Gratsianskiĭ N A
Kardiologiia. 2010;50(6):4-21.
Standard double antiplatelet therapy (aspirin plus clopidogrel) used in patients with coronary artery disease during acute coronary syndromes (ACS) and/or in conjunction with percutaneous coronary interventions (PCI) has some limitations. Relatively large proportion of patients has "laboratory" resistance to clopidogrel - an essential component of standard therapy. Basic weakness of this agent is necessity to be converted into active metabolite by CYP 450 enzymes. Other drugs potentially interfere with this conversion. The puzzle of clinical value of obvious laboratory interaction of clopidogrel with its conjecturally almost obligatory companions proton pump inhibitors is still unresolved. It has been shown recently that loss of function alleles of some CYP450 genes especially CYP2C19*2 are responsible for reduced reaction of platelets to clopidogrel. Detection of this allele is possible. However practical application of such genetic testing is subject of disagreement among experts. Another way for therapy guidance is use of platelet function testing. But at present there is no agreement concerning preferable test. Studies aimed at clarification of practical role of some laboratory test are close to completion. Recognition of resistance by any method calls forth administration of higher doses of clopidogrel or use of novel agents. CURRENT trial has recently demonstrated advantages of clopidogrel double dose in ACS patients subjected to PCI. Novel P2Y12 receptor inhibitors prasugrel and ticagrelor have been shown to be superior to clopidogrel in large randomized trials. Direct P2Y12 antagonist ticagrelor seems to be especially attractive because of effect on total mortality and acceptable rate of bleeding. Among agents under study thrombin receptor blockers appear most promising.
标准双联抗血小板治疗(阿司匹林加氯吡格雷)用于急性冠状动脉综合征(ACS)期间的冠心病患者和/或与经皮冠状动脉介入治疗(PCI)联合使用时存在一些局限性。相当大比例的患者对氯吡格雷(标准治疗的重要组成部分)存在“实验室”抵抗。这种药物的基本弱点是需要通过CYP 450酶转化为活性代谢物。其他药物可能会干扰这种转化。氯吡格雷与其推测几乎必不可少的伴侣质子泵抑制剂之间明显的实验室相互作用的临床价值之谜仍未解决。最近有研究表明,某些CYP450基因尤其是CYP2C19*2的功能缺失等位基因是导致血小板对氯吡格雷反应降低的原因。检测这种等位基因是可行的。然而,这种基因检测的实际应用在专家之间存在分歧。另一种指导治疗的方法是使用血小板功能检测。但目前对于哪种检测方法更优尚无定论。旨在阐明某些实验室检测实际作用的研究已接近完成。通过任何方法识别出抵抗后,都需要加大氯吡格雷剂量或使用新型药物。CURRENT试验最近证明了在接受PCI的ACS患者中双倍剂量氯吡格雷的优势。新型P2Y12受体抑制剂普拉格雷和替卡格雷在大型随机试验中已显示出优于氯吡格雷。直接P2Y12拮抗剂替卡格雷因其对总死亡率的影响和可接受的出血率似乎特别有吸引力。在正在研究的药物中,凝血酶受体阻滞剂似乎最有前景。