Poor correlation between 6β-hydroxycortisol:cortisol molar ratios and midazolam clearance as measure of hepatic CYP3A activity

British Journal of Clinical Pharmacology

Volumn 62, Issue 2, 2006, Pages 187-195

  Chen, Ya Chi ^a   Gotzkowsky, S Karl ^a   Nafziger, Anne N ^b   Kulawy, Robert W ^c   Rocci Jr , Mario L ^c   Bertino Jr , Joseph S ^b   Kashuba, Angela D M ^a  

^a UNIVERSITY OF NORTH CAROLINA   (United States)

^b BASSETT HEALTHCARE   (United States)

^c ICON PLC   (United Kingdom)

Author keywords

6 hydroxycortisol; 6 hydroxycortisol cortisol molar ratio; CYP3A; Fluvoxamine; Midazolam clearance; Phenotyping

Indexed keywords

6 BETA-HYDROXYCORTISOL; 6BETA HYDROXYHYDROCORTISONE; BIOLOGICAL MARKER; CYTOCHROME P450 3A; DRUG DERIVATIVE; FLUVOXAMINE; HYDROCORTISONE; MIDAZOLAM;

ADULT; ARTICLE; BLOOD; CROSSOVER PROCEDURE; DRUG ANTAGONISM; DRUG EFFECT; ENZYMOLOGY; FEMALE; HUMAN; INTRAVENOUS DRUG ADMINISTRATION; LIVER; MALE; METABOLIC CLEARANCE RATE; METABOLISM; PHENOTYPE; URINE;

ADULT; BIOLOGICAL MARKERS; CROSS-OVER STUDIES; CYTOCHROME P-450 CYP3A; FEMALE; FLUVOXAMINE; HUMANS; HYDROCORTISONE; INJECTIONS, INTRAVENOUS; LIVER; MALE; METABOLIC CLEARANCE RATE; MIDAZOLAM; PHENOTYPE;

EID: 33748254753     PISSN: 03065251     EISSN: 13652125     Source Type: Journal    
DOI: 10.1111/j.1365-2125.2006.02628.x     Document Type: Article

References (35)

