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首页> 外文期刊>The Journal of Clinical Pharmacology: Official Journal of the American College of Clinical Pharmacology >Effect of Brivaracetam on CYP3A Activity, Measured by Oral Midazolam
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Effect of Brivaracetam on CYP3A Activity, Measured by Oral Midazolam

机译：口服咪达唑仑测定的布立西坦对CYP3A活性的影响

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摘要

Brivaracetam is a synaptic vesicle protein 2A ligand in phase III development for epilepsy. A phase I, open-label, randomized study was conducted in 42 healthy male participants to assess the effect of brivaracetam on CYP3A activity using midazolam as a probe. Participants were randomized to oral brivaracetam 5, 50, or 150mg/day from Day 8 to Day 14. A single oral dose (7.5mg) of midazolam was administered on Days 1, 13, and 20, and full pharmacokinetic profiles were obtained. For all brivaracetam doses, the areas under the plasma concentration-time curves from 0 to infinity (AUC(inf)) for midazolam and 1-hydroxymidazolam were similar on Days 13 and 20 compared with Day 1. Following brivaracetam 150mg/day, the Day 13/Day 1 AUC(inf) ratio (90% confidence interval) was 1.09 (0.97, 1.21) and 1.04 (0.93, 1.17) for midazolam and 1-hydroxymidazolam, respectively. For the Day 20/Day 1 comparison, the corresponding AUC(inf) ratios were 1.10 (0.98, 1.23) and 1.07 (0.97, 1.18). Maximum midazolam plasma concentration was increased on both Day 13 and Day 20 vs. Day 1 but the relevance of this finding was unclear. This study indicates that brivaracetam up to 150mg/day has no significant inducing or inhibiting effect on CYP3A activity.
机译：Brivaracetam是处于癫痫的III期发育阶段的突触小泡蛋白2A配体。 I期开放标签的随机研究在42名健康男性受试者中进行，以咪达唑仑为探针评估布立西坦对CYP3A活性的影响。从第8天到第14天，将参与者随机分为口服口服口服布瓦西坦5、50或150mg /天，在第1、13和20天给予咪达唑仑单次口服剂量（7.5mg），并获得完整的药代动力学特征。对于所有的布列西坦剂量，在第13天和第20天与第1天相比，咪达唑仑和1-羟基咪达唑仑的血浆浓度-时间曲线下从0到无穷大（AUC（inf））的面积相似。布列西坦150mg /天后咪达唑仑和1-羟基咪达唑仑的13 /天1 AUC（inf）比（90％置信区间）分别为1.09（0.97，1.21）和1.04（0.93，1.17）。对于第20天/第1天的比较，相应的AUC（inf）比率为1.10（0.98，1.23）和1.07（0.97，1.18）。与第1天相比，第13天和第20天最高咪达唑仑血浆浓度均增加，但这一发现的相关性尚不清楚。这项研究表明，达150mg /天的布立西坦对CYP3A活性没有明显的诱导或抑制作用。

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