Dose-dependent intestinal and hepatic first-pass metabolism of midazolam, a cytochrome P450 3A substrate with differently modulated enzyme activity in rats

Journal of Pharmacy and Pharmacology

Volumn 51, Issue 1, 1999, Pages 67-72

  Higashikawa, Fumiko ^a   Murakami, Teruo ^a   Kaneda, Tatsuya ^a   Kato, Akiko ^a   Takano, Mikihisa ^a  

^a HIROSHIMA UNIV SCHOOL OF MEDICINE   (Japan)

Author keywords

[No Author keywords available]

Indexed keywords

CYTOCHROME P450; DEXAMETHASONE; KETOCONAZOLE; MIDAZOLAM;

ANIMAL CELL; ANIMAL EXPERIMENT; ARTICLE; CONTROLLED STUDY; DOSE RESPONSE; DRUG ABSORPTION; DRUG BIOAVAILABILITY; ENZYME ACTIVITY; INTRAGASTRIC DRUG ADMINISTRATION; INTRAVENOUS DRUG ADMINISTRATION; JEJUNUM; LIVER METABOLISM; MALE; MESENTERY; NONHUMAN; RAT;

EID: 0032977985     PISSN: 00223573     EISSN: None     Source Type: Journal    
DOI: 10.1211/0022357991771971     Document Type: Article

References (15)

1. Debri, K., Boobis, A. R., Davies, D. S., Edwards, R. J. (1995) Distribution and induction of CYP3A1 and CYP3A2 in rat liver and extrahepatic tissues. Biochem. Pharmacol. 50: 2047-2056
2. Ghosal, A., Satoh, H., Thomas, P. E., Bush, E., Moore, D. (1996) Inhibition and kinetics of cytochrome P4503A activity in microsomes from rat, human, and cDNA-expressed human cytochrome P450. Drug Metab. Dispos. 24: 940-947
3. Gorski, J. C., Hall, S. D., Jones, D. R., VandenBranden, M., Wrighton, S. A. (1994) Regioselective biotransformation of midazolam by members of the human cytochrome P450 3A (CYP3A) subfamily. Biochem. Pharmacol. 47: 1643-1653
4. Guengerich, F. P. (1992) Characterization of human cytochrome P450 enzymes. FASEB J. 6: 745-748
5. Kolars, J. C., Schmiedlin-Ren, P., Schuetz, J. D., Fang, C., Watkins, P. B. (1992) Identification of rifampin-inducible P450IIIA4 (CYP3A4) in human small bowel enterocytes. J. Clin. Invest. 90: 1871-1878
6. Kronbach, T., Mathys, D., Umeno, M., Gonzalez, F. J., Meyer, U. A. (1989) Oxidation of midazolam and triazolam by human liver cytochrome P450IIIA4. Mol. Pharmacol. 36: 89-96
7. Lee, P. C., Werlin, S. L. (1995) The induction of hepatic cytochrome P450 3A in rats: effects of age. Proc. Soc. Exp. Biol. Med. 210: 134-139
8. Lown, K. S., Kolars, J. C., Thummel, K. E., Barnett, J. L., Kunze, K. L., Wrighton, S. A., Watkins, P. B. (1994) Interpatient heterogeneity in expression of CYP3A4 and CYP3A5 in small bowel. Lack of prediction by the erythromycin breath test. Drug Metab. Dispos. 22: 947-955
9. Mahnke, A., Roos, P. H., Hanstein, W. G., Chabot, G. G. (1996) In vivo induction of cytochrome P450 CYP3A expression in rat leukocytes using various inducers. Biochem. Pharmacol. 51: 1579-1582
10. Olkkola, K. T., Backman, J. T., Neuvonen, P. J. (1994) Midazolam should be avoided in patients receiving the systemic antimycotics ketoconazole or itraconazole. Clin. Pharmacol. Ther. 55: 481-485
11. Paine, M. F., Shen, D. D., Kunze, K. L., Perkins, J. D., Marsh, C. L., McVicar, J. P., Barr, D. M., Gillies, B. S., Thummel, K. E. (1996) First-pass metabolism of midazolam by the human intestine. Clin. Pharmacol. Ther. 60: 14-24
12. Porter, T. D., Coon, M. J. (1991) Cytochrome P-450. Multiplicity of isoforms, substrates, and catalytic and regulatory mechanisms. J. Biol. Chem. 266: 13469-13472
13. Thummel, K. E., O'Shea, D., Paine, M. F., Shen, D. D., Kunze, K. L., Perkins, J. D., Wilkinson, G. R. (1996) Oral first-pass elimination of midazolam involves both gastrointestinal and hepatic CYP3A-mediated metabolism. Clin. Pharmacol. Ther. 59: 491-502
14. Watanabe, F., Sato, M., Kato, A., Murakami, T., Higashi, Y., Yata, N. (1997) First-pass metabolism of ONO-5046 (N-[2-[4-(2,2-dimethylpropionyloxy)phenylsulfonylamino]benzoyl]aminoacetic acid), a novel elastase inhibitor, in rats. Biol. Pharm. Bull. 20: 392-396
15. Wrighton, S. A., Ring, B. J. (1994) Inhibition of human CYP3A catalyzed 1′-hydroxy midazolam formation by ketoconazole, nifedipine, erythromycin, cimetidine, and nizatidine. Pharm. Res. 11: 921-924