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首页> 外文期刊>The Journal of Clinical Pharmacology: Official Journal of the American College of Clinical Pharmacology >Pioglitazone: effect on CYP3A4 activity.
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Pioglitazone: effect on CYP3A4 activity.

机译：吡格列酮：对CYP3A4活性的影响。

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摘要

Clinical studies demonstrate CYP3A4 enzyme induction with troglitazone, a thiazolidinedione derivative structurally related to pioglitazone. The objective of this prospective, open-label study conducted in healthy volunteers was to evaluate the influence of multiple-dose pioglitazone therapy on the urinary excretion ratio of 6-beta-hydroxycortisol to cortisol, an endogenous marker of CYP3A4 activity. Twelve subjects were given pioglitazone hydrochloride 45 mg daily for 14 days. Urine was collected over a 24-hour period before pioglitazone and after administration of the last tablet. Baseline and posttreatment CYP3A4 activity was assessed with the urinary 6-beta-hydroxycortisol/cortisol ratio. The mean +/- SD 6-beta-hydroxycortisol/cortisol ratios before and after treatment were 8.3 +/- 4.4 and 9.4 +/- 4.0, respectively (p = 0.29). The mean change from baseline was a nonsignificant 20.2%. Nine subjects had a small increase and 3 subjects had a reduction in the ratio. Using the ratio as a marker of CYP3A4 activity, the data support a lack of inductive effect on CYP3A4 by multiple-dose pioglitazone therapy. Thus, administration of pioglitazone should not result in clinically significant effects on the pharmacokinetics of other CYP3A4 substrates.
机译：临床研究表明曲格列酮是CYP3A4酶的诱导剂，曲格列酮是与吡格列酮结构相关的噻唑烷二酮衍生物。在健康志愿者中进行的这项前瞻性，开放性研究的目的是评估多剂量吡格列酮治疗对6-β-羟基皮质醇与皮质醇（一种CYP3A4活性内源性标志物）的尿排泄率的影响。每天给十二名受试者服用盐酸吡格列酮45 mg，持续14天。在吡格列酮治疗前和最后一次服用片剂后的24小时内收集尿液。用尿中的6-β-羟基皮质醇/皮质醇比率评估基线和治疗后CYP3A4的活性。治疗前后的平均+/- SD6-β-羟基皮质醇/皮质醇比分别为8.3 +/- 4.4和9.4 +/- 4.0（p = 0.29）。与基线相比的平均变化不显着20.2％。 9名受试者的比例有所增加，而3名受试者的比例有所降低。使用该比率作为CYP3A4活性的标记，数据支持多剂量吡格列酮治疗对CYP3A4缺乏诱导作用。因此，吡格列酮的给药不应对其他CYP3A4底物的药代动力学产生临床上显着的影响。

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