Persistent inhibition of CYP3A4 by ketoconazole in modified Caco-2 cells

Pharmaceutical Research

Volumn 17, Issue 3, 2000, Pages 299-305

  Gibbs, Megan A ^a   Baillie, Mark T ^a   Shen, Danny D ^a   Kunze, Kent L ^a   Thummel, Kenneth E ^a  

^a UNIVERSITY OF WASHINGTON   (United States)

Author keywords

Caco 2; CYP3A4; Drug metabolism; Ketoconazole; Midazolam

Indexed keywords

CALCITRIOL; CYTOCHROME P450; HUMAN SERUM ALBUMIN; KETOCONAZOLE; MIDAZOLAM;

ANIMAL CELL; ARTICLE; CELL STRAIN CACO 2; CONCENTRATION RESPONSE; DRUG METABOLISM; ENZYME ACTIVITY; ENZYME INHIBITION; ENZYME SUBSTRATE; MONOLAYER CULTURE; NONHUMAN; PRIORITY JOURNAL;

ANTIFUNGAL AGENTS; CACO-2 CELLS; CYTOCHROME P-450 ENZYME SYSTEM; ENZYME ACTIVATION; GABA MODULATORS; HUMANS; HYDROXYLATION; KETOCONAZOLE; MIDAZOLAM; MIXED FUNCTION OXYGENASES; VITAMIN D;

EID: 0034001534     PISSN: 07248741     EISSN: None     Source Type: Journal    
DOI: 10.1023/A:1007550717526     Document Type: Article

References (20)

1. 1. J. C. Kolars, K. S. Lown, P. Schmiedlin-Ren, M. Ghosh, C. Fang, S. A. Wrighton, R. M. Merion, and P. B. Watkins. CYP3A gene expression in human gut epithelium. Pharmacogenetics 4:247-259 (1994).
2. 2. M. F. Paine, M. Khalighi, J. M. Fisher, D. D. Shen, K. L. Kunze, C. L. Marsh, J. D. Perkins, and K. E. Thummel. Characterization of inter-and intra-intestinal differences in human CYP3A-dependent metabolism. J. Pharmacol. Exp. Ther. 283:1552-1562 (1997).
3. 3. M. F. Paine, D. D. Shen, K. L. Kunze, J. D. Perkins, C. L. Marsh, J. P. McVicar, D. M. Barr, B. S. Gillies, and K. E. Thummel. First-pass metabolism of midazolam by the human intestine. Clin. Pharmacol. Ther. 60:14-24 (1996).
4. 4. K. E. Thummel, D. D. Shen, T. D. Podoll, K. L. Kunze, W. F. Trager, P. S. Hartwell, V. A. Raisys, C. L. Marsh, J. P. McVicar, D. M. Barr, J. D. Perkins, and R. L. Carithers Jr. Use of midazolam as a human cytochrome P450 3A probe: I. In vitro-in vivo correlations in liver transplant patients. J. Pharmacol. Exp. Ther. 271:549-556 (1994).
5. 5. J. C. Kolars, W. M. Awni, R. M. Merion, and P. B. Watkins. First-pass metabolism of cyclosporin by the gut. Lancet 338:1488-1490 (1991).
6. 6. D. K. Turgeon, D. P. Normolle, A. B. Leightman, T. M. Annesley, D. E. Smith, and P. B. Watkins. Erythromycin breath test predicts oral clearance of cyclosporine in kidney transplant recipients. Clin. Pharmacol. Ther. 52:471-478 (1992).
7. 7. M. P. Ducharme, L. H. Warbasse, and D. J. Edwards. Disposition of intravenous and oral cyclosporine after administration with grapefruit juice. Clin. Pharmacol. Ther. 57:485-491 (1995).
8. 8. H. H. T. Kupferschmidt, H. R. Ha, W. H. Ziegler, P. J. Meier, and S. Krähenbühl. Interaction between grapefruit juice and midazolam in humans, Clin. Pharmacol. Ther. 58:20-28 (1995).
9. 9. K. S. Lown, D. G. Bailey, R. J. Fontana, S. K. Janardan, C. H. Adair, L. A. Fortlage, M. B. Brown, W. Guo, and P. B. Watkins. Grapefruit juice increases felodipine oral availability in humans by increasing intestinal CYP3A protein expression. J. Clin. Invest. 99:2545-2553 (1997).
10. 10. D. Y. Gomez, V. J. Wacher, S. J. Tomlanovich, M. F. Hebert, and L. Z. Benet. The effects of ketoconazole on the intestinal metabolism and bioavailability of cyclosporine. Clin. Pharmacol. Ther. 58:15-19 (1995).
11. 11. J. Baxter, C. Brass, and J. Schentag. Pharmacokinetics of ketoconazole administered intravenously to dogs and orally as tablet and solution to humans and dogs. J. Pharm. Sci. 75:433-447 (1986).
12. 12. T. Daneshmend, and D. Warnock. Clinical pharmacokinetics of ketoconazole. Clin. Pharmacokinet. 14:13-34 (1988).
13. 13. J. Madsen. Effects of gender, age, and body mass index on gastrointestinal transit times. Digest Dis. Sci. 37:1548-1553 (1992).
14. 3. Mol. Pharmacol. 51:741-754 (1997).
15. 3 modified Caco-2 cell monolayers. J. Pharmacol. Exp. Ther. 289:1134-1142 (1999).
16. 16. M. A. Gibbs, K. E. Thummel, D. D. Shen, and K. L. Kunze. Inhibition of CYP3A in human intestinal and liver microsomes: Comparison of Ki values and impact of CYP3A5 expression. Drug Metab. Dispos. 27:180-187 (1999).
17. 17. J. V. Tyle. Ketoconazole: Mechanism of action, spectrum of activity, pharmacokinetics, drug interactions, adverse reactions and therapeutic use. Pharmacotherapy 4:343-373 (1984).
18. 18. L. Floren, I. Bekersky, L. Benet, Q. Mekki, D. Dressler, J. Lee, J. Roberts, and M. Hebert. Tacrolimus oral bioavailability double with coadministration of ketoconazole. Clin. Pharmacol. Ther. 62:41-49 (1997).
19. 19. J. C. Fleishaker, P. G. Pearson, L. C. Wienkers, L. K. Pearson, and G. R. Graves. Biotransformation of tirilazad in humans: 2. Effect of ketoconazole on tirilazad clearance and oral bioavailability. J. Pharmacol. Exp. Ther. 277:991-998 (1996).
20. 20. E. Antignac, B. Koch, and J. Narbonne. Interactions of imidazole with purified cytochrome P450: Spectral modifications. In, I. Schuster, (ed), Cytochrome P450: Biochemcistry and Biophysics, Taylor and Francis, New York, 1989, pp. 195-199.