Wooster M B, Luzier A B
Department of Pharmacy Practice, State University of New York at Buffalo 14260, USA.
Ann Pharmacother. 1999 Mar;33(3):318-24. doi: 10.1345/aph.18006.
To summarize the published data on reteplase, the most recent thrombolytic agent approved by the Food and Drug Administration for use in the management of acute myocardial infarction in adults.
Published data on reteplase identified by MEDLINE searches (January 1985-June 1997), as well as other pertinent literature.
Reteplase is a new thrombolytic agent derived from human tissue plasminogen activator. Its mechanism of action is similar to that of alteplase, but it differs in pharmacokinetic and pharmacodynamic properties. Certain structural changes contribute to differences in pharmacokinetic properties such as a prolonged half-life (15 min), which allows it to be administered as two 10-MU bolus injections. Reteplase has been shown to have fibrin specificity similar to that of alteplase, but with a lower binding affinity for fibrin. This enables reteplase to bind to the thrombus repeatedly and increases its fibrinolytic potential. In clinical trials, reteplase demonstrated more rapid and complete coronary patency compared with alteplase, without a significant increase in clinical adverse events. However, the improvement in coronary artery patency with reteplase versus alteplase did not result in a reduction in mortality in the GUSTO III trial.
Despite evidence that use of reteplase results in an improved coronary artery patency rate versus accelerated infusion alteplase, an improvement in mortality rate with reteplase was not shown. Reteplase may have an advantage over alteplase due to a more rapid and simpler dosing regimen, but the significance of this difference is yet to be determined.
总结有关瑞替普酶的已发表数据。瑞替普酶是美国食品药品监督管理局批准用于治疗成人急性心肌梗死的最新溶栓药物。
通过MEDLINE检索（1985年1月至1997年6月）以及其他相关文献确定的关于瑞替普酶的已发表数据。
瑞替普酶是一种源自人组织纤溶酶原激活剂的新型溶栓药物。其作用机制与阿替普酶相似，但在药代动力学和药效学特性方面有所不同。某些结构变化导致药代动力学特性存在差异，例如半衰期延长（15分钟），这使得它可以通过两次10MU静脉推注给药。已证明瑞替普酶具有与阿替普酶相似的纤维蛋白特异性，但对纤维蛋白的结合亲和力较低。这使得瑞替普酶能够反复与血栓结合并增加其纤溶潜力。在临床试验中，与阿替普酶相比，瑞替普酶显示出更快速和完全的冠状动脉再通，且临床不良事件没有显著增加。然而，在GUSTO III试验中，瑞替普酶与阿替普酶相比，冠状动脉再通的改善并未导致死亡率降低。
尽管有证据表明使用瑞替普酶与加速输注阿替普酶相比可提高冠状动脉再通率，但未显示瑞替普酶能降低死亡率。由于给药方案更快速和简单，瑞替普酶可能比阿替普酶具有优势，但这种差异的意义尚待确定。
