Terpening Chris
Departments of Family Medicine and Clinical Pharmacy, West Virginia University-Charleston Division, Charleston, West Virginia, USA.
Clin Med Insights Cardiol. 2010 Dec 1;4:117-28. doi: 10.4137/CMC.S4323.
The thienopyridine antiplatelet agent clopidogrel is an effective drug for the prevention of vascular events. However, data has accumulated over time to suggest it is prone to significant interpatient variability. While there are several factors that contribute to this, one of the most important is variability in forming the active metabolite necessary for clopidogrel function. Several enzymes are involved in formation of this metabolite, and two, CYP2C19 and P-glycoprotein, appear to have alleles that both occur frequently in the population and have a clinically significant impact. Patients carrying these alleles can be identified, but it remains to be determined if this information is necessary or sufficient for risk stratification. Furthermore, if patients with high-risk alleles are identified, it is unclear how treatment should be adjusted.
噻吩并吡啶类抗血小板药物氯吡格雷是预防血管事件的有效药物。然而，随着时间的推移，积累的数据表明它易于出现显著的患者间变异性。虽然有几个因素导致了这种情况，但最重要的因素之一是形成氯吡格雷发挥作用所必需的活性代谢物的变异性。几种酶参与了这种代谢物的形成，其中两种，即细胞色素P450 2C19（CYP2C19）和P-糖蛋白，似乎具有在人群中频繁出现且具有临床显著影响的等位基因。携带这些等位基因的患者可以被识别出来，但这种信息对于风险分层是否必要或充分仍有待确定。此外，如果识别出具有高危等位基因的患者，尚不清楚应如何调整治疗。
