Dose-dependent pharmacokinetics of midazolam in rats: influence of hepatic first-pass metabolism

References

• Aiba T, Takehara Y, Okuno M, Hashimoto Y. 2003. Poor correlation between intestinal and hepatic metabolic rates of CYP3A4 substrates in rats. Pharm Res. 20 (5):745–748.
   PubMed Web of Science ®Google Scholar
• Brown HS, Wilby AJ, Alder J, Houston JB. 2010. Comparative use of isolated hepatocytes and hepatic microsomes for cytochrome P450 inhibition studies: transporter-enzyme interplay. Drug Metab Dispos. 38 (12):2139–2146.
   PubMed Web of Science ®Google Scholar
• Chien JY, Lucksiri A, Ernest CS, Gorski JC, Wrighton SA, Hall SD. 2006. Stochastic prediction of Cyp3a-mediated inhibition of midazolam clearance by ketoconazole. Drug Metab Dispos. 34 (7):1208–1219.
   PubMed Web of Science ®Google Scholar
• Debri K, Boobis AR, Davies DS, Edwards RJ. 1995. Distribution and induction of CYP3A1 and CYP3A2 in rat liver and extrahepatic tissues. Biochem Pharmacol. 50 (12):2047–2056.
   PubMed Web of Science ®Google Scholar
• Fasinu PS, Gutmann H, Schiller H, James A-D, Bouic PJ, Rosenkranz B. 2013. The potential of Sutherlandia frutescens for herb-drug interaction. Drug Metab Dispos. 41 (2):488–497.
   PubMed Web of Science ®Google Scholar
• Ghosal A, Satoh H, Thomas PE, 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 (9):940–947.
   PubMed Web of Science ®Google Scholar
• Hamdy DA, Brocks DR. 2011. Effect of hyperlipidemia on ketoconazole–midazolam drug–drug interaction in rat. J Pharm Sci. 100 (11):4986–4992.
   PubMed Web of Science ®Google Scholar
• 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 (1):67–72.
   PubMed Web of Science ®Google Scholar
• Jiang X, Zhuang Y, Xu Z, Wang W, Zhou H. 2016. Development of a physiologically based pharmacokinetic model to predict disease-mediated therapeutic protein–drug interactions: modulation of multiple cytochrome P450 enzymes by interleukin-6. Aaps J. 18 (3):767–776.
   PubMed Web of Science ®Google Scholar
• Kajikawa N, Doi M, Kusaba J-i, Aiba T. 2014. Effect of carrageenan-induced acute peripheral inflammation on the pharmacokinetics and hepatic metabolism of midazolam in rats. Drug Metab Pharmacokinet. 29 (5):400–406.
   PubMed Web of Science ®Google Scholar
• Kanazawa H, Okada A, Igarashi E, Higaki M, Miyabe T, Sano T, Nishimura R. 2004. Determination of midazolam and its metabolite as a probe for cytochrome P450 3A4 phenotype by liquid chromatography–mass spectrometry. J Chromatogr A. 1031 (1-2):213–218.
   PubMed Web of Science ®Google Scholar
• 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 (4):305–317.
   PubMed Web of Science ®Google Scholar
• Kobayashi K, Urashima K, Shimada N, Chiba K. 2002. Substrate specificity for rat cytochrome P450 (CYP) isoforms: screening with cDNA-expressed systems of the rat. Biochem Pharmacol. 63 (5):889–896.
   PubMed Web of Science ®Google Scholar
• 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 (3):1228–1237.
   PubMed Web of Science ®Google Scholar
• Kronbach T, Mathys D, Umeno M, Gonzalez FJ, Meyer UA. 1989. Oxidation of midazolam and triazolam by human liver cytochrome P450IIIA4. Mol Pharmacol. 36 (1):89–96.
   PubMed Web of Science ®Google Scholar
• Kuze J, Mutoh T, Takenaka T, Morisaki K, Nakura H, Hanioka N, Narimatsu S. 2009. Separate evaluation of intestinal and hepatic metabolism of three benzodiazepines in rats with cannulated portal and jugular veins: comparison with the profile in non-cannulated mice. Xenobiotica. 39 (11):871–880.
   PubMed Web of Science ®Google Scholar
• Lee LS, Bertino JS, Jr, Nafziger AN. 2006. Limited sampling models for oral midazolam: midazolam plasma concentrations, not the ratio of 1-hydroxymidazolam to midazolam plasma concentrations, accurately predicts AUC as a biomarker of CYP3A activity. J Clin Pharmacol. 46(2):229–234.
   PubMed Web of Science ®Google Scholar
• Lee JS, Kim SH. 2019. Dose-dependent pharmacokinetics of tofacitinib in rats: influence of hepatic and intestinal first-pass metabolism. Pharmaceutics. 11 (7):318.
   PubMed Web of Science ®Google Scholar
• Lenoir C, Niederer A, Rollason V, Desmeules JA, Daali Y, Samer CF. 2022. Prediction of cytochromes P450 3A and 2C19 modulation by both inflammation and drug interactions using physiologically based pharmacokinetics. CPT Pharmacometrics Syst Pharmacol. 11(1):30–43.
   PubMedGoogle Scholar
• Lin Y, Wei Y, Hu X, Wu M-L, Yao J, Ying X, Fu X, Ding M, Qiao L. 2019. Evaluation of lentinan effects on cytochrome P450 activity in rats by a cocktail method. Iran J Basic Med Sci. 22 (3):296–301.
