Characteristics of novel anticoagulants marketed in China and the development of their clinical application
YOU Guo-jiaoa, DU Li-pinga, CHEN Yue-xinb*,MEI Dana*
a. Department of pharmacy; b. Department of vascular surgery, Peking Union Medical College Hospital, Chinese Academy of Medical Sciences,Beijing 100730, China
Abstract:Objective: To provide references for the clinical use of new anticoagulants. Methods: The characteristics of new anticoagulants were reviewed, clinical trial results were referred, and the update antithrombotic therapy guidelines were interpreted. Results: The effects of traditional anticoagulants (heparin, low molecular weight heparin and warfarin) are clear and reliable, but these drugs still have their own drawbacks. In contrast, new anticoagulants have more stable pharmacokinetic properties and fewer drug-drug/ food interactions, which make them safer and more convenient. Conclusion: New anticoagulants show more advantages compared with the traditional anticoagulants, and have brought new choices for the treatments of thromboembolic disease, atrial fibrillation and coronary heart disease.
尤国皎, 都丽萍, 陈跃鑫, 梅丹. 我国已上市新型抗凝药物的特点及临床应用进展[J]. 临床药物治疗杂志, 2017, 15(1): 1-7.
YOU Guo-jiao, DU Li-ping, CHEN Yue-xin,MEI Dan. Characteristics of novel anticoagulants marketed in China and the development of their clinical application. CLINICAL MEDICATION JOURNAL, 2017, 15(1): 1-7.
[1] Mastroiacovo D, Sala G, Dentali F. The safety of fondaparinux sodium for the treatment of venous thromboembolism [J]. Expert Opin Drug Saf, 2016, 15(9): 1259-1265.
[2] Bauer K A. Fondaparinux sodium: a selective inhibitor of factor Xa[J]. Am J Health- Syst Ph, 2001, 58(Suppl 2):S14-S17.
[3] Fareed J, Jeske W P. Small-molecule direct antithrombins: argatroban [J]. Best Pract& Res Clin Ha, 2004, 17(1):127-138.
[4] Van Ryn J, Stangier J, Haertter S, et al. Dabigatran etexilate-a novel, reversible, oral direct thrombin inhibitor: interpretation of coagulation assays and reversal of anticoagulant activity[J].Thromb Haemostasis, 2010, 103(6):1116-1127.
[5] Schulman S, Crowther M A. How I treat with anticoagulants in 2012: new and old anticoagulants, and when and how to switch [J]. Blood, 2012, 119(13):3016-3023.
[6] Perzborn E, Roehrig S, Straub A, et al. Rivaroxaban: anew oral factor Xainhibitor[J]. Arterioscl Throm Vas, 2010, 30(3): 376-381.
[7] Samama M M. The mechanism of action of rivaroxaban-an oral, direct factor Xa inhibitor-compared with other anticoagulants[J]. Thromb Res, 2011,127(6): 497-504.
[8] Lip G Y, Larsen TB, Skj?th F, et al. Indirect comparisons of new oral anticoagulant drugs for efficacy and safety when used for stroke prevention in atrial fibrillation [J]. J Am Coll Cardiol, 2012, 60(8): 738-746.
[9] Baber U, Mastoris I, Mehran R. Balancing ischaemia and bleeding risks with novel oral anticoagulants[J]. Nat Rev Cardiol, 2014,11(12): 693-703.
[10] Sharma M, Corneliu V R, Patel J P, et al. Efficacy and harms of direct oral anticoagulants in the elderly for stroke prevention in atrial fibrillation and secondary prevention of venous thromboembolism CLINICAL PERSPECTIVE: systematic review and meta-analysis[J]. Circulation, 2015, 132(3): 194-204.
[11] 周建光,周颖奇. 新型口服抗凝药的特点和临床研究[J]. 临床药物治疗杂志, 2013, 11(5): 8-14.
[12] 邓文宁,马长生. 临床规范使用新型抗凝药物[J]. 中国循环杂志, 2013, 28(6):404-407.
[13] 中华心血管病杂志血栓循证工作组. 非瓣膜病心房颤动患者应用新型口服抗凝药物中国专家共识[J]. 中华心血管病杂志, 2014, 42(5):362-369.
[14] Stangier J. Clinical pharmacokinetics and pharmacodynamics of the oral direct thrombin inhibitor dabigatran etexilate[J]. Clin Pharmacokinet, 2008, 47(5):285-295.
[15] Stangier J, Rathgen K, St?hle H, et al. The pharmacokinetics, pharmacodynamics and tolerability of dabigatran etexilate, a new oral direct thrombin inhibitor, in healthy male subjects[J]. Brit J Clin Pharmaco, 2007, 64(3): 292-303.
