Publication Cover
Xenobiotica
the fate of foreign compounds in biological systems
Volume 42, 2012 - Issue 11
457
Views
10
CrossRef citations to date
0
Altmetric
General Xenobiochemistry

Impact of nonlinear midazolam pharmacokinetics on the magnitude of the midazolam-ketoconazole interaction in rats

, , , &
Pages 1058-1068 | Received 09 Feb 2012, Accepted 06 Apr 2012, Published online: 11 May 2012

References

  • Bachmann KA. (2006). Inhibition constants, inhibitor concentrations and the prediction of inhibitory drug drug interactions: pitfalls, progress and promise. Curr Drug Metab 7:1–14.
  • Bailey DG, Bend JR, Arnold JM, Tran LT, Spence JD. (1996). Erythromycin-felodipine interaction: magnitude, mechanism, and comparison with grapefruit juice. Clin Pharmacol Ther 60:25–33.
  • Bjornsson TD, Callaghan JT, Einolf HJ, Fischer V, Gan L, Grimm S, Kao J, King SP, Miwa G, Ni L, Kumar G, McLeod J, Obach RS, Roberts S, Roe A, Shah A, Snikeris F, Sullivan JT, Tweedie D, Vega JM, Walsh J, Wrighton SA; Pharmaceutical Research and Manufacturers of America (PhRMA) Drug Metabolism/Clinical Pharmacology Technical Working Group; FDA Center for Drug Evaluation and Research (CDER). (2003). The conduct of in vitro and in vivo drug-drug interaction studies: a Pharmaceutical Research and Manufacturers of America (PhRMA) perspective. Drug Metab Dispos 31:815–832.
  • Davies B, Morris T. (1993). Physiological parameters in laboratory animals and humans. Pharm Res 10:1093–1095.
  • Fahmi OA, Maurer TS, Kish M, Cardenas E, Boldt S, Nettleton D. (2008). A combined model for predicting CYP3A4 clinical net drug-drug interaction based on CYP3A4 inhibition, inactivation, and induction determined in vitro. Drug Metab Dispos 36:1698–1708.
  • Galetin A, Burt H, Gibbons L, Houston JB. (2006). Prediction of time-dependent CYP3A4 drug-drug interactions: impact of enzyme degradation, parallel elimination pathways, and intestinal inhibition. Drug Metab Dispos 34:166–175.
  • Granvil CP, Yu AM, Elizondo G, Akiyama TE, Cheung C, Feigenbaum L, Krausz KW, Gonzalez FJ. (2003). Expression of the human CYP3A4 gene in the small intestine of transgenic mice: in vitro metabolism and pharmacokinetics of midazolam. Drug Metab Dispos 31:548–558.
  • Higashikawa F, Murakami T, Kaneda T, Kato A, Takano M. (1999). Dose-dependent intestinal and hepatic first-pass metabolism of midazolam, a cytochrome P450 3A substrate with differently modulated enzyme activity in rats. J Pharm Pharmacol 51:67–72.
  • Honig PK, Wortham DC, Zamani K, Conner DP, Mullin JC, Cantilena LR. (1993). Terfenadine-ketoconazole interaction. Pharmacokinetic and electrocardiographic consequences. JAMA 269:1513–1518.
  • Kanazu T, Okamura N, Yamaguchi Y, Baba T, Koike M. (2005). Assessment of the hepatic and intestinal first-pass metabolism of midazolam in a CYP3A drug-drug interaction model rats. Xenobiotica 35:305–317.
  • Kanazu T, Yamaguchi Y, Okamura N, Baba T, Koike M. (2004). Model for the drug-drug interaction responsible for CYP3A enzyme inhibition. II: establishment and evaluation of dexamethasone-pretreated female rats. Xenobiotica 34:403–413.
