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Xenobiotica
the fate of foreign compounds in biological systems
Volume 44, 2014 - Issue 12
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Research Article

Role of hepatic blood flow and metabolism in the pharmacokinetics of ten drugs in lean, aged and obese rats

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Pages 1108-1116 | Received 27 Mar 2014, Accepted 04 Jun 2014, Published online: 20 Jun 2014

References

  • Abernethy DR, Greenblatt DJ. (1985). Phenytoin disposition in obesity. Determination of loading dose. Arch Neurol 42:468–71
  • Abernethy DR, Greenblatt DJ, Divoll M, et al. (1981). Alterations in drug distribution and clearance due to obesity. J Pharmacol Exp Ther 217:681–5
  • Abernethy DR, Greenblatt DJ, Divoll M, Shader RI. (1983). Prolonged accumulation of diazepam in obesity. J Clin Pharmacol 23:369–76
  • Andersson T, Miners JO, Veronese ME, Birkett DJ. (1994). Diazepam metabolism by human liver microsomes is mediated by both S-mephenytoin hydroxylase and CYP3A isoforms. Br J Clin Pharmacol 38:131–7
  • Ashforth EI, Carlile DJ, Chenery R, Houston JB. (1995). Prediction of in vivo disposition from in vitro systems: clearance of phenytoin and tolbutamide using rat hepatic microsomal and hepatocyte data. J Pharmacol Exp Ther 274:761–6
  • Bae SK, Cao S, Seo KA, et al. (2008). Cytochrome P450 2B6 catalyzes the formation of pharmacologically active sibutramine (N-{1-[1-(4-chlorophenyl)cyclobutyl]-3-methylbutyl}-N,N-dimethylamine) metabolites in human liver microsomes. Drug Metab Dispos 36:1679–88
  • Bargar EM, Walle UK, Bai SA, Walle T. (1983). Quantitative metabolic fate of propranolol in the dog, rat, and hamster using radiotracer, high performance liquid chromatography, and gas chromatography-mass spectrometry techniques. Drug Metab Dispos 11:266–72
  • Belpaire FM, Rosseel MT, Vermeulen AM, et al. (1993). Stereoselective pharmacokinetics of atenolol in the rat: influence of aging and of renal failure. Mech Ageing Dev 67:201–10
  • Blouin RA, Bauer LA, Miller DD, et al. (1982). Vancomycin pharmacokinetics in normal and morbidly obese subjects. Antimicrob Agents Chemother 21:575–80
  • Blouin RA, Warren GW. (1999). Pharmacokinetic considerations in obesity. J Pharm Sci 88:1–7
  • Bogaards JJ, Bertrand M, Jackson P, et al. (2000). Determining the best animal model for human cytochrome P450 activities: a comparison of mouse, rat, rabbit, dog, micropig, monkey and man. Xenobiotica 30:1131–52
  • Brill MJ, Diepstraten J, van Rongen A, et al. (2012). Impact of obesity on drug metabolism and elimination in adults and children. Clin Pharmacokinet 51:277–304
  • Casati A, Putzu M. (2005). Anesthesia in the obese patient: pharmacokinetic considerations. J Clin Anesth 17:134–45
  • Cheymol G. (2000). Effects of obesity on pharmacokinetics implications for drug therapy. Clin Pharmacokinet 39:215–31
  • Cheymol G, Poirier JM, Carrupt PA, et al. (1997). Pharmacokinetics of β-adrenoceptor blockers in obese and normal volunteers. Br J Clin Pharmacol 43:563–70
  • Cho S-J, Yoon I-S, Kim D-D. (2013). Obesity-related physiological changes and their pharmacokinetic consequences. J Pharm Invest 43:161–9
  • Doose DR, Wang SS, Padmanabhan M, et al. (2003). Effect of topiramate or carbamazepine on the pharmacokinetics of an oral contraceptive containing norethindrone and ethinyl estradiol in healthy obese and nonobese female subjects. Epilepsia 44:540–9
  • Edelman AB, Cherala G, Stanczyk FZ. (2010). Metabolism and pharmacokinetics of contraceptive steroids in obese women: a review. Contraception 82:314–23
  • Engineer MS, Ho DH, Bodey GP Sr. (1981). Comparison of vancomycin disposition in rats with normal and abnormal renal functions. Antimicrob Agents Chemother 20:718–22
  • Farrell GC, Teoh NC, McCuskey RS. (2008). Hepatic microcirculation in fatty liver disease. Anat Rec 291:684–92
  • Fracasso C, Guiso G, Garattini S, Caccia S. (1988). Disposition of D-fenfluramine in lean and obese rats. Appetite 10:45–55
  • Ghobadi C, Johnson TN, Aarabi M, et al. (2011). Application of a systems approach to the bottom-up assessment of pharmacokinetics in obese patients: expected variations in clearance. Clin Pharmacokinet 50:809–22
