INGIBITOR FAKTORA Kha SVERTYVAEMOSTI KROVI RIVAROKSABAN PRI MERTsATEL'NOY ARITMII


Cite item

Full Text

Abstract

The article presents data concerning rivaroxaban, a first factor Xa inhibitor that was approved for clinical use. Pharmacodynamics and pharmacokinetics of the drug, drug interactions, and clinical aspects of the application are discussed. The results of large randomized phase III ROCKET-AF study which evaluated the effectiveness of rivaroxaban compared with warfarin are analyzed. Based on the results of this study, rivaroxaban has been registered in Russia as an alternative to warfarin for the prevention of thromboembolic complications in patients with atrial fibrillation.

Full Text

Restricted Access

About the authors

I. V Zotova

D. A Zateyshchikov

References

  1. Krishnaswamy S., Vlasuk G.P., Bergum P.W., et al. Assembly of the prothrombinase complex enhances the inhibition of bovine factor Xa by tick anticoagulant peptide. Biochemistry 1994;33:7897-907.
  2. HeOrault J.P., Bernat A., Pflieger A.M., et al. Comparative effects of two direct and indirect factor Xa inhibitors on free and clot-bound prothrombinase. J Pharmacol Exp Ther 1997;283:16-22.
  3. Gailani D., Renne Т. Intrinsic pathway of coagulation and arterial thrombosis. Arterioscler Thromb Vasc Biol 2007;27:2507-13.
  4. Dunwiddie C. Antistasin, a leech-derived inhibitor of factor Xa. Kinetic analysis of enzyme inhibition and identification of the reactive site. J Biol Chem 1989;264:16694-99.
  5. Perzborn E., Strassburger J., Wilmen A., et al. In vitro and in vivo studies of the novel antithrombotic agent BAY 59-7939 - an oral, direct Factor Xa inhibitor. J Thromb Haemost 2005;3:514-21.
  6. Depasse F., Busson J., Mnich J., et al. Effect of BAY 59-7939 - a novel, oral, direct Factor Xa inhibitor - on clot-bound Factor Xa activity in vitro. J Thromb Haemost, 2005;3(1):Abstract P1104.
  7. Xu X.S., Moore K., Burton P., et al. Population Pharmacokinetics and Pharmacodynamics of Rivaroxaban in Patients with Acute Coronary Syndromes. Br J Clin Pharmacol 2012; doi: 10.1111/j.1365-2125.2012.04181.x.
  8. Mueck W., Eriksson B.I., Bauer K.A., et al. Population pharmacokinetics and pharmacodynamics of rivaroxaban - an oral, direct factor xa inhibitor - in patients undergoing major orthopaedic surgery. Clin Pharmacokinet 2008;47:203-16.
  9. Xarelto. Summary of Product Characteristics (2010). Available at: http://www.xarelto.com.
  10. Kubitza D., Becka M., Voith B., et al. Safety, pharmacodynamics and pharmacokinetics of single doses of BAY 59-7939, an oral direct factor Xa inhibitor. Clin Pharmacol Ther 2005; 78:412-21.
  11. Kubitza D., Becka M., Wensing G., et al. Safety, pharmacodynamics and pharmacokinetics of BAY 59-7939 - an oral, direct Factor Xa inhibitor - after multiple dosing in healthy male subjects. Eur J Clin Pharmacol 2005;61:873-80.
  12. Perzborn E., Lange U. Rivaroxaban - an oral, direct Factor Xa inhibitor - inhibits tissue factor-mediated platelet aggregation. J Thromb Haemost 2007;5(2):Abstract P-W-642.
  13. Perzborn E., Strassburger J., Wilmen A., et al. Biochemical and pharmacologic properties of BAY 59-7939, an oral, direct Factor Xa inhibitor. Pathophysiol. Haemost. Thromb, 2004;33(2):Abstract PO079.
