulant activity is neutralized by an antibody selective to dabigatran in in vitro and in vivo models. J Am Coll Cardiol 57:E1130