Effect of efavirenz on the pharmacokinetics of ketoconazole in HIV-infected patients

被引：11

作者：

Sriwiriyajan, Somchai ^{[1
]}

Mahatthanatrakul, Werawath

Ridtitid, Wibool

Jaruratanasirikul, Sutep

机构：

[1] Prince Songkla Univ, Fac Med, Dept Med, Hat Yai 90110, Thailand

[2] Prince Songkla Univ, Fac Sci, Dept Pharmacol, Hat Yai 90112, Thailand

来源：

EUROPEAN JOURNAL OF CLINICAL PHARMACOLOGY | 2007年 / 63卷 / 05期

关键词：

drug interaction; efavirenz; ketoconazole; HIV-infected patients; pharmacokinetics;

D O I：

10.1007/s00228-007-0282-8

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Objective: To investigate the effect of efavirenz on the ketoconazole pharmacokinetics in HIV-infected patients. Methods: Twelve HIV-infected patients were assigned into a one-sequence, two-period pharmacokinetic interaction study. In phase one, the patients received 400 mg of ketoconazole as a single oral dose on day 1; in phase two, they received 600 mg of efavirenz once daily in combination with 150 mg of lamivudine and 30 or 40 mg of stavudine twice daily on days 2 to 16. On day 16, 400 mg of ketoconazole was added to the regimen as a single oral dose. Ketoconazole pharmacokinetics were studied on days 1 and 16. Results: Pretreatment with efavirenz significantly increased the clearance of ketoconazole by 201%. C-max and AUC(0-24) were significantly decreased by 44 and 72%, respectively. The T-1/2 was significantly shorter by 58%. Conclusion: Efavirenz has a strong inducing effect on the metabolism of ketoconazole.

引用

页码：479 / 483

页数：5

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