1. Slaughter RL, Edwards DJ. Recent advances: the cytochrome P450 enzymes. Ann Pharmacother 1995; 29: 619-24.
2. Anzenbacher P, Anzenbacherova E. Cytochromes P450 and metabolism of xenobiotics. Cell Mol Life Sci 2001; 58: 737-47.
3. Thummel KE, Shen DD, Podoll TD, Kunze KL, Trager WF, Bacchi CE, Marsh CL, McVicar JP, Barr DM, Perkins JD, et al. Use of midazolam as a human cytochrome P4503A probe; II. Characterization of inter- and intraindividual hepatic CYP3A variability after liver transplantation. J Pharmacol Ther 1994; 27: 557-66.
4. Forrester LM, Henderson CJ, Glancey MJ, Back DJ, Park BK, Ball SE, Kitteringham NR, McLaren AW, Miles JS, Skett P, et al. Relative expression of cytochrome P450 isozymes in human liver and association with the metabolism of drugs and xenobiotics. Biochem J 1992; 281: 359-68.
5. Dowling TC, Briglia AE, Fink JC, Hanes DS, Light PD, Stackiewicz L, Karyekar CS, Eddington ND, Weir MR, Henrich WL. Characterization of hepatic cytochrome p4503A activity in patients with end-stage renal disease. Clin Pharmacol Ther 2003; 73: 427-34.
6. Bonate PL. Gender-related differences in xenobiotic metabolism. Clin Pharmacol 1991; 31: 684-90.
7. Harris RZ, Benet LZ, Schwart JB. Gender effects in pharmacokinetics and pharmacodynamics. Drugs 1995; 50: 222-39.
8. Kashuba AD, Bertino JS Jr, Rocci ML Jr, Kulawy RW, Beck DJ, Nafziger AN. Quantification of 3-month intraindividual variability and the influence of sex and menstrual cycle phase on CYP3A activity as measured by phenotyping with intravenous midazolam. Clin Pharmacol Ther 1998; 64: 269-77.
9. Ohkita C, Goto M. Increased 6β-hydroxycortisol excretion in pregnant women: implication of drug-metabolizing enzyme induction. DICP Ann Pharmacother 1990; 24: 814-6.
10. Gass RJA, Gal J, Fogle PW, Detmar D, Gerbr JG. Neither dapsone hydroxylation nor cortisol 6-beta-hydroxylation detects the inhibition of CYP3A4 by HIV-1 protease inhibitors. Eur J Clin Pharmacol 1998; 54: 741-7.
11. Kovacs SJ, Martin DE, Evritt DE, Patterson SD, Jorkasky DK. Urinary excretion of 6-beta-hydroxycortisol as an in vivo marker for CYP3A induction: applications and recommendations. Clin Pharmacol Ther 1998; 63: 617-22.
12. Benet LZ. There are no useful CYP3A probes that quantitatively predict the in vivo kinetics of other CYP3A substrates and no expectation that one will be found. Mol Interv 2005; 5: 79-83.
13. Masica AL, Mayo G, Wilkinson GR. In vivo comparisons of constitutive cytochrome P450 3A activity assessed by alprazolam, triazolam, and midazolam. Clin Pharmacol Ther 2004; 76: 341-9.
14. Wenk M, Todesco L, Krahenbuhl S. Effect of St John's wort on the activities of CYP1A2, CYP3A4, CYP2D6, N-acetyltransferase 2, and xanthine oxidase in healthy males and females. Br J Clin Pharmacol 2004; 57: 495-9.
15. Anderson GD, Rosito G, Mohustsy MA, Elmer GW. Drug interaction potential of soy extract and Panax ginseng. J Clin Pharmacol 2003; 43: 643-8.
16. Ushiama H, Echizen H, Nachi S, Ohnishi A. Dose-dependent inhibition of CYP3A activity by clarithromycin during Helicobacter pylori eradication therapy assessed by changes in plasma lansoprazole levels and partial cortisol clearance to 6β-hydroxycortisol. Clin Pharmacol Ther 2002; 72: 33-43.
17. Boulence X, Ollier C. CYP3A induction: use and analysis of 6-β-hydroxycortisol/cortisol ratio after repeated administration of drug in clinic. Drug Metab Rev 2005; 37: 28 (Abstract) 59.
18. Ged CR, Rouillon JM, Pichard L, Combalbert J, Bressot N, Bories P, Michel H, Beaune P, Maurel P. The increase in urinary excretion of 6-beta-hydroxycortisol as a marker of human hepatic cytochrome P450IIIA induction. Br J Clin Pharmacol 1989; 28: 373-87.
19. Kinirons MT, O'Shea D, Downing TE, Fitzwilliam AT, Joellenbeck L, Groopman JD, Wilkinson GR, Wood AJ. Absence of correlations among three putative in vivo probes of human cytochrome P4503A activity in young healthy men. Clin Pharmacol Ther 1993; 54: 621-9.
20. Hunt CM, Watkins PB, Sanger P, Stave GM, Barlascini N, Watlington CO, Wright JT Jr, Guzelian PS. Heterogeneity of CPY3A isoforms metabolizing erythromycin and cortisol. Clin Pharmacol Ther 1992; 51: 18-23.
21. Streetman DS, Bertino JS Jr, Nafziger AN. Phenotyping of drug-metabolizing enzymes in adults: a review of in-vivo cytochrome P450 phenotyping probes. Pharmacogenetics 2000; 10: 187-216.
22. Watkins PB, Turgeon DK, Saenger P, Lown KS, Kolars JC, Hamilton T, Fishman K, Guzelian PS, Voorhees JJ. Comparison of urinary 6-beta-cortisol and the erythromycin breath test as measures of hepatic P450IIIA (CYP3A) activity. Clin Pharmacol Ther 1992; 52: 265-73.
23. Kim RB, Wandel C, Leake B, Cvetkovic M, Fromm MF, Dempsey PJ, Roden MM, Belas F, Chaudhary AK, Roden DM, Wood AJ, Wilkinson GR. Interrelationship between inhibitors and substrates of human CYP3A and P-glycoprotein. Pharm Res 1999; 16: 408-14.
24. Katz FH, Lipman MM, Frantz AG, Jailer JW. The physiologic significance of 6β-hydroxycortisol in human corticoid metabolism. J Clin Endocrinol 1971; 32: 192-200.
25. 450 3A4 activity in premenopausal and postmenopausal women based on 6β-hydroxycortisol:cortisol ratios. Pharmacotherapy 1998; 18: 1271-6.
26. Inagaki K, Inagaki M, Kataoka T, Sekido I, Gill MA, Nishida M. A wide interindividual variability of urinary 6beta-hydroxycortisol to free cortisol in 487 healthy Japanese subjects in near basal condition. Ther Drug Monit 2002; 24: 722-7.
27. Eeckhoudt SL, Desager JP, Robert AR, Leclercq I, Verbeeck RK, Horsmans Y. Midazolam and cortisol metabolism before and after CYP3A induction in humans. Int J Clin Pharmacol Ther 2001; 39: 293-9.
28. Ushiama H, Echizen H, Nachi S, Ohnishi A. Dose-dependent inhibition of CYP3A activity by clarithromycin during Helicobactor pylori eradication therapy assessed by changes in plasma lansoprazole levels and partial cortisol clearance to 6β-hydroxycortisol. Clin Pharmacol Ther 2002; 72: 33-43.
29. Bidart M, Lesgards G. Direct injection analysis of 6β- hydroxycortisol and cortisol in urine by HPLC-UV with online ISRP precolumn. J Liquid Chromatogr 1995; 18: 725-38.
30. Lykkesfeldt J, Loft S, Poulsen HE. Simultaneous determination of urinary free cortisol and 6β-hydroxycortisol by high-performance liquid chromatography to measure human CYP3A activity. J Chromatogr B Biomed Appl 1994; 660: 23-9.
31. Bienvenu T, Rey E, Pons G, D'Athis P, Olive G. A simple noninvasive procedure for the investigation of cytochrome P450 IIIA-dependent enzymes in humans. Int J Clin Pharmacol Ther Toxicol 1991; 29: 441-5.
32. Rogers JF, Rocci ML Jr, Haughey DB, Bertino JS Jr. An evaluation of the suitability of intravenous midazolam as an in vivo marker for hepatic cytochrome P4503A activity. Clin Pharmacol Ther 2003; 73: 153-8.
33. Furuta T, Suzuki A, Mori C, Shibasaki H, Yokokawa A, Kasuya Y. Evidence for the validity of cortisol 6 beta-hydroxylation clearance as a new index for in vivo cytochrome P450 3A phenotyping in humans. Drug Metab Dispos 2003; 31: 1283-7.
34. Watkins PB. Noninvasive tests of CYP3A enzymes. Pharmacogenetics 1994; 4: 171-84.
35. Lewis DVF, Eddershaw PJ, Goldfarb PS, Tarbit MH. Molecular modeling of CYP3A4 from an alignment with CYP102: identification of key interactions between putative active site residues and CYP3A-specific chemicals. Xenobiotica 1996; 26: 1067-86.