Clinical pharmacokinetics of fexofenadine enantiomers.

阅读量:

47

作者:

T Uno

展开

摘要:

Drug-transporters play an important role in the disposition of clinical medicines. Although there are plural studies that have reported on the stereoselective pharmacokinetics related to cytochrome P450s, previous reports of the stereoselective pharmacokinetics related to drug-transporters including P-glycoprotein have been lacking. This article reviews the pharmacokinetic differences between fexofenadine enantiomers in humans and summarizes the previous reports that co-administration of P-glycoprotein inhibitors has altered the stereoselective pharmacokinetics of fexofenadine enantiomers. Both in vitro and in vivo studies have demonstrated that both itraconazole and verapamil are potent P-glycoprotein inhibitors. Therefore, by comparing the stereoselective pharmacokinetics of (R)- and (S)-fexofenadine with or without itraconazole and verapamil, the contribution of P-glycoprotein-mediated transport to fexofenadine stereoselective pharmacokinetics could be estimated. In our studies, the plasma concentrations of (R)-fexofenadine were greater than those of the corresponding (S)-enantiomer. Co-administration of itraconazole and/or verapamil significantly increased the AUC(0 - 24) of both enantiomers; their influence on the P-glycoprotein-mediated transport of (S)-fexofenadine was greater than that of the (R)-enantiomer. However, because t(max) and t(1/2) were constant in both studies, the fexofenadine stereoselective pharmacokinetics appears to be due to P-glycoprotein efflux activity in the small intestine, which suggests that P-glycoprotein probably possesses the chiral discriminatory abilities.

展开

DOI:

10.1517/17425250903382615

被引量:

112

年份:

2010

通过文献互助平台发起求助,成功后即可免费获取论文全文。

我们已与文献出版商建立了直接购买合作。

你可以通过身份认证进行实名认证,认证成功后本次下载的费用将由您所在的图书馆支付

您可以直接购买此文献,1~5分钟即可下载全文,部分资源由于网络原因可能需要更长时间,请您耐心等待哦~

身份认证 全文购买

相似文献

参考文献

引证文献

辅助模式

0

引用

文献可以批量引用啦~
欢迎点我试用!

关于我们

百度学术集成海量学术资源,融合人工智能、深度学习、大数据分析等技术,为科研工作者提供全面快捷的学术服务。在这里我们保持学习的态度,不忘初心,砥砺前行。
了解更多>>

友情链接

百度云百度翻译

联系我们

合作与服务

期刊合作 图书馆合作 下载产品手册

©2025 Baidu 百度学术声明 使用百度前必读

引用