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

Xenobiotica

Volumn 44, Issue 11, 2014, Pages 1039-1045

  Suzuki, Motoya ^a   Komura, Hiroshi ^a   Yoshikawa, Tomonori ^a   Enya, Seiji ^a   Nagao, Akemi ^a   Takubo, Hiroaki ^a   Kogayu, Motohiro ^a  

^a JAPAN TOBACCO INC   (Japan)

Author keywords

Absorption; Digoxin; Knockout rat; Oatp; P glycoprotein; Quinidine

Indexed keywords

AURANTIIN; DIGOXIN; GLYCOPROTEIN; MULTIDRUG RESISTANCE PROTEIN 1A; ORGANIC ANION TRANSPORTER; QUINIDINE SULFATE; UNCLASSIFIED DRUG; FLAVANONE DERIVATIVE; MULTIDRUG RESISTANCE PROTEIN; MULTIDRUG RESISTANCE PROTEIN 3; QUINIDINE; SLCO1A5 PROTEIN, RAT;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; DRUG ABSORPTION; DRUG BLOOD LEVEL; DRUG ELIMINATION; DRUG HALF LIFE; GASTROINTESTINAL ABSORPTION; MAXIMUM PLASMA CONCENTRATION; NONHUMAN; PLASMA CONCENTRATION-TIME CURVE; RAT; TIME TO MAXIMUM PLASMA CONCENTRATION; WILD TYPE; ANIMAL; GENE INACTIVATION; GENETICS; METABOLISM; SPRAGUE DAWLEY RAT;

RATTUS;

ANIMALS; DIGOXIN; FLAVANONES; GASTROINTESTINAL ABSORPTION; GENE KNOCKOUT TECHNIQUES; ORGANIC ANION TRANSPORTERS, SODIUM-INDEPENDENT; P-GLYCOPROTEINS; QUINIDINE; RATS; RATS, SPRAGUE-DAWLEY;

EID: 84911462568     PISSN: 00498254     EISSN: 13665928     Source Type: Journal    
DOI: 10.3109/00498254.2014.920551     Document Type: Article

References (46)

1. Augustine LM, Markelewicz Jr RJ, Boekelheide K, Cherrington NJ. (2005). Xenobiotic and endobiotic transporter mRNA expression in the blood-testis barrier. Drug Metab Dispos 33:182-9.
2. 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.
3. Bentz J, O'Connor MP, Bednarczyk D, et al. (2013). Variability in Pglycoprotein 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.
4. 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.
5. Chandra P, Brouwer KL. (2004). The complexities of hepatic drug transport: current knowledge and emerging concepts. Pharm Res 21: 719-35.
6. Chen C, Liu X, Smith BJ. (2003). Utility of mdr1 gene-deficient mice in drug discovery and development. Curr Drug Metab 4:272-91.
7. 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.
8. Cummins CL, Jacobsen W, Benet LZ. (2002). Unmasking the dynamic interplay between intestinal P-glycoprotein and CYP3A4. J Pharmacol Exp Ther 300:1036-45.
9. Doherty JE, Perkins WH. (1962). Studies with tritiated digoxin in human subjects after intravenous administration. Am Heart J 63: 528-36.
10. 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.
11. Fromm MF, Kim RB, Stein CM, et al. (1999). Inhibition of Pglycoprotein-mediated drug transport: a unifying mechanism to explain the interaction between digoxin and quinidine. Circulation 99:552-7.
12. 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.
13. 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.
14. 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.
15. 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.
16. Gramatté T, Oertel R, Terhaag B, Kirch W. (1996). Direct demonstration of small intestinal secretion and site-dependent absorption of the b-blocker talinolol in humans. Clin Pharmacol Ther 59:541-9.
17. Harrison LI, Gibaldi M. (1976). Pharmacokinetics of digoxin in the rat. Drug Metab Dispos 4:88-93.
18. Juliano RL, Ling V. (1976). A surface glycoprotein modulating drug permeability in Chinese hamster ovary cell mutants. Biochim Biophys Acta 455:152-62.
19. 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.
20. 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.
21. 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.
22. 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.
23. 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.
24. Lam JL, Benet LZ. (2004). Hepatic microsome studies are insufficient to characterize in vivo hepatic metabolic clearance and metabolic drugdrug interactions: studies of digoxin metabolism in primary rat hepatocytes versus microsomes. Drug Metab Dispos 32:1311-16.
25. Lin JH. (2007). Transporter-mediated drug interactions: clinical implications and in vitro assessment. Expert Opin Drug Metab Toxicol 3: 81-92.
26. 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.
27. 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.
28. 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.
29. 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.
30. 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.
31. Pedersen KE, Dorph-Pedersen A, Hvidt S, et al. (1981). Digoxinverapamil interaction. Clin Pharmacol Ther 30:311-16.
32. Sakaeda T, Nakamura T, Horinouchi M, et al. (2001). MDR1 genotyperelated pharmacokinetics of digoxin after single oral administration in healthy Japanese subjects. Pharm Res 18:1400-4.
33. Salphati L, Benet LZ. (1998). Effects of ketoconazole on digoxin absorption and disposition in rat. Pharmacology 56:308-13.
34. Salphati L, Benet LZ. (1999). Metabolism of digoxin and digoxigenin digitoxosides in rat liver microsomes: involvement of cytochrome P4503A. Xenobiotica 29:171-85.
35. 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.
36. 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.
37. Su SF, Huang JD. (1996). Inhibition of the intestinal digoxin absorption and exsorption by quinidine. Drug Metab Dispos 24:142-7.
38. 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.
39. 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.
40. 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.
41. 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.
42. 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.
43. 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.
44. 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.
45. 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.
46. 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.