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Xenobiotica
the fate of foreign compounds in biological systems
Volume 44, 2014 - Issue 11
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Xenobiotic Transporters

Characterization of gastrointestinal absorption of digoxin involving influx and efflux transporter in rats: application of mdr1a knockout (−/−) rats into absorption study of multiple transporter substrate

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Pages 1039-1045 | Received 17 Mar 2014, Accepted 29 Apr 2014, Published online: 19 May 2014

References

  • Augustine LM, Markelewicz RJ Jr, Boekelheide K, Cherrington NJ. (2005). Xenobiotic and endobiotic transporter mRNA expression in the blood-testis barrier. Drug Metab Dispos 33:182–9
  • Balimane PV, Patel K, Marino A, Chong S. (2004). Utility of 96 well Caco-2 cell system for increased throughput of P-gp screening in drug discovery. Eur J Pharm Biopharm 58:99–105
  • Bentz J, O'Connor MP, Bednarczyk D, et al. (2013). Variability in P-glycoprotein inhibitory potency (IC50) using various in vitro experimental systems: implications for universal digoxin drug-drug interaction risk assessment decision criteria. Drug Metab Dispos 41:1347–66
  • Bourdet DL, Pritchard JB, Thakker DR. (2005). Differential substrate and inhibitory activities of ranitidine and famotidine toward human organic cation transporter 1 (hOCT1; SLC22A1), hOCT2 (SLC22A2), and hOCT3 (SLC22A3). J Pharmacol Exp Ther 315:1288–97
  • Chandra P, Brouwer KL. (2004). The complexities of hepatic drug transport: current knowledge and emerging concepts. Pharm Res 21:719–35
  • Chen C, Liu X, Smith BJ. (2003). Utility of mdr1 gene-deficient mice in drug discovery and development. Curr Drug Metab 4:272–91
  • Chiba M, Ishii Y, Sugiyama Y. (2009). Prediction of hepatic clearance in human from in vitro data for successful drug development. AAPS J 11:262–76
  • Cummins CL, Jacobsen W, Benet LZ. (2002). Unmasking the dynamic interplay between intestinal P-glycoprotein and CYP3A4. J Pharmacol Exp Ther 300:1036–45
  • Doherty JE, Perkins WH. (1962). Studies with tritiated digoxin in human subjects after intravenous administration. Am Heart J 63:528–36
  • Fenner KS, Troutman MD, Kempshall S, et al. (2009). Drug-drug interactions mediated through P-glycoprotein: clinical relevance and in vitro-in vivo correlation using digoxin as a probe drug. Clin Pharmacol Ther 85:173–81
  • Fromm MF, Kim RB, Stein CM, et al. (1999). Inhibition of P-glycoprotein-mediated drug transport: a unifying mechanism to explain the interaction between digoxin and quinidine. Circulation 99:552–7
  • Funakoshi S, Murakami T, Yumoto R, et al. (2005). Role of organic anion transporting polypeptide 2 in pharmacokinetics of digoxin and methyldigoxin in rats. J Pharm Sci 94:1196–203
  • Gao B, Stieger B, Noé B, et al. (1999). Localization of the organic anion transporting polypeptide 2 (Oatp2) in capillary endothelium and choroids plexus epithelium of rat brain. J Histochem Cytochem 47:1255–63
  • Geurts AM, Cost GJ, Freyvert Y, et al. (2009). Knockout rats via embryo microinjection of zinc-finger nucleases. Science 325:433 . doi: 10.1126/science.1172447
  • Goralski KB, Hartmann G, Piquette-Miller M, Renton KW. (2003). Downregulation of mdr1a expression in the brain and liver during CNS inflammation alters the in vivo disposition of digoxin. Br J Pharmacol 139:35–48
  • Gramatté T, Oertel R, Terhaag B, Kirch W. (1996). Direct demonstration of small intestinal secretion and site-dependent absorption of the β-blocker talinolol in humans. Clin Pharmacol Ther 59:541–9
  • Harrison LI, Gibaldi M. (1976). Pharmacokinetics of digoxin in the rat. Drug Metab Dispos 4:88–93
  • Juliano RL, Ling V. (1976). A surface glycoprotein modulating drug permeability in Chinese hamster ovary cell mutants. Biochim Biophys Acta 455:152–62
  • Kallem R, Kulkarni CP, Patel D, et al. (2012). A simplified protocol employing elacridar in rodents: a screening model in drug discovery to assess P-gp mediated efflux at the blood brain barrier. Drug Metab Lett 6:134–44
  • Kato M, Chiba K, Hisaka A, et al. (2003). The intestinal first-pass metabolism of substrates of CYP3A4 and P-glycoprotein. Quantitative analysis based on information from the literature. Drug Metab Pharmacokinet 18:365–72
  • Koitabashi Y, Kumai T, Matsumoto N, et al. (2006). Orange juice increased the bioavailability of pravastatin, 3-hydroxi-3-methylglutaryl CoA reductase inhibitor, in rats and healthy human subjects. Life Sci 78:2852–9
  • Komura H, Iwaki M. (2008). Species difference in in vitro and in vivo small intestinal metabolism of CYP3A substrates. J Pharm Sci 97:1775–800
