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首页> 外文期刊>Cardiovascular therapeutics >Effects of laropiprant, a selective prostaglandin D(2) receptor 1 antagonist, on the pharmacokinetics of rosiglitazone.
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Effects of laropiprant, a selective prostaglandin D(2) receptor 1 antagonist, on the pharmacokinetics of rosiglitazone.

机译：拉罗哌特，一种选择性的前列腺素D（2）受体1拮抗剂，对罗格列酮药代动力学的影响。

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摘要

Laropiprant (LRPT), a prostaglandin D(2) receptor-1 antagonist shown to reduce niacin-induced flushing symptoms, has been combined with niacin for treatment of dyslipidemia. This open-label, randomized, 2-period crossover study assessed the pharmacokinetics of single-dose rosiglitazone in the presence and absence of multiple-dose LRPT. Twelve healthy male and female subjects, 34-64 years of age, received two, once-daily oral treatments in random sequence separated by >/=3-day washout: (1) multiple-dose LRPT 40 mg/day for 7 days (Days 1 to 7) coadministered with single-dose rosiglitazone 4 mg on Day 6; (2) single-dose rosiglitazone 4 mg on Day 1. Comparability was declared because the 90% confidence interval (CI) for the AUC(0-infinity) geometric mean ratio (GMR; rosiglitazone + LRPT/rosiglitazone alone) [0.92 (0.86, 0.99)], was contained within prespecified bounds (0.70, 1.43). The C(max) GMR (90% CI) for rosiglitazone was 0.98 (0.95, 1.02). There was no evidence of clinically meaningful alterations in the pharmacokinetics of rosiglitazone, a probe CYP2C8 substrate, following coadministration of multiple-dose LRPT in healthy subjects. Therefore, findings suggest that LRPT does not inhibit CYP2C8-mediated metabolism.
机译：Laropiprant（LRPT），一种前列腺素D（2）受体1拮抗剂，可减少烟酸引起的潮红症状，已与烟酸联合治疗血脂异常。这项开放标签，随机，2期交叉研究评估了在存在和不存在多剂量LRPT的情况下单剂量罗格列酮的药代动力学。 12名年龄在34-64岁之间的健康男性和女性受试者接受了两次每日一次的口服治疗，治疗顺序随机，间隔为> / = 3天;（1）多剂量LRPT 40 mg /天，共7天（第1至7天）在第6天与单剂量罗格列酮4 mg并用; （2）第1天单剂罗格列酮4 mg。宣布可比性，因为AUC（0-无穷大）几何平均比（GMR;罗格列酮+ LRPT /罗格列酮单独使用）的90％置信区间（CI）[0.92（0.86 ，0.99）]包含在预定范围内（0.70，1.43）。罗格列酮的C（最大）GMR（90％CI）为0.98（0.95，1.02）。没有证据表明在健康受试者中多剂量LRPT并用后，罗格列酮（一种探针CYP2C8底物）的药代动力学具有临床意义的改变。因此，发现提示LRPT不抑制CYP2C8介导的代谢。

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