Cardiology Unit, Department of Medicine and Cardiovascular Research Unit, University of Vermont, Burlington, VT 05446, USA.
Br J Clin Pharmacol. 2011 Oct;72(4):672-82. doi: 10.1111/j.1365-2125.2010.03879.x.
Glycoprotein (GP) IIb-IIIa antagonists inhibit the aggregation of activated platelets. Three agents are approved for clinical use. In this review, the characteristics of each agent, their pharmacodynamic profile, results in pivotal clinical trials and the associated clinical implications are discussed. GP IIb-IIIa antagonists have greatest benefit when used as adjunctive therapy during percutaneous coronary intervention (PCI) when the patient has intra-coronary thrombosis. These agents appear to provide greatest benefit when used in combination with heparin. The clinical niche for parenteral GP IIb-IIIa antagonists is evolving. The rapid onset and offset of GP IIb-IIIa antagonists plus dosing designed to inhibit extensively platelet aggregation differentiates them from oral agents. The contemporary niche appears to include patients in transition, such as individuals requiring emergent PCI before oral agents are fully active and for unstable patients requiring transport to PCI centres, particularly in patients likely to have intracoronary thrombus. Subsequent studies should evaluate the optimal duration of therapy with GP IIb-IIIa antagonists.
糖蛋白 (GP) IIb-IIIa 拮抗剂可抑制激活血小板的聚集。有三种药物已被批准用于临床。在这篇综述中，讨论了每种药物的特点、药代动力学特征、主要临床试验结果及其相关的临床意义。当患者发生冠状动脉内血栓时，GP IIb-IIIa 拮抗剂在经皮冠状动脉介入治疗 (PCI) 时作为辅助治疗最有效。这些药物与肝素联合使用时似乎效果最佳。静脉内 GP IIb-IIIa 拮抗剂的临床应用正在发展。GP IIb-IIIa 拮抗剂起效迅速、作用时间短，且设计用于抑制广泛的血小板聚集，这使其与口服药物有所区别。目前，这类药物似乎适用于过渡阶段的患者，如需要紧急 PCI 治疗且口服药物尚未完全起效的患者，以及需要转运至 PCI 中心的不稳定患者，尤其是那些可能存在冠状动脉内血栓的患者。后续研究应评估 GP IIb-IIIa 拮抗剂治疗的最佳持续时间。
