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首页> 外文期刊>The Journal of Clinical Pharmacology: Official Journal of the American College of Clinical Pharmacology >Steady-state pharmacokinetics of isotretinoin and its 4-oxo metabolite: implications for fetal safety.
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Steady-state pharmacokinetics of isotretinoin and its 4-oxo metabolite: implications for fetal safety.

机译：异维A酸及其4-氧代代谢产物的稳态药代动力学：对胎儿安全性的影响。

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摘要

Isotretinoin is the most potent human teratogen on the market. Women for whom contraception fails may conceive during or soon after discontinuing isotretinoin therapy, making its elimination kinetics a crucial determinant of fetal safety. The steady-state pharmacokinetics of isotretinoin and its major 4-oxo metabolite were studied in 16 adult patients treated for acne who were receiving doses that ranged from 0.47 to 1.7 mg/kg daily. This is the first study of the pharmacokinetics of isotretinoin in women of childbearing age (n = 11). The clinical efficacy and tolerability of isotretinoin was investigated, and the correlation between these data and steady-state serum concentrations of isotretinoin was tested. The concentration-time data best fitted a two-compartment open model with linear elimination. There was no correlation between efficacy and tolerability of isotretinoin and steady-state serum concentrations. There was no correlation between dose of isotretinoin and steady-state concentration, due to the large variability in apparent clearance. Values for elimination half-life (t1/2) of isotretinoin and its metabolite were 29+/-40 hours and 22+/-10 hours, respectively. These data suggest a longer elimination t1/2 of the parent drug than previously reported. This is probably due to the longer sampling time used in this study (as long as 28 days). This study suggests that a greater variability exists in the safe time after discontinuation of the drug for onset of conception.
机译：异维A酸是市场上最有效的人致畸剂。避孕失败的妇女可能会在异维A酸治疗期间或之后受孕，这使其消除动力学成为决定胎儿安全性的关键因素。异维A酸及其主要的4-氧代代谢产物的稳态药代动力学在接受痤疮治疗的16名成年患者中进行了研究，这些患者每天的剂量范围为0.47至1.7 mg / kg。这是异维A酸在育龄妇女（n = 11）中药代动力学的首次研究。研究了异维A酸的临床疗效和耐受性，并测试了这些数据与异维A酸稳态血清浓度之间的相关性。浓度时间数据最适合采用线性消除的两室开放模型。异维A酸的功效和耐受性与稳态血清浓度之间没有相关性。由于表观清除率差异很大，因此异维A酸的剂量与稳态浓度之间没有相关性。异维A酸及其代谢产物的消除半衰期（t1 / 2）值分别为29 +/- 40小时和22 +/- 10小时。这些数据表明母体药物消除t1 / 2的时间比以前报道的时间更长。这可能是由于本研究中使用了更长的采样时间（长达28天）。这项研究表明，在停药后因受孕而出现的安全时间存在较大的变异性。

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