[16] Esmon C T. Targeting factor Xa and thrombin: impact on coagulation and beyond[J].Thromb Haemostasis, 2013, 111(4): 625-633.
[17] Clive K, Elie A, Joseph O, et al. Antithrombotic therapy for VTE disease CHEST guideline and expert panel report[J]. Chest, 2016, 149(2): 315-352.
[18] 中华医学会外科学分会血管外科学组. 深静脉血栓形成的诊断和治疗指南(第二版)[J]. 中华普通外科杂志, 2012, 27(7): 605-607.
[19] 中华医学会心血管病学分会肺血管病学组. 急性肺栓塞诊断与治疗中国专家共识(2015)[J]. 中华心血管病杂志, 2016, 44(3): 197-211.
[20] 中华医学会骨科学分会. 中国骨科大手术静脉血栓栓塞症预防指南[J]. 中华骨科杂志, 2016, 36(2): 65-71.
[21] January C T, Wann L S, Alpert J S, et al. 2014 AHA/ACC/HRS Guideline for the management of patients with atrial fibrillation[J]. J Am Coll Cardiol, 2014, 64(21): e1-e76.
[22] Kirchhof P, Benussi S,Kotecha D, et al. 2016 ESC Guidelines for the management of atrial fibrillation developed in collaboration with EACTS[J]. Europace, 2016, 18(11): 1609-1678.
[23] 中华医学会心电生理和起搏分会、中国医师协会心率学专业委员会心房颤动防治专家工作委员会. 心房颤动:目前的认识和治疗建议-2015[J]. 中华心律失常学杂志, 2015, 19(5): 321-384.
[24] Kirchhof P, Benussi S, Kotecha D, et al. 2016 ESC Guidelines for the management of atrial fibrillation developed in collaboration with EACTS: The Task Force for the management of atrial fibrillation of the European Society of Cardiology (ESC)Developed with the special contribution of the European Heart Rhythm Association (EHRA) of the ESCEndorsed by the European Stroke Organisation (ESO)[J]. Eur Heart J, 2016, ehw210.
[25] Heidbuchel H, Verhamme P, Alings M, et al. European Heart Rhythm Association Practical Guide on the use of new oral anticoagulants in patients with non-valvular atrial fibrillation[J]. Europace, 2013, 15(5): 625-651.
[26] 胡大一,郭艺芳. 心房颤动抗凝治疗中国专家共识[J]. 心脑血管病防治, 2012, 12(3): 173-177.
[27] Roffi M, Patrono C, Collet J P, et al. 2015 ESC Guidelines for the management of acute coronary syndromes in patients presenting without persistent ST-segment elevation: Task Force for the Management of Acute Coronary Syndromes in Patients Presenting without Persistent ST-Segment Elevation of the European Society of Cardiology (ESC)[J]. Eur Heart J, 2016, 37(3): 267-315.
[28] 中华医学会心血管病学分会. 不稳定性心绞痛和非ST 段抬高心肌梗死诊断与治疗指南[J]. 中华心血管病杂志, 2007, 35(4): 295- 304.
[29] Levine G N, Bates E R, Blankenship J C, et al. 2015 ACC/AHA/SCAI Focused Update on Primary Percutaneous Coronary Intervention for Patients With ST-Elevation Myocardial Infarction[J]. J Am Coll Cardiol, 2016, 67(10): 1235-1250.
[30]Task Force on the management of ST-segment elevation acute myocardial infarction of the European Society of Cardiology (ESC). ESC Guidelines for the management of acute myocardial infarction in patients presenting with ST-segment elevation [J].Eur Heart J, 2012, 33(20): 2569-2619.
[31] 中华医学会心血管病学分会. 急性ST 段抬高型心肌梗死诊断和治疗指南[J]. 中华心血管病杂志, 2015, 43(5): 380-393.
[32] Mega J L, Braunwald E, Wiviott S D, et al.Rivaroxaban in patients with a recent acute coronary syndrome[J].N Engl J Med, 2012, 366(1):9-19.
[33] Linkins L A, Dans A L, Moores L K, et al. Treatment and prevention of heparin-induced thrombocytopenia: Antithrombotic Therapy and Prevention of Thrombosis, 9th ed: American College of Chest Physicians Evidence-Based Clinical Practice Guidelines[J]. Chest, 2012, 141(Suppl 2): e495S–e530S.
[34] Watson H, Davidson S, Keeling D. Guidelines on the diagnosis and management of heparin-induced thrombocytopenia: second edition[J]. Brit J Haematol, 2012, 159(5):528-540.
[35] 郭梦园, 赵志刚, 孙树森, 等. 新型口服抗凝药与华法林临床应用的比较[J]. 药品评价, 2015, (4):24-29.