LaMonte Marian P, Brown Philip M, Hursting Marcie J
University of Maryland School of Medicine, Baltimore, MD 21201-1595, USA.
Expert Rev Cardiovasc Ther. 2005 Jan;3(1):31-41. doi: 10.1586/14779072.3.1.31.
Argatroban, a direct thrombin inhibitor, effectively inhibits free and clot-bound thrombin without the need of a cofactor and exerts dose-dependent anticoagulant effects that are rapidly active and rapidly reversible (elimination half-life: 39-51 min). Argatroban provides predictable parenteral anticoagulation and is well tolerated with an acceptably low bleeding risk in a variety of clinical settings, including heparin-induced thrombocytopenia, acute ischemic stroke, percutaneous coronary intervention and hemodialysis. This review will discuss the clinical pharmacology and utility of argatroban; in particular, clinical trial experiences will be discussed in patients with, or at risk of, heparin-induced thrombocytopenia (where heparins must be avoided) including those requiring hemodialysis or percutaneous coronary intervention, and in patients with acute ischemic stroke (where heparins are not generally recommended).
阿加曲班是一种直接凝血酶抑制剂,可有效抑制游离和与凝块结合的凝血酶,无需辅助因子,并发挥剂量依赖性抗凝作用,起效迅速且作用可逆(消除半衰期:39 - 51分钟)。阿加曲班可提供可预测的肠外抗凝作用,在包括肝素诱导的血小板减少症、急性缺血性中风、经皮冠状动脉介入治疗和血液透析在内的各种临床环境中,耐受性良好,出血风险低至可接受程度。本综述将讨论阿加曲班的临床药理学和应用;特别是,将讨论肝素诱导的血小板减少症患者或有该风险的患者(必须避免使用肝素)(包括需要血液透析或经皮冠状动脉介入治疗的患者)以及急性缺血性中风患者(一般不推荐使用肝素)的临床试验经验。