A comparison of 4-hydroxycholesterol:cholesterol and 6-hydroxycortisol:cortisol as markers of CYP3A4 induction

被引：37

作者：

Arrhen, Yvonne Marde ^{[1
]}

Nylen, Hanna ^{[2
]}

Lovgren-Sandblom, Anita ^{[2
]}

Kanebratt, Kajsa P. ^{[3
]}

Wide, Katarina ^{[4
]}

Diczfalusy, Ulf ^{[2
]}

机构：

[1] Karolinska Univ Hosp, Huddinge, Sweden

[2] Karolinska Inst, Dept Lab Med, Huddinge, Sweden

[3] AstraZeneca R&D, CVGI IMed DMPK, Molndal, Sweden

[4] Karolinska Inst, Dept CLINTEC, Huddinge, Sweden

来源：

BRITISH JOURNAL OF CLINICAL PHARMACOLOGY | 2013年 / 75卷 / 06期

基金：

瑞典研究理事会;

关键词：

CYP3A4; endogenous markers; induction; LC-MS; MS; rifampicin; ENDOGENOUS MARKER; 4-BETA-HYDROXYCHOLESTEROL; HUMANS; 6-BETA-HYDROXYCORTISOL; INHIBITION; RIFAMPICIN;

D O I：

10.1111/bcp.12016

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Aim To compare plasma 4-hydroxycholesterol:cholesterol with urinary 6-hydroxycortisol:cortisol as markers of cytochrome P4503A4 activity before and after treatment with rifampicin for 2 weeks. Method 6-hydroxycortisol and cortisol were determined by liquid chromatography tandem mass spectrometry and 4-hydroxycholesterol was determined by gas chromatographymass spectrometry in three groups of healthy volunteers. Results Induction ratios for 6-hydroxycortisol:cortisol were 1.8, 3.9 and 4.5 for 20mgday1, 100mgday1 or 500mgday1 of rifampicin, respectively. The corresponding ratios for 4-hydroxycholesterol:cholesterol were 1.5, 2.4 and 3.8. Conclusions Plasma 4-hydroxycholesterol:cholesterol gave similar induction ratios to urinary 6-hydroxycortisol:cortisol.

引用

页码：1536 / 1540

页数：5

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