  14. Biemond B.J., Perzborn E., Friederich P.W., et al. Prevention and treatment of experimental thrombosis in rabbits with rivaroxaban (BAY 59-7939) - an oral, direct Factor Xa inhibitor. Thromb Haemost 2007;97:471-77.
  15. Perzborn E., Harwardt M. Direct Thrombin Inhibitors, but Not Factor Xa Inhibitors, Enhance Thrombin Formation in Human Plasma by Interfering with the Thrombin-Thrombomodulin-Protein C System. Blood (ASH Annual Meeting Abstracts). 2008; 112:Abstract 528.
  16. Kubitza D., Becka M., Mueck W., Zuehlsdorf M. The effect of extreme age, and gender, on the pharmacology and tolerability of rivaroxaban - an oral, direct Factor Xa inhibitor. Blood 2006;108:Abstract 905.
  17. Kubitza D., Becka M., Zuehlsdorf M., Mueck W. Body weight has limited influence on the safety, tolerability, pharmacokinetics, or pharmacodynamics of rivaroxaban (BAY 59-7939) in healthy subjects. J Clin Pharmacol 2007;47:218-26.
  18. European Medicines Agency (EMEA). CHMP Assessment Report for Xarelto. Available at: http://www.emea.europa.eu/humandocs/ PDFs/EPAR/xarelto/H-944-en6.pdf. 2008. Accessed January 14, 2010.
  19. Weinz C., et al. Pharmacokinetics of BAY 59-7939 - an oral, direct FactorXa inhibitor - in rats and dogs. Xenobiotica 2005;35:891-910.
  20. Graff J. Effects of the oral, direct Factor Xa inhibitor rivaroxaban on platelet-induced thrombin generation and prothrombinase activity. J Clin. Pharmacol 2007;47:1398-407.
  21. Weinz C., Schwarz T., Kubitza D., et al. Metabolism and excretion of rivaroxaban, an oral, direct Factor Xa inhibitor, in rats, dogs and humans. Drug Metab Dispos 2009;37:1056-64.
  22. Halabi A., Kubitza D., Zuehlsdorf M., et al. Effect of hepatic impairment on the pharmacokinetics, pharmacodynamics and tolerability of riva-roxaban - an oral, direct Factor Xa inhibitor. J Thromb Haemost 2007;5(2):Abstract P-M-635.
  23. Nutescu E., Chuatrisorn I., Hellenbart E. Drug and dietary interactions of warfarin and novel oral anticoagulants: an update. [Review]. J Thromb Thrombolysis 2011;31(3):326-43. doi: 10.1007/s11239-011-0561-1.
  24. Gnoth M.J., Buetehorn Ulf., Muenster U., et al. In vitro and in vivo P-glycoprotein transport characteristics of rivaroxaban. J Pharmacol and experim therapeutics, 2011;338(1);372-80.
  25. Kubitza D., Mueck W., Becka M. No interaction between rivaroxaban - a novel, oral, direct factor Xa inhibitor and atorvastatin. Pathophysiol Haemost Thromb 2008;36:A40.
  26. Kubitza D., Becka M., Zuehlsdorf M. No interaction between the novel, oral direct Factor Xa inhibitor BAY 59-7939 and digoxin. J Clin Pharmacol 2006;46:702.Abstract 11.
  27. Kubitza D., Becka M., Zuehlsdorf M., Mueck W. Effect of food, an antacid and the H2 antagonist ranitidine on the absorption of BAY 59-7939 (rivaroxaban), an oral, direct Factor Xa inhibitor, in healthy subjects. J Clin Pharmacol 2006;46:549-58.
  28. Moore K.T., Plotnikov A.N., Thyssen A., et al. Effect of multiple doses of omeprazole on the pharmacokinetics, pharmacodynamics and safety of a single dose of rivaroxaban. J Cardiovasc Pharmacol 2011;58(6):581-88.
