Tissue factor-mediated activation of the prothrombin complex concentrate (PCC) is differently inhibited by dabigatran, rivaroxaban, and apixaban: Potential clinical implication

Clinical and Applied Thrombosis/Hemostasis

Volumn 19, Issue 6, 2013, Pages 589-599

  Sadeghi, Nasiredin ^a   Kahn, Daniel ^a   Jeske, Walter ^a   Hoppensteadt, Debra ^a   Fareed, Jawed ^a  

^a LOYOLA UNIVERSITY MEDICAL CENTER   (United States)

Author keywords

(PCCs) Profilnine SD; apixaban; dabigatran; lepirudin; Neoplastine Cl Plus; otamixaban; prothrombin complex concentrates; rivaroxaban; Simplastin Excel; Thromboplastin C Plus

Indexed keywords

ANTICOAGULANT AGENT; APIXABAN; ARGATROBAN; BLOOD CLOTTING FACTOR 10A; BLOOD CLOTTING FACTOR 11A; DABIGATRAN; EDOXABAN; LEPIRUDIN; OTAMIXABAN; PROTHROMBIN COMPLEX; RECOMBINANT BLOOD CLOTTING FACTOR 9; RIVAROXABAN; THROMBOPLASTIN;

ANTICOAGULATION; ARTICLE; BLEEDING; CONTROLLED STUDY; CROSS REACTION; HUMAN; NONHUMAN; PRIORITY JOURNAL; RABBIT; SURFACE ENHANCED LASER DESORPTION IONIZATION TIME OF FLIGHT MASS SPECTROMETRY; WESTERN BLOTTING;

(PCCS)-PROFILNINE SD; APIXABAN; DABIGATRAN; LEPIRUDIN; NEOPLASTINE CL PLUS; OTAMIXABAN; PROTHROMBIN COMPLEX CONCENTRATES; RIVAROXABAN; SIMPLASTIN EXCEL; THROMBOPLASTIN C PLUS;

ANTICOAGULANTS; BENZIMIDAZOLES; BETA-ALANINE; BLOOD COAGULATION FACTORS; ELECTROPHORESIS, POLYACRYLAMIDE GEL; FACTOR XA; HUMANS; MORPHOLINES; PROTHROMBIN; PYRAZOLES; PYRIDONES; THIOPHENES; THROMBIN; THROMBOPLASTIN;

EID: 84887898735     PISSN: 10760296     EISSN: 19382723     Source Type: Journal    
DOI: 10.1177/1076029613479819     Document Type: Article

References (29)

