新型口服抗凝血剂达比加群酯的研究进展

华法林是大多数国家长期抗凝的主要药物之一。华法林虽然可以口服给药,但其治疗范围狭窄,必须严格掌握治疗指征。此外华法林与其他药物相互作用大,个体差异较大,治疗期间需严密观察病情,并依据国际标准化比率随时调整用量。在近几年中许多新的抗凝血剂已经开发出来。达比加群酯是一种新型口服的直接凝血酶抑制剂。本研究综述了达比加群酯的临床研究进展及潜在适应证,为该药物的临床应用提供依据。     

从房颤缺血性脑卒中的药物预防和治疗看口服抗凝剂的进展

本文通过汇总分析华法林、利伐沙班和达比加群酯等的上市情况、药动学参数、代谢特点和临床研究数据等,介绍了预防和治疗房颤缺血性脑卒中的口服抗凝剂的研究进展.结果表明,利伐沙班和达比加群酯无需监测INR值和个体化调整剂量,即可达到抗凝、预防缺血性脑卒中的作用,且不会增加大出血的风险.随着更加科学完善的临床试验的完成和结论得出,利伐沙班和达比加群酯将在抗凝治疗中占据一席之地,华法林的主导地位也将受到一定影响.     

Monitoring anticoagulant therapy with new oral agents

Thromboembolic disease is a major leading cause of mortality and morbidity in industrialized countries. Currently, the management of these patients is challenging due to the availability of new drugs with proven efficacy and security compared to traditional oral vitamin K antagonists. These compounds are characterized by a predictable pharmacokinetic profile for which blood monitoring is not routinely needed. Nevertheless, some data have suggested inter-patient variability in the anticoagulant effect of these drugs, raising concerns about their effectiveness and safety. Although mass-spectrometry is the gold standard to determine drug plasma concentrations, this method is not widely available in every-day practice and some coagulation assays are commonly used to determine the anticoagulant effect of these drugs. The present review aims to summarize the current knowledge regarding the clinical question of how and when to monitor patients with new anticoagulant oral agents.     

Oral Anticoagulant Use After Bariatric Surgery: A Literature Review and Clinical Guidance

Bariatric surgery may alter the absorption, distribution, metabolism, or elimination (disposition) of orally administered drugs via changes to the gastrointestinal tract anatomy, body weight, and adipose tissue composition. As some patients who have undergone bariatric surgery will need therapeutic anticoagulation for various indications, appropriate knowledge is needed regarding anticoagulant drug disposition and resulting efficacy and safety in this population. We review general considerations about oral drug disposition in patients after bariatric surgery, as well as existing literature on oral anticoagulation after bariatric surgery. Overall, available evidence on therapeutic anticoagulation is very limited, and individual drug studies are necessary to learn how to safely and effectively use the direct oral anticoagulants. Given the sparsity of currently available data, it appears most prudent to use warfarin with international normalized ratio monitoring, and not direct oral anticoagulants, when full-dose anticoagulation is needed after bariatric surgery.     

达比加群/华法林联合益气活血中药治疗心房颤动合并急性冠状动脉综合征的临床疗效观察

目的探讨达比加群/华法林联合益气活血中药治疗心房颤动合并急性冠状动脉综合征的临床疗效。方法选取首都医科大学附属北京天坛医院2014年10月—2017年10月心房颤动合并急性冠脉综合征患者168例,采用随机数字表法分为两组,对照组84例采用华法林联合益气活血中药治疗,观察组84例采用达比加群联合益气活血中药治疗,于治疗前后行凝血功能、血脂指标检测,记录两组患者栓塞事件和出血事件发生情况,比较两组患者治疗效果及药物不良反应发生情况。结果与本组治疗前比较,两组治疗后凝血酶原时间(PT)、活化部分凝血活酶时间(APTT)、凝血酶时间(TT)、D-二聚体(D-D)、血浆纤维蛋白原降解产物(FDP)、总胆固醇(TC)、甘油三酯(TG)、低密度脂蛋白胆固醇(LDL-C)显著降低;高密度脂蛋白胆固醇(HDL-C)显著增加(P<0.05)。观察组治疗后PT、APTT、TT、D-二聚体、FDP、TC、TG、LDL-C均低于对照组,HDL-C高于对照组(P<0.05)。观察组栓塞事件发生率、出血事件发生率、药物不良反应发生率均低于对照组(P<0.05)。观察组预后好于对照组(P<0.05)。结论达比加群/华法林联合益气活血中药均可用于心房颤动合并急性冠脉综合征患者的临床治疗,达比加群联合益气活血中药疗效更佳,可显著改善患者的凝血功能和血脂状况,值得临床推广使用。     

达比加群酯对非瓣膜性房颤患者抗凝治疗效果及安全性的Meta分析

目的评价达比加群酯对非瓣膜性房颤患者抗凝治疗的效果及安全性。方法检索有关达比加群酯对非瓣膜性房颤患者抗凝治疗的随机对照试验及多中心对照研究等文献,并进行质量评估,采用RevMan 5.2对符合条件的研究进行Meta分析,评价达比加群酯对非瓣膜性房颤患者的抗凝效果及安全性。结果符合纳入标准的文献共7篇(中文1篇,英文6篇),总样本量为33 502例。Meta分析显示,与华法林比较,达比加群酯明显降低房颤患者脑卒中发生率(OR=0.82,95%CI 0.73⁰.93,P=0.001)、全因出血率(OR=0.86,95%CI 0.790.93,P=0.001)、全因出血率(OR=0.86,95%CI 0.79⁰.95,P=0.003)及颅内出血发生率(OR=0.42,95%CI 0.290.95,P=0.003)及颅内出血发生率(OR=0.42,95%CI 0.29⁰.62,P=0.001);而动脉栓塞率(OR=0.75,95%CI 0.450.62,P=0.001);而动脉栓塞率(OR=0.75,95%CI 0.45¹.25,P=0.28)及全因死亡率(OR=0.91,95%CI 0.821.25,P=0.28)及全因死亡率(OR=0.91,95%CI 0.82¹.00,P=0.06)无明显差异。结论达比加群酯可有效降低房颤患者脑卒中、全因出血及颅内出血的风险,疗效优于传统药物华法林且安全性高。     

新型抗凝药物防治静脉血栓栓塞症的研究进展

静脉血栓栓塞症(VTE)是由多种遗传性和获得性危险因素共同作用的结果,抗凝治疗是预防和治疗VTE的基础.传统抗凝药物如低分子肝素和华法林防治VTE的有效性已被临床实践充分证实,但其缺点也不容忽视.近年来新型抗凝药物如利伐沙班、阿哌沙班和达比加群等在预防和治疗VTE领域进行了大量临床研究,其安全性与有效性均得到证实,为临床医师治疗VTE提供了更多的选择.