  29. Kubitza D., Becka M., Mueck W., Zuehlsdorf M. Safety, tolerability, pharmacodynamics, and pharmacokinetics of rivaroxaban - an oral direct Factor Xa inhibitor - are not affected by aspirin. J Clin Pharmacol 2006;46:981-90.
  30. Kubitza D., Becka M., Mueck W., Zuehlsdorf M. Co-administration of rivaroxaban - a novel, oral, direct Factor Xa inhibitor - and clopidogrel in healthy subjects. Eur Heart J 2007;28(1):189. Abstract P1272.
  31. Smith S.A., Morrissey J.H. Thromboplastin composition affects the sensitivity of prothrombin time (PT) clotting tests to direct Factor Xa inhibitors. wabstractx. Blood (ASH Annual Meeting Abstracts) 2007;110:928.
  32. Barrett Y.C., Wang Z., Frost C., Shenker A. Clinical laboratory measurement of direct factor Xa inhibitors: anti-Xa assay is preferable to prothrombin time assay. Thromb Haemost 2010;104:1263-71.
  33. Samama M.M., Le Flem L., Guinet C., et al. Suitability of chromogenic anti-FXa methods to measure rivaroxaban in human plasma wabstractx. J Thromb Haemost 2009;7(2):693.
  34. Harenberg J., Erdle S., Marx S., Kramer R. Determination of rivaroxaban in human plasma samples. Semin Thromb Hemost, 2012;38(2): 178-84. doi: 10.1055/s-0032-1301415.
  35. Eriksson B.I., Borris L.C., Friedman R.J., et al. RECORD1 Study Group. Rivaroxaban versus enoxaparin for thromboprophylaxis after hip arthroplasty. N Engl J Med 2008; 358:2765-75.
  36. Kakkar A.K., Brenner B., Dahl O.E., et al. Extended duration rivaroxaban versus short-term enoxaparin for the prevention of venous thromboembolism after total hip arthroplasty: a double-blind, randomised controlled trial. Lancet 2008;372:31-9.
  37. Lassen M.R., Ageno W., Borris L.C., et al. Rivaroxaban versus enoxaparin for thromboprophylaxis after total knee arthroplasty. N Engl J Med 2008;358:2776-86.
  38. Turpie A.G., Lassen M.R., Davidson B.L., et al. Rivaroxaban versus enoxaparin for thromboprophylaxis after total knee arthroplasty (RECORD4): a randomised trial. Lancet 2009;373:1673-80.
  39. Patel M.R., Mahaffey K.W., Garg J., et al. Rivaroxaban versus warfarin in nonvalvular atrial fibrillation. [Comparative Study Multicenter Study Randomized Controlled Trial Research Support, Non-U.S. Gov't]. N Engl J Med 2011;365(10):883-91.
  40. Mega J.L., Braunwald E., Wiviott S., et al. Rivaroxaban in patients with a recent acute coronary syndrome. [Clinical Trial, Phase III Multicenter Study Randomized Controlled Trial Research Support, Non-U.S. Gov't]. N Engl J Med 2011;366(1):9-19.
  41. del Zoppo G.J., Eliasziw M. New Option in anticoagulation for atrial fibrillation. N Eng J Med 2011;365(10):952-53.
  42. Wallentin L., Yusuf S., Ezekowitz M.D., et al. On behalf of the RE-LY investigators. Efficacy and safety of dabigatran compared with warfarin at different levels of international normalised ratio control for stroke prevention in atrial fibrillation: an analysis of the RE-LY trial. Lancet 2010;376(9745):975-83.
  43. Инструкция по применению препарата Ксарелто. http://www.bayerpharma.ru/html/ pdf/instruction/ksarelto_spaf.pdf.

Supplementary files

Supplementary Files
Action
1. JATS XML
Download

Copyright (c) 2013 Bionika Media

This website uses cookies

You consent to our cookies if you continue to use our website.

About Cookies