Low-dose ticagrelor yields an antiplatelet efficacy similar to that of standard-dose ticagrelor in healthy subjects: an open-label randomized controlled trial.
Low-dose ticagrelor yields an antiplatelet efficacy similar to that of standard-dose ticagrelor in healthy subjects: an open-label randomized controlled trial.
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在健康受试者中，低剂量替格瑞洛的抗血小板功效与标准剂量替格瑞洛相似：一项开放标签随机对照试验。
DOI：
10.1038/srep31838
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发表时间：
2016-08-24
影响因子：
4.6
通讯作者：
Ma L
中科院分区：
文献类型：
--
作者：
Li P;Gu Y;Yang Y;Chen L;Liu J;Gao L;Qin Y;Cai Q;Zhao X;Wang Z;Ma L
替格瑞洛的抗血小板疗效高于氯吡格雷，但可能伴有出血风险增加。本研究评价了低剂量替格瑞洛在中国健康志愿者中的抗血小板作用和药代动力学特征。30例健康受试者随机接受标准剂量替格瑞洛（180 mg负荷剂量，90 mg每日两次[bid] [n = 10]）、低剂量替格瑞洛（90 mg负荷剂量，45 mg bid [n = 10]）或氯吡格雷（600 mg负荷剂量，75 mg每日一次[n = 10]）。在基线和给药后0.5、1、2、4、8、24、48和72小时，使用VerifyNow P2 Y12测定评估血小板反应性。测量替格瑞洛和AR-C124910 XX浓度用于药代动力学分析。在给药后0.5、1、2、4、8和48小时，低剂量和标准剂量替格瑞洛组的P2 Y12反应单位抑制百分比高于氯吡格雷组（均P < 0.05），但在任何时间点，两种替格瑞洛剂量之间均无显著差异（P > 0.05）。标准剂量的替格瑞洛和ARC 124910 XX的血浆浓度比低剂量的替格瑞洛高约2倍。未报告严重不良事件。总之，低剂量替格瑞洛对中国健康受试者血小板功能的抑制作用比氯吡格雷更快、更强，抗血小板疗效与标准剂量替格瑞洛相似。
Ticagrelor has a greater antiplatelet efficacy than clopidogrel but may be accompanied by an increased risk of bleeding. This study evaluated the antiplatelet effect and pharmacokinetic profile of low-dose ticagrelor in healthy Chinese volunteers. Thirty healthy subjects were randomized to receive standard-dose ticagrelor (180-mg loading dose, 90-mg twice daily [bid] [n = 10]), low-dose ticagrelor (90-mg loading dose, 45-mg bid [n = 10]), or clopidogrel (600-mg loading dose, 75-mg once daily [n = 10]). Platelet reactivity was assessed by using the VerifyNow P2Y12 assay at baseline and 0.5, 1, 2, 4, 8, 24, 48, and 72 hours post-dosing. The ticagrelor and AR-C124910XX concentrations were measured for pharmacokinetic analysis. The percentage inhibition of P2Y12 reaction units was higher in the low-dose and standard-dose ticagrelor group than in the clopidogrel group at 0.5, 1, 2, 4, 8, and 48 hours post-dosing (P < 0.05 for all), but did not differ significantly between the two ticagrelor doses at any time-point (P > 0.05). The plasma ticagrelor and ARC124910XX concentrations were approximately 2-fold higher with standard-dose versus low-dose ticagrelor. No serious adverse events were reported. In conclusion, low-dose ticagrelor achieved faster and higher inhibition of platelet functions in healthy Chinese subjects than did clopidogrel, with an antiplatelet efficacy similar to that of standard-dose ticagrelor.