Publication Cover
Xenobiotica
the fate of foreign compounds in biological systems
Volume 34, 2004 - Issue 11-12
153
Views
20
CrossRef citations to date
0
Altmetric
Research Article

In vitro metabolism of quazepam in human liver and intestine and assessment of drug interactions

&
Pages 1001-1011 | Received 12 Jul 2004, Published online: 22 Sep 2008

Reference

  • ANKIER, S. I. and GOA, K. L., 1988, Quazepam. A preliminary review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in insomnia. Drugs, 35, 42–62.
  • BOURRIE, M., MEUNIER, V., BERGER, Y. and FABRE, G., 1996, Cytochrome P450 isoform inhibitors as a tool for the investigation of metabolic reactions catalyzed by human liver microsomes. Journal of Pharmacology and Experimental Therapeutics, 277, 321–332.
  • CHUNG, W. G. and CHA, Y. N., 1997, Oxidation of caffeine to theobromine and theophylline is catalyzed primarily by fiavin-containing monooxygenase in liver microsomes. Biochemical and Biophysical Research Communications, 235, 685–688.
  • COLLER, J. K., SomoGYI, A. A. and BOCHNER, F., 1999, Flunitrazepam oxidative metabolism in human liver microsomes: involvement of CYP2C19 and CYP3A4. Xenobiotica, 29, 973–986.
  • ECHIZEN, H., KAWASAKI, H., CHIBA, K., TANI, M. and ISHIZAKI, T., 1993, A potent inhibitory effect of erythromycin and other macrolide antibiotics on the mono-N-dealkylation metabolism of disopyramide with human liver microsomes. Journal of Pharmacology and Experimental Therapeutics, 264, 1425–1431.
  • FUJISAKI, H., HIROTSU, K., OGAWA, T., MIZUKI, K., MIZUTA, H. and ARIMA, N., 2001, Metabolism of quazepam and its metabolites in humans: identification of metabolic enzymes and evaluation of drug interaction in vitro. Xenobiotic Metabolism and Disposition, 16, 558–568. [in Japanese]
  • GIANCARLO, G. M., VENKATAKRISHNAN, K., GRANDA, B. W., VON MOLTKE, L. L. and GREENBLATT, D. J., 2001, Relative contributions of CYP2C9 and 2C19 to phenytoin 4-hydroxylation in vitro: inhibition by sulfaphenazole, omeprazole, and ticlopidine. European Journal of Clinical Pharmacology, 57, 31–36.
  • HALPERT, J. R., GUENGERICH, F. P., BEND, J. R. and CORREIA, M. A., 1994, Selective inhibitors of cytochromes P450. Toxicology and Applied Pharmacology, 125, 163–175.
  • HARDIN, T. C., GRAYBILL, J. R., FETCHICK, R., WOESTENBORGHS, R., RINALDI, M. G. and KUHN, J. G., 1988, Pharmacokinetics of itraconazole following oral administration to normal volunteers. Antimicrobial Agents and Chemotherapy, 32, 1310–1313.
  • HEYKANTS, J., VAN PEER, A., VAN DE VELDE, V., VAN ROOY, P., MEULDERMANS, W., LAVRIJSEN, K., WOESTENBORGHS, R., VAN CUTSEM, J. and CAUWENBERGH, G., 1989, The clinical pharmacokinetics of itraconazole: an overview. Mycoses, 32, 67–87.
  • HILBERT, J. M., Tomo, L., MORITZEN, V., BARNETT, A., SYMCHOWICZ, S. and ZAMPAGLIONE, N., 1986, Relationships of brain and plasma levels of quazepam, fiurazepam, and their metabolites with pharmacological activity in mice. Life Sciences, 39,161–168.
  • KATO, K., YASUI-FURUKORI, N., FUKASAWA, T., AOSHIMA, T., SUZUKI, A., KANNO, M. and OTANI, K., 2003, Effects of itraconazole on the plasma kinetics of quazepam and its two active metabolites after a single oral dose of the drug. Therapeutic Drug Monitoring, 25, 473–477.
  • KOLARS, J. C., LOWN, K. S., SCHMIEDLIN-REN, P., GHOSH, M., FANG, C., WRIGHTON, S. A., MERTON, R. M. and WATKINS, P. B., 1994, CYP3A gene expression in human gut epithelium. Pharmacogenetics, 4, 247–259.
  • LAPPLE, F., VON RICHTER, 0., FROMM, M. F., RICHTER, T., THON, K. P., WISSER, H., GRIESE, E. U., EICHELBAUM, M. and KIVISTO, K. T., 2003, Differential expression and function of CYP2C isoforms in human intestine and liver. Pharmacogenetics, 13, 565–575.
  • MANCY, A., DIJOL S., Poi., S., GUENGERICH, P. and MANSUY, D., 1996, Interaction of sulfaphenazole derivatives with human liver cytochromes P450 2C: molecular origin of the specific inhibitory effects of sulfaphenazole on CYP 2C9 and consequences for the substrate binding site topology of CYP 2C9. Biochemistry, 35, 16205–16212.
  • NEGRONI, R. and ARECHAVALA, A. I., 1993, Itraconazole: pharmacokinetics and indications. Archives of Medical Research, 24, 387–393.
  • NEWTON, D. J., WANG, R. W. and Lu, A. Y., 1995, Cytochrome P450 inhibitors. Evaluation of specificities in the in vitro metabolism of therapeutic agents by human liver microsomes. Drug Metabolism and Disposition, 23, 154–158.
  • OBACH, R. S., ZHANG, Q. Y., DUNBAR, D. and KAMINSKY, L. S., 2001, Metabolic characterization of the major human small intestinal cytochrome p450s. Drug Metabolism and Disposition, 29, 347–352.
  • PAINE, M. F., KHALIGHI, M., FISHER, J. M., SHEN, D. D., KUNZE, K. L., MARSH, C. L., PERKINS, J. D. and THUMMEL, K. E., 1997, Characterization of interintestinal and intraintestinal variations in human CYP3A-dependent metabolism. Journal of Pharmacology and Experimental Therapeutics, 283, 1552–1562.
  • RODRIGUEZ, R. J. and ACOSTA, D., JR, 1997, Metabolism of ketoconazole and deacetylated ketoconazole by rat hepatic microsomes and fiavin-containing monooxygenases, Drug Metabolism and Disposition, 25, 772–777.
  • VENKATAKRISHNAN, K., VON MOLTKE, L. L. and GREENBLATT, D. J., 2001, Human drug metabolism and the cytochromes P450: application and relevance of in vitro models. Journal of Clinical Pharmacology, 41, 1149–1179.
  • YAMAOKA, K., TANIGAWARA, Y., NAKAGAWA, T. and UNO, T., 1981, A pharmacolinetic analysis program (MULTI) for microcomputer. Journal of Pharmacobiodynamics, 4, 879–885.
  • YEUNG, C. K., LANG, D. H., THUMMEL, K. E. and RETTIE, A. E., 2000, Immunoquantitation of FM01 in human liver, kidney, and intestine. Drug Metabolism and Disposition, 28, 1107–1111.
  • ZAMPAGLIONE, N., HILBERT, J. M., NING, J., CHUNG, M., GURAL, R. and SYMCHOWICZ, S., 1985, Disposition and metabolic fate of 14C-quazepam in man. Drug Metabolism and Disposition, 13, 25–29.
  • ZHANG, Q. Y., DUNBAR, D., OSTROWSKA, A., ZEISLOFT, S., YANG, J. and KAMINSKY, L. S., 1999, Characterization of human small intestinal cytochromes P-450. Drug Metabolism and Disposition, 27, 804–809.

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.