Fareed Jawed, Jeske Walter P, Hoppensteadt Debra A, Walenga Jeanine M
Stritch School of Medicine, Loyola University Chicago, 2160 South First Avenue, Maywood, IL 60153, USA.
Future Cardiol. 2006 Jul;2(4):403-14. doi: 10.2217/14796678.2.4.403.
The small molecule, arginomimetic drug argatroban is the first synthetic direct antithrombin to be approved for clinical use. Argatroban reversibly binds to and inhibits both soluble and clot-bound thrombin. In contrast to other direct thrombin inhibitors, argatroban upregulates nitric oxide, enhancing its antithrombotic effect, does not generate antibodies, is not susceptible to degradation by proteases and is hepatically cleared. It has a predictable anticoagulant effect. Argatroban has proven efficacy and safety for prophylaxis and treatment of patients with thrombosis associated with heparin-induced thrombocytopenia (HIT), and for percutaneous coronary intervention in HIT and non-HIT patients. Pilot studies suggest that further investigations to establish the use of argatroban in ischemic stroke, acute coronary syndrome, hemodialysis, blood oxygenation, off-pump cardiac surgery and other clinical indications are warranted.
小分子类拟精氨酸药物阿加曲班是首个被批准用于临床的合成直接凝血酶抑制剂。阿加曲班可逆性地结合并抑制可溶性和凝块结合性凝血酶。与其他直接凝血酶抑制剂不同，阿加曲班可上调一氧化氮，增强其抗血栓形成作用，不会产生抗体，不易被蛋白酶降解，且经肝脏清除。它具有可预测的抗凝作用。阿加曲班已被证明在预防和治疗与肝素诱导的血小板减少症（HIT）相关的血栓形成患者以及HIT和非HIT患者的经皮冠状动脉介入治疗中具有疗效和安全性。初步研究表明，有必要进一步开展研究以确定阿加曲班在缺血性中风、急性冠状动脉综合征、血液透析、血液氧合、非体外循环心脏手术及其他临床适应症中的应用。
