ИНГИБИТОР ФАКТОРА Ха СВЕРТЫВАЕМОСТИ КРОВИ РИВАРОКСАБАН ПРИ МЕРЦАТЕЛЬНОЙ АРИТМИИ
- Авторы: Зотова И.В1, Затейщиков Д.А1
-
Учреждения:
- Учебно-научный медицинский центр УД Президента РФ, Москва
- Выпуск: № 9 (2013)
- Страницы: 35-41
- Раздел: Статьи
- URL: https://journals.eco-vector.com/2073-4034/article/view/281371
- ID: 281371
Цитировать
Полный текст
Аннотация
В статье представлены данные, касающиеся первого дошедшего до клинического использования ингибитора фактора Ха свертываемости крови ривароксабана. Освещены фармакодинамика и фармакокинетика препарата, его лекарственные взаимодействия, клинические аспекты применения. Проанализированы результаты крупного рандомизированного исследования III фазы ROCKET-AF, в котором изучалась эффективность ривароксабана по сравнению с варфарином. На основании результатов этого исследования ривароксабан был зарегистрирован в России в качестве профилактики развития тромбоэмболических осложнений у больных мерцательной аритмией как альтернатива варфарину.
Полный текст

Об авторах
И. В Зотова
Учебно-научный медицинский центр УД Президента РФ, Москва
Д. А Затейщиков
Учебно-научный медицинский центр УД Президента РФ, Москвад.м.н., профессор
Список литературы
- 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.
- 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.
- Gailani D., Renne Т. Intrinsic pathway of coagulation and arterial thrombosis. Arterioscler Thromb Vasc Biol 2007;27:2507-13.
- 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.
- 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.
- 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.
- 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.
- 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.
- Xarelto. Summary of Product Characteristics (2010). Available at: http://www.xarelto.com.
- 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.
- 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.
- 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.
- 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.
- 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.
- 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.
- 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.
- 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.
- 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.
- Weinz C., et al. Pharmacokinetics of BAY 59-7939 - an oral, direct FactorXa inhibitor - in rats and dogs. Xenobiotica 2005;35:891-910.
- 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.
- 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.
- 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.
- 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.
- 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.
- 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.
- 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.
- 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.
- 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.
- 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.
- 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.
- 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.
- 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.
- 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.
- 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.
- 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.
- 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.
- 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.
- 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.
- 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.
- 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.
- del Zoppo G.J., Eliasziw M. New Option in anticoagulation for atrial fibrillation. N Eng J Med 2011;365(10):952-53.
- 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.
- Инструкция по применению препарата Ксарелто. http://www.bayerpharma.ru/html/ pdf/instruction/ksarelto_spaf.pdf.
Дополнительные файлы
