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首页> 外文期刊>The Journal of Clinical Pharmacology: Official Journal of the American College of Clinical Pharmacology >Absence of effect of terbinafine on the activity of CYP1A2, NAT-2, and xanthine oxidase.
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Absence of effect of terbinafine on the activity of CYP1A2, NAT-2, and xanthine oxidase.

机译：没有特比萘芬对CYP1A2，NAT-2和黄嘌呤氧化酶活性的影响。

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摘要

Terbinafine is an allylamine antifungal agent used for the treatment of onychomycosis. It has previously been reported to interact with caffeine and is metabolized in part by the cytochrome P450 systems. This open-label, randomized, crossover study was conducted to examine the effect of terbinafine on the activity of cytochrome P450 1A2 (CYP1A2), N-acetyltransferase (NAT-2), and xanthine oxidase (XO). Twelve healthy nonsmoking adult volunteers were enrolled. Each received single doses of caffeine (100 mg), and urine was collected for a 16-hour period with and without multiple-dose oral administration of terbinafine (250 mg daily for 3 days). Study periods were separated by a 4-week washout period. Urinary caffeine metabolite ratios were used to assess CYP1A2, NAT-2 and XO activity. Comparison of mean metabolic ratios for treatment with and without terbinafine indicated that terbinafine did not appear to alter the activity of CYP1A2, NAT-2, or XO, all of which regulate the biotransformation of caffeine.
机译：特比萘芬是用于治疗甲癣的烯丙胺抗真菌剂。先前已报道它与咖啡因相互作用，并被细胞色素P450系统部分代谢。这项开放标签，随机，交叉研究旨在检查特比萘芬对细胞色素P450 1A2（CYP1A2），N-乙酰基转移酶（NAT-2）和黄嘌呤氧化酶（XO）活性的影响。招募了十二名健康的非吸烟成人志愿者。每个人接受单剂量的咖啡因（100毫克），并在有和没有多剂量口服特比萘芬（每天250毫克，共3天）的情况下收集尿液，持续16小时。研究期间隔为4周的清除期。尿咖啡因代谢物比率用于评估CYP1A2，NAT-2和XO活性。比较使用和不使用特比萘芬治疗的平均代谢率表明，特比萘芬似乎没有改变CYP1A2，NAT-2或XO的活性，它们均调节咖啡因的生物转化。

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