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比伐卢定的临床药理学。

Clinical pharmacology of bivalirudin.

作者信息

Reed Michael D, Bell Dawn

机构信息

Case Western Reserve University School of Medicine, Cleveland, Ohio, USA.

出版信息

Pharmacotherapy. 2002 Jun;22(6 Pt 2):105S-111S. doi: 10.1592/phco.22.10.105s.33616.

DOI:10.1592/phco.22.10.105s.33616
PMID:12064567
Abstract

Much progress has been made in understanding and treating acute coronary syndromes. For patients undergoing percutaneous transluminal coronary angioplasty, anticoagulant therapy during the procedure must strike a balance between providing sufficient anticoagulation to prevent thrombus formation and ischemic complications while averting hemorrhagic complications. Bivalirudin, a thrombin-specific anticoagulant, is the only anticoagulant that reduces both ischemic and bleeding complications associated with percutaneous coronary intervention (PCI). Bivalirudin is easy to use, provides predictable anticoagulation, inactivates both free and clot-bound thrombin, and blocks thrombin-mediated platelet activation and aggregation. Drug-drug interaction studies have found no clinically relevant interactions between bivalirudin and ticlopidine, abciximab, tirofiban, or eptifibatide. Bivalirudin is well tolerated by patients who previously received low-molecular-weight heparin (LMWH), when LMWH is discontinued 8-14 hours before bivalirudin is started. Similarly, switching from heparin to bivalirudin at the time of PCI reduces both ischemic and bleeding events.

摘要

在急性冠状动脉综合征的认识和治疗方面已经取得了很大进展。对于接受经皮腔内冠状动脉成形术的患者,手术期间的抗凝治疗必须在提供足够的抗凝以预防血栓形成和缺血性并发症,同时避免出血性并发症之间取得平衡。比伐卢定,一种凝血酶特异性抗凝剂,是唯一能减少与经皮冠状动脉介入治疗(PCI)相关的缺血性和出血性并发症的抗凝剂。比伐卢定使用方便,能提供可预测的抗凝效果,可使游离和与凝块结合的凝血酶失活,并阻断凝血酶介导的血小板活化和聚集。药物相互作用研究发现比伐卢定与噻氯匹定、阿昔单抗、替罗非班或依替巴肽之间不存在临床相关的相互作用。当在开始使用比伐卢定前8 - 14小时停用低分子量肝素(LMWH)时,先前接受过LMWH的患者对比伐卢定耐受性良好。同样,在PCI时从肝素转换为比伐卢定可减少缺血性和出血性事件。

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