  • Hanley MJ, Abernethy DR, Greenblatt DJ. (2010). Effect of obesity on the pharmacokinetics of drugs in humans. Clin Pharmacokinet 49:71–87
  • Igari Y, Sugiyama Y, Sawada Y, et al. (1982). Tissue distribution of 14C-diazepam and its metabolites in rats. Drug Metab Dispos 10:676–9
  • Irizar A, Barnett CR, Flatt PR, Ioannides C. (1995). Defective expression of cytochrome P450 proteins in the liver of the genetically obese Zucker rat. Eur J Pharmacol 293:385–93
  • Marchant NC, Breen MA, Wallace D, et al. (1992). Comparative biodisposition and metabolism of 14C-(±)-fenfluramine in mouse, rat, dog and man. Xenobiotica 22:1251–66
  • McCuskey RS, Ito Y, Robertson GR, et al. (2004). Hepatic microvascular dysfunction during evolution of dietary steatohepatitis in mice. Hepatology 40:386–93
  • Mehvar R, Gross ME, Kreamer RN. (1990). Pharmacokinetics of atenolol enantiomers in humans and rats. J Pharm Sci 79:881–5
  • Micu AL, Miksys S, Sellers EM, et al. (2003). Rat hepatic CYP2E1 is induced by very low nicotine doses: an investigation of induction, time course, dose response, and mechanism. J Pharmacol Exp Ther 306:941–7
  • Mokdad AH, Ford ES, Bowman BA, et al. (2003). Prevalence of obesity, diabetes, and obesity-related health risk factors, 2001. JAMA 289:76–9
  • Moon YJ, Lee AK, Chung HC, et al. (2003). Effects of acute renal failure on the pharmacokinetics of chlorzoxazone in rats. Drug Metab Dispos 31:776–84
  • Must A, Spadano J, Coakley EH, et al. (1999). The disease burden associated with overweight and obesity. JAMA 282:1523–9
  • Nakamura T, Takano M, Yasuhara M, Inui K. (1996). In-vivo clearance study of vancomycin in rats. J Pharm Pharmacol 48:1197–200
  • O'Shea D, Davis SN, Kim RB, Wilkinson GR. (1994). Effect of fasting and obesity in humans on the 6-hydroxylation of chlorzoxazone: a putative probe of CYP2E1 activity. Clin Pharmacol Ther 56:359–67
  • Pasarin M, La Mura V, Gracia-Sancho J, et al. (2012). Sinusoidal endothelial dysfunction precedes inflammation and fibrosis in a model of NAFLD. PLoS One 7:e32785
  • Roberts BJ, Song BJ, Soh Y, et al. (1995). Ethanol induces CYP2E1 by protein stabilization. Role of ubiquitin conjugation in the rapid degradation of CYP2E1. J Biol Chem 270:29632–5
  • Sadeque AJ, Usmani KA, Palamar S, et al. (2012). Identification of human UDP-glucuronosyltransferases involved in N-carbamoyl glucuronidation of lorcaserin. Drug Metab Dispos 40:772–8
  • Saito K, Sakai N, Kim HS, et al. (2004). Strain differences in diazepam metabolism at its three metabolic sites in sprague-dawley, brown norway, dark agouti, and wistar strain rats. Drug Metab Dispos 32:959–65
  • Salazar DE, Sorge CL, Corcoran GB. (1988). Obesity as a risk factor for drug-induced organ injury. VI. Increased hepatic P450 concentration and microsomal ethanol oxidizing activity in the obese overfed rat. Biochem Biophys Res Commun 157:315–20
  • Saltiel AR. (2000). Series introduction: the molecular and physiological basis of insulin resistance: emerging implications for metabolic and cardiovascular diseases. J Clin Invest 106:163–4
  • Wang M, Tian X, Leung L, et al. (2011). Comparative pharmacokinetics and metabolism studies in lean and diet- induced obese mice: an animal efficacy model for 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitors. Drug Metab Lett 5:55–63
  • Wojcicki J, Jaroszynska M, Drozdzik M, et al. (2003). Comparative pharmacokinetics and pharmacodynamics of propranolol and atenolol in normolipaemic and hyperlipidaemic obese subjects. Biopharm Drug Dispos 24:211–18
  • Yamazaki H, Komatsu T, Takemoto K, et al. (2001). Decreases in phenytoin hydroxylation activities catalyzed by liver microsomal cytochrome P450 enzymes in phenytoin-treated rats. Drug Metab Dispos 29:427–34
  • Yang TJ, Shou M, Korzekwa KR, et al. (1998). Role of cDNA-expressed human cytochromes P450 in the metabolism of diazepam. Biochem Pharmacol 55:889–96
  • Yoshimoto K, Echizen H, Chiba K, et al. (1995). Identification of human CYP isoforms involved in the metabolism of propranolol enantiomers--N-desisopropylation is mediated mainly by CYP1A2. Br J Clin Pharmacol 39:421–31
  • Yoshinari K, Takagi S, Yoshimasa T, et al. (2006). Hepatic CYP3A expression is attenuated in obese mice fed a high-fat diet. Pharm Res 23:1188–200

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