  • Komura H, Iwaki M. (2011). In vitro and in vivo small intestinal metabolism of CYP3A and UGT substrates in preclinical animals species and humans: species difference. Drug Metab Rev 43:476–98
  • Lam JL, Benet LZ. (2004). Hepatic microsome studies are insufficient to characterize in vivo hepatic metabolic clearance and metabolic drug-drug interactions: studies of digoxin metabolism in primary rat hepatocytes versus microsomes. Drug Metab Dispos 32:1311–16
  • Lin JH. (2007). Transporter-mediated drug interactions: clinical implications and in vitro assessment. Expert Opin Drug Metab Toxicol 3:81–92
  • Lumen AA, Li L, Li J, et al. (2013). Transporter inhibition of digoxin using several common P-gp expressing cell lines is not necessarily reporting only on inhibitor binding to P-gp. PLoS One 8:1–16
  • Minematsu T, Iwai M, Umehara K, et al. (2010). Characterization of human organic cation transporter 1 (OCT1/SLC22A1)- and OCT2 (SLC22A2)-mediated transport of 1-(2-methyoxyethyl)-2-methyl-4,9-dioxo-3-(pyrazin-2-ylmethyl)-4,9-dihydro-1H-naphtho[2,3-d]imidazolium bromide (YM155 monobromide), a novel small molecule survivin suppressant. Drug Metab Dispos 38:1–4
  • Ming X, Ju W, Wu H, et al. (2009). Transport of dicationic drugs pentamidine and furamidine by human organic cation transporters. Drug Metab Dispos 37:424–30
  • Nader AM, Foster DR. (2014). Suitability of digoxin as a P-glycoprotein probe: implications of other transporters on sensitivity and specificity. J Clin Pharmacol 54:3–13
  • Nishimura T, Kato Y, Amano N, et al. (2008). Species difference in intestinal absorption mechanism of etoposide and digoxin between cynomolgus monkey and rat. Pharm Res 25:2467–76
  • Pedersen KE, Dorph-Pedersen A, Hvidt S, et al. (1981). Digoxin-verapamil interaction. Clin Pharmacol Ther 30:311–16
  • Sakaeda T, Nakamura T, Horinouchi M, et al. (2001). MDR1 genotype-related pharmacokinetics of digoxin after single oral administration in healthy Japanese subjects. Pharm Res 18:1400–4
  • Salphati L, Benet LZ. (1998). Effects of ketoconazole on digoxin absorption and disposition in rat. Pharmacology 56:308–13
  • Salphati L, Benet LZ. (1999). Metabolism of digoxin and digoxigenin digitoxosides in rat liver microsomes: involvement of cytochrome P4503A. Xenobiotica 29:171–85
  • Shirasaka Y, Li Y, Shibue Y, et al. (2009). Concentration-dependent effect of naringin on intestinal absorption of β1-adrenoceptor antagonist talinolol mediated by P-glycoprotein and organic anion transporting polypeptide (Oatp). Pharm Res 26:560–7
  • Shirasaka Y, Kuraoka E, Spahn-Langguth H, et al. (2010). Species difference in the effect of grapefruit juice on intestinal absorption of talinolol between human and rat. J Pharmacol Exp Ther 332:181–9
  • Su SF, Huang JD. (1996). Inhibition of the intestinal digoxin absorption and exsorption by quinidine. Drug Metab Dispos 24:142–7
  • Sugimoto H, Hirabayashi H, Kimura Y, et al. (2011). Quantitative investigation of the impact of P-glycoprotein inhibition on drug transport across blood-brain barrier in rats. Drug Metab Dispos 39:8–14
  • Sun H, Huang Y, Frassetto L, Benet LZ. (2004). Effects of uremic toxins on hepatic uptake and metabolism of erythromycin. Drug Metab Dispos 32:1239–46
  • Tachibana T, Kato M, Sugiyama Y. (2012). Prediction of nonlinear intestinal absorption of CYP3A4 and P-glycoprotein substrates from their in vitro Km values. Pharm Res 29:651–68
  • Thiebaut F, Tsuruo T, Hamada H, et al. (1989). Immunohistochemical localization in normal tissues of different epitopes in the multidrug transport protein P170: evidence for localization in brain capillaries and crossreactivity of one antibody with a muscle protein. J Histochem Cytochem 37:159–64
  • Tsuda M, Terada T, Ueba M, et al. (2009). Involvement of human multidrug and toxin extrusion 1 in the drug interaction between cimetidine and metformin in renal epithelial cells. J Pharmacol Exp Ther 329:185–91
  • Walters HC, Craddock AL, Fusegawa H, et al. (2000). Expression, transport properties, and chromosomal location of organic anion transporter subtype 3. Am J Physiol Gastrointest Liver Physiol 279:G1188–200
  • Weiss M, Li P, Roberts MS. (2010). An improved nonlinear model describing the hepatic pharmacokinetics of digoxin: evidence for two functionally different uptake systems and saturable binding. Pharm Res 27:1999–2007
  • Yarim M, Moro S, Huber R, et al. (2005). Application of QSAR analysis to organic anion transporting polypeptide 1a5 (Oatp1a5) substrates. Bioorg Med Chem 13:463–71
  • Zhang H, Yao M, Morrison RA, Chong S. (2003). Commonly used surfactant, Tween 80, improves absorption of P-glycoprotein substrate, digoxin, in rats. Arch Pharm Res 26:768–72

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