  • Kotegawa T, Laurijssens BE, Von Moltke LL, Cotreau MM, Perloff MD, Venkatakrishnan K, Warrington JS, Granda BW, Harmatz JS, Greenblatt DJ. (2002). In vitro, pharmacokinetic, and pharmacodynamic interactions of ketoconazole and midazolam in the rat. J Pharmacol Exp Ther 302:1228–1237.
  • Kremers P. (2002). Can drug-drug interactions be predicted from in vitro studies? ScientificWorldJournal 2:751–766.
  • Kuroha M, Azumano A, Kuze Y, Shimoda M, Kokue E. (2002). Effect of multiple dosing of ketoconazole on pharmacokinetics of midazolam, a cytochrome P-450 3A substrate in beagle dogs. Drug Metab Dispos 30:63–68.
  • Lin JH, Lu AY. (1998). Inhibition and induction of cytochrome P450 and the clinical implications. Clin Pharmacokinet 35:361–390.
  • Mandlekar SV, Rose AV, Cornelius G, Sleczka B, Caporuscio C, Wang J, Marathe PH. (2007). Development of an in vivo rat screen model to predict pharmacokinetic interactions of CYP3A4 substrates. Xenobiotica 37:923–942.
  • Marathe PH, Rodrigues AD. (2006). In vivo animal models for investigating potential CYP3A- and Pgp-mediated drug-drug interactions. Curr Drug Metab 7:687–704.
  • Ogasawara A, Kume T, Kazama E. (2007). Effect of oral ketoconazole on intestinal first-pass effect of midazolam and fexofenadine in cynomolgus monkeys. Drug Metab Dispos 35:410–418.
  • Pang KS, Rowland M. (1977). Hepatic clearance of drugs. I. Theoretical considerations of a “well-stirred” model and a “parallel tube” model. Influence of hepatic blood flow, plasma and blood cell binding, and the hepatocellular enzymatic activity on hepatic drug clearance. J Pharmacokinet Biopharm 5:625–653.
  • Rodrigues AD. (2007). Prioritization of clinical drug interaction studies using in vitro cytochrome P450 data: proposed refinement and expansion of the “rank order” approach. Drug Metab Lett 1:31–35.
  • Rodrigues AD, Winchell GA, Dobrinska MR. (2001). Use of in vitro drug metabolism data to evaluate metabolic drug-drug interactions in man: the need for quantitative databases. J Clin Pharmacol 41:368–373.
  • Staffa JA, Chang J, Green L. (2002). Cerivastatin and reports of fatal rhabdomyolysis. N Engl J Med 346:539–540.
  • Tsunoda SM, Velez RL, von Moltke LL, Greenblatt DJ. (1999). Differentiation of intestinal and hepatic cytochrome P450 3A activity with use of midazolam as an in vivo probe: effect of ketoconazole. Clin Pharmacol Ther 66:461–471.
  • Vuppugalla R, Kim S, Zvyaga T, Han Y, Balimane P, Marathe P, Rodrigues AD. (2010). Anticipating and Minimizing Drug Interactions in a Drug Discovery and Development Setting: An Industrial Perspective. In:Pang KS, Rodrigues AD, Raimund PM, ed. Enzyme- and transporter-based drug-drug interactions: Progress and future challenges. New York: Springer, 585–624.
  • Weaver RJ. (2001). Assessment of drug-drug interactions: concepts and approaches. Xenobiotica 31:499–538.
  • White RE. (2000). High-throughput screening in drug metabolism and pharmacokinetic support of drug discovery. Annu Rev Pharmacol Toxicol 40:133–157.
  • Yao C, Levy RH. (2002). Inhibition-based metabolic drug-drug interactions: predictions from in vitro data. J Pharm Sci 91:1923–1935.
  • Zhang X, Galinsky RE, Kimura RE, Quinney SK, Jones DR, Hall SD. (2010). Inhibition of CYP3A by erythromycin: in vitro-in vivo correlation in rats. Drug Metab Dispos 38:61–72.

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.