单次口服非那雄胺片对血清胆红素水平的影响

doi:10.19803/j.1672-8629.20210275

摘要/Abstract

摘要： 目的研究非那雄胺在中国健康志愿者使用中的安全性,为临床合理用药提供参考。方法通过2项单次口服5 mg非那雄胺受试制剂和参比制剂的随机、双交叉、2周期的生物等效性研究,共103名中国健康男性志愿者完成了空腹和高脂餐后试验,监测并记录实验室检查参数、生命体征和不良事件。结果 2项试验中,非那雄胺均耐受良好,没有发生严重不良反应。实验室检查异常的不良事件中,血清胆红素水平升高出现的频次最多,最长在10 d内恢复至正常。结论非那雄胺是一种有效的、选择性的UGT1A4竞争性抑制剂,在血清胆红素的代谢中起关键作用。非那雄胺可能导致血清胆红素升高,建议临床用药时应注意与非那雄胺相关的血清胆红素升高风险。

关键词: 非那雄胺, 血清胆红素升高, 生物等效性研究, 安全性, 药品不良反应, 不良事件

Abstract: Objective To study the safety and adverse events of finasteride in healthy Chinese subjects and to provide reference for rational use of drugs. Methods A total of 103 healthy Chinese male volunteers were enrolled in fasting and fed states in two randomized, crossover, two-period, bioequivalence studies of the test preparation of single oral 5 mg finasteride. All laboratory parameters, vital signs, and adverse events were monitored and recorded throughout the study. Results In both trials, finasteride was well tolerated and no serious adverse events were reported. Among the adverse events that were observed, the elevation of bilirubin levels was the most frequent in each trial, and resolved within 10 days. Conclusion Finasteride is a potent and selective UGT1A4-competitive inhibitor that is critical to the metabolism of bilirubin. Finasteride may cause bilirubin elevation. It is recommended that clinicians pay attention to the risk of bilirubin elevation associated with finasteride in clinical use.

Key words: finasteride, bilirubin elevation, bioequivalence study, safety, adverse drug reaction, adverse event

中图分类号:

R977
R994.11

李玲珺, 陶蕾, 魏峻, 李弘扬, 蔡宝乐, 马鹏程. 单次口服非那雄胺片对血清胆红素水平的影响[J]. 中国药物警戒, 2022, 19(11): 1202-1205.

LI Lingjun, TAO Lei, WEI Jun, LI Hongyang, CAI Baole, MA Pengcheng. Effects of a single oral administration of finasteride tablets on bilirubin levels[J]. Chinese Journal of Pharmacovigilance, 2022, 19(11): 1202-1205.

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