   PubMed Web of Science ®Google Scholar
• Mao J, Mohutsky MA, Harrelson JP, Wrighton SA, Hall SD. 2011. Prediction of CYP3A-mediated drug-drug interactions using human hepatocytes suspended in human plasma. Drug Metab Dispos. 39 (4):591–602.
   PubMed Web of Science ®Google Scholar
• Murakami T, Nakanishi M, Yoshimori T, Okamura N, Norikura R, Mizojiri K. 2003. Separate assessment of intestinal and hepatic first-pass effects using a rat model with double cannulation of the portal and jugular veins. Drug Metab Pharmacokinet. 18 (4):252–260.
   PubMedGoogle Scholar
• Nishimura T, Amano N, Kubo Y, Ono M, Kato Y, Fujita H, Kimura Y, Tsuji A. 2007. Asymmetric intestinal first-pass metabolism causes minimal oral bioavailability of midazolam in cynomolgus monkey. Drug Metab Dispos. 35 (8):1275–1284.
   PubMed Web of Science ®Google Scholar
• Qin X, Duan W, Xue X, Chen X, Huang M, Bi H. 2016. Optimization of midazolam dosage and pharmacokinetics of CYP3A probe substrate in rats. Acta Pharmaceutica Sinica. 51 (05):834–838.
   PubMedGoogle Scholar
• Riegelman S, Loo JCK, Rowland M. 1968. Shortcomings in pharmacokinetic analysis by conceiving the body to exhibit properties of a single compartment. J Pharm Sci. 57 (1):117–123.
   PubMed Web of Science ®Google Scholar
• Sekiguchi N, Kato M, Takada M, Watanabe H, Higashida A, Sakai S, Ishigai M, Aso Y. 2008. In vivo approach for the evaluation of mechanism-based inhibition of cytochrome P450 3A in rats. Xenobiotica. 38 (4):368–381.
   PubMed Web of Science ®Google Scholar
• Sekiguchi N, Kato M, Takada M, Watanabe H, Takata S, Mitsui T, Aso Y, Ishigai M. 2011. Quantitative prediction of mechanism-based inhibition caused by mibefradil in rats. Drug Metab Dispos. 39 (7):1255–1262.
   PubMed Web of Science ®Google Scholar
• Tabata K, Yamaoka K, Fukuyama T, Nakagawa T. 1995. Evaluation of intestinal absorption into the portal system in enterohepatic circulation by measuring the difference in portal–venous blood concentrations of diclofenac. Pharm Res. 12 (6):880–883.
   PubMed Web of Science ®Google Scholar
• Taesotikul T, Nakajima M, Tassaneeyakul W, Yokoi T. 2012. Effects of Phyllanthus amarus on the pharmacokinetics of midazolam and cytochrome P450 activities in rats. Xenobiotica. 42 (7):641–648.
   PubMed Web of Science ®Google Scholar
• Thummel KE, O'Shea D, Paine MF, Shen DD, Kunze KL, Perkins JD, Wilkinson GR. 1996. Oral first-pass elimination of midazolam involves both gastrointestinal and hepatic CYP3A-mediated metabolism*. Clin Pharmacol Ther. 59 (5):491–502.
   PubMed Web of Science ®Google Scholar
• Thummel KE, Shen DD, Podoll TD, Kunze KL, Trager WF, Hartwell PS, Raisys VA, Marsh CL, McVicar JP, Barr DM. 1994. 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 (1):549–556.
   PubMed Web of Science ®Google Scholar
• Venkatapura Chandrashekar D, DuBois B, Mehvar R. 2021. UPLC-MS/MS analysis of the Michaelis-Menten kinetics of CYP3A-mediated midazolam 1′- and 4-hydroxylation in rat brain microsomes. J Chromatogr B Analyt Technol Biomed Life Sci. 1180:122892.
   PubMed Web of Science ®Google Scholar
• Vuppugalla R, Zhang Y, Chang S, Rodrigues AD, Marathe PH. 2012. Impact of nonlinear midazolam pharmacokinetics on the magnitude of the midazolam-ketoconazole interaction in rats. Xenobiotica. 42 (11):1058–1068.
   PubMed Web of Science ®Google Scholar
• Wandel C, Böcker R, Böhrer H, Browne A, Rügheimer E, Martin E. 1994. Midazolam is metabolized by at least three different cytochrome P450 enzymes. Br J Anaesth. 73 (5):658–661.
   PubMed Web of Science ®Google Scholar
• Wu C-Y, Benet LZ. 2005. Predicting drug disposition via application of BCS: transport/absorption/elimination interplay and development of a biopharmaceutics drugdisposition classification system. Pharm Res. 22 (1):11–23.
   PubMed Web of Science ®Google Scholar
• Xia C, Sun J, Wang G, Shang L, Zhang X, Zhang R, Peng Y, Wang X, Hao H, Xie L, et al. 2010. Herb-drug interactions: in vivo and in vitro effect of Shenmai injection, a herbal preparation, on the metabolic activities of hepatic cytochrome P450 3A1/2, 2C6, 1A2, and 2E1 in rats. Planta Med. 76 (3):245–250.
   PubMed Web of Science ®Google Scholar
• Yamamoto S, Kosugi Y, Hirabayashi H, Moriwaki T. 2018. Impact of P-glycoprotein on intestinal absorption of an inhibitor of apoptosis protein antagonist in rats: mechanisms of nonlinear pharmacokinetics and food effects. Pharm Res. 35(10):190.
   PubMed Web of Science ®Google Scholar