1. Linhardt RJ. Heparin: an important drug enters its seventh decade. Chem Indust. 1991 ; 2: 45-50
2. Laurent TC, Tengblad A, Thunberg L, Hook M, Lindahl U. The molecular-weight-dependence of the anti-coagulant activity of heparin. Biochem J. 1978 ; 175 (2). 691-701
3. Capila I, Linhardt RJ. Heparin-protein interactions. Angew Chem Int Ed Engl. 2002 ; 41 (3). 391-412
4. Gandhi NS, Mancera RL. The structure of glycosaminoglucans and their interactions with proteins. Chem Biol Drug Des. 2008 ; 72 (6). 455-482
5. Rosenberg RD, Damus PS. The purification and mechanism of action of human antithrombin-heparin cofactor. J Biol Chem. 1973 ; 248 (18). 6490-6505
6. Thunberg L, Backstrom G, Lindahl U. Further characterization of the antithrombin binding sequence in heparin. Carbohydr Res. 1982 ; 100: 393-410
7. Choay J, Petitou M, Lormeau JC, Sinay P, Casu B, Gatti G. Structure-activity relationship in heparin: a synthetic pentasaccharide with high affinity for antithrombin III and eliciting high antifactor Xa activity. Biochem Biophys Res Commun. 1983 ; 116 (2). 492-499
8. Olson ST, Bjork I, Sheffer R, Craig PA, Shore JD, Choay J. Role of the antithrombin binding pentasaccharide in heparin acceleration of antithrombin-protease reactions. Resolution of the antithrombin conformational change contribution to heparin rate enhancement. J Biol Chem. 1992 ; 267 (18). 12528-12538
9. VanBoeckel CAA, Petitou M. The unique antithrombin III binding domain of heparin: a lead to new synthetic antithrombotics. Angew Chemie Int Ed. 1993 ; 32 (12). 1671-1690
10. Olson ST, Halvorson HR, Bjoork I. Quantitative characterization of the thrombin-heparin interaction. Discrimination between specific and nonspecific binding models. J Biol Chem. 1991 ; 266 (10). 6342-6352
11. Gervin AS. Complications of heparin therapy. Surg Gynecol Obst. 1975 ; 140 (5). 789-796
12. Kelton JG, Warkentin TE. Heparin-induced thrombocytopenia: a historical perspective. Blood. 2008 ; 112 (7). 2607-2616
13. Gandhi NS, Mancera RL. Heparin/heparin sulphate-based drugs. Drug Discov Today. 2010 ; 15 (23-24). 1058-1069
14. Quinalan DJ, McQuillan A, Eikelboom JW. Low molecular weight heparin compared with intravenous unfractionated heparin for treatment of pulmonary embolism: a meta-analysis of randomized, controlled trials. Ann Intern Med. 2004 ; 140 (3). 175-183
15. Kakkar AK. Low and ultra low molecular weight heparins. Best Prac Res Clin Haematol. 2004 ; 17 (1). 77-87
16. Gowthami M, Arepally MD, Thomas L Ortel MD. Heparin-induced thrombocytopenia. N Engl J. 2006 ; 355 (8). 809-817
17. Johnson JA, Gong L, Whirl-Carrillo M, et al. Clinical pharmacogenetic Implementation Consortium Guidelines for CYP2C9 and VKORRC1 genotypes and warfarin dosing. Clinical Pharmacol Ther. 2011 ; 90 (4). 625-629
18. Connolly SJ, Ezekowitz MD, Yusuf S, et al. RE-LY Steering Committee and Investigators. Dabigatran versus warfarin in patients with atrial fibrillation. N Engl J Med. 2009 ; 361 (12). 1139-1151
19. Hanley JP. Warfarin reversal. J Clinc Pathol. 2004 ; 57 (11). 1132-1139
20. Samama CM. Prothrombin complex concentrates: a brief review. Eur J Anaesthesiol. 2008 ; 25 (10). 784-789
21. Schick KS, Fertmann JM, Jauch KW, Hoffman JN. Prothrombin complex concentrate in surgical patients: retrospective evaluation of vitamin K antagonist reversal and treatment of severe bleeding. Crit Care. 2009 ; 13 (6). R191
22. Pindur G, Morsdorf S. The use of prothrombin complex concentrates in the treatment of hemorrhages induced by oral anticoagulation. Thromb Res. 1999 ; 95 (4 suppl 1). S57 - S61
23. Hellstern P, Halbmayer WM, Kohler M, Seitz R, Muller-Berghaus G. Prothrombin complex concentrates: indication, contraindications, and risks: a task force summary. Thromb Res. 1999 ; 95 (4 suppl 1). S3 - S6
24. Bebulin VH (Factor IX Complex). Westlake Village, CA: Baxter Healthcare Corporation ; 2006 :
25. Profilnine® SD (Factor IX Complex). Los Angeles, CA: Grifols Biological Inc ; 2010 :
26. Kohler M, Hellstern P, Lechler E, Uberfuhr P, Muller-Berghaus G. Thromboembolic complication associated with the use of prothrombin complex and factor IX concentrates. Thromb Haemost. 1998 ; 80 (3). 399-402
27. Sadeghi N, Zhu H, Setty S, Cunanan J, Hoppensteadt D, Fareed J. Cross-reactivity of various thrombin products with anti-rabbit antibodies to bovine, human, and recombinant thrombin. Clin Appl Thromb Hemost. 2012 ; 18 (3). 243-248
28. Eerenberg ES, Kamphuisen PW, Sijpkens MK, Meijers JC, Buller HR, Levi M. Reversal of rivaroxaban and dabigatran by prothrombin complex concentrate: a randomized, placebo-controlled, crossover study in healthy subjects. Circulation. 2011 ; 124 (14). 1573-1579
29. Leissinger CA, Blatt PM, Hoot WK, Ewenstein B. Role of prothrombin complex concentrates in reversing warfarin anticoagulation: a review of the literature. Am J Hematol. 2008 ; 83 (2). 137-143