Effect of P-glycoprotein on intestinal absorption and brain penetration of antiallergic agent bepotastine besilate

Drug Metabolism and Disposition

Volumn 34, Issue 5, 2006, Pages 793-799

  Ohashi, Rikiya ^a   Kamikozawa, Yukari ^a   Sugiura, Mika ^a   Fukuda, Hajime ^a   Yabuuchi, Hikaru ^b   Tamai, Ikumi ^c  

^a MITSUBISHI TANABE PHARMA CORPORATION   (Japan)

^b GenoMembrane Inc   (Japan)

^c TOKYO UNIVERSITY OF SCIENCE   (Japan)

Author keywords

[No Author keywords available]

Indexed keywords

ADENOSINE TRIPHOSPHATASE; ANTIALLERGIC AGENT; BETOTASTINE; CARBON 14; CYCLOSPORIN A; FEXOFENADINE; GLYCOPROTEIN P; GLYCOPROTEIN P INHIBITOR; MULTIDRUG RESISTANCE PROTEIN 1; QUINIDINE; VERAPAMIL;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; BINDING AFFINITY; CELL STRAIN; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG ABSORPTION; DRUG BLOOD LEVEL; DRUG BRAIN LEVEL; DRUG DISTRIBUTION; DRUG PENETRATION; DRUG PROTEIN BINDING; DRUG TRANSPORT; ENZYME ACTIVITY; ENZYME ASSAY; INTESTINE ABSORPTION; INTESTINE MUCOSA PERMEABILITY; KNOCKOUT MOUSE; MALE; MOUSE; MOUSE STRAIN; NONHUMAN; PRIORITY JOURNAL; PROTEIN EXPRESSION; RAT; SMALL INTESTINE; STRAIN DIFFERENCE; WILD TYPE;

ADENOSINE TRIPHOSPHATASES; ANIMALS; ANTI-ALLERGIC AGENTS; AUTORADIOGRAPHY; BIOLOGICAL TRANSPORT, ACTIVE; BRAIN; CHROMATOGRAPHY, LIQUID; INTESTINAL ABSORPTION; KINETICS; LLC-PK1 CELLS; MALE; MASS SPECTROMETRY; MICE; MICE, KNOCKOUT; P-GLYCOPROTEIN; PIPERIDINES; PYRIDINES; RATS; RATS, SPRAGUE-DAWLEY; STIMULATION, CHEMICAL; SWINE; TERFENADINE; VERAPAMIL;

ANIMALIA;

EID: 33645827555     PISSN: 00909556     EISSN: 1521009X     Source Type: Journal    
DOI: 10.1124/dmd.105.007559     Document Type: Article

References (38)

1. Adachi Y, Suzuki H, and Sugiyama Y (2001) Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res (NY) 18:1660-1668.
2. Artursson P (1990) Epithelial transport of drugs in cell culture. I: a model for studying the passive diffusion of drugs over intestinal absorptive (Caco-2) cells. J Pharm Sci 79:476-482.
3. Cvetkovic M, Leake B, Fromm MF, Wilkinson GR, and Kim RB (1999) OATP and P-glycoprotein transporters mediate the cellular uptake and excretion of fexofenadine. Drug Metab Dispos 27:866-871.
4. Dresser GK, Bailey DG, Leake BF, Schwarz UI, Dawson PA, Freeman DI, and Kim RB (2002) Fruit juices inhibit organic anion transporting polypeptide-mediated drug uptake to decrease the oral availability of fexofenadine. Clin Pharmacol Ther 71:11-20.
5. Dresser GK, Kim RB, and Bailey DG (2005) Effect of grapefruit juice volume on the reduction of fexofenadine bioavailability: possible role of organic anion transporting polypeptides. Clin Pharmacol Ther 77:170-177.
6. Fricker G, Drewe J, Huwyler J, Gutmann H, and Beglinger C (1996) Relevance of p-glycoprotein for the enteral absorption of cyclosporin A: in vitro-in vivo correlation. Br J Pharmacol 118:1841-1847.
7. 14C]ebastine after a single administration in rats. Arzneim-Forsch 44:527-538.
8. Honda H, Murata K, Hamazaki A, Sakamoto O, Ueno H, and Fujiwara H (1997) Inhibitory effect of betotastine on anaphylactic and histamine-induced reactions in guinea pig. Jpn Pharmacol Ther 25:879-888.
9. Ishiguro N, Nozawa T, Tsujihata A, Saito A, Kishimoto W, Yokoyama K, Yotsumoto T, Sakai K, Igarashi T, and Tamai I (2004) Influx and efflux transport of H1-antagonist epinastine across the blood-brain barrier. Drug Metab Dispos 32:519-524.
10. Kadosaka T, Shiraishi K, Mizuuchi H, Maki T, Banno K, and Sato T (1997) Phase I study of TAU-284: repeated oral administration in healthy male volunteers. J Clin Ther Med 13:1155-1168.
11. Kamath AV, Yao M, Zhang Y, and Chong S (2005) Effect of fruit juices on the oral bioavailability of fexofenadine in rats. J Pharm Sci 94:233-239.
12. Kato M, Nishida A, Aga Y, Kita J, Kudo Y, Narita H, and Endo T (1997) Pharmacokinetic and pharmacodynamic evaluation of central effect of the novel antiallergic agent betotastine besilate. Arzneim-Forsch 47:1116-1124.
13. Lin JH and Yamazaki M (2003) Clinical relevance of P-glycoprotein in drug therapy. Drug Metab Rev 35:417-454.
14. Mizuuchi H, Katsura T, Saito H, Hashimoto Y, and Inui KI (1999) Transport characteristics of diphenhydramine in human intestinal epithelial Caco-2 cells: contribution of pH-dependent transport system. J Pharmacol Exp Ther 290:388-392.
15. Mouly S and Paine MF (2003) P-glycoprotein increases from proximal to distal regions of human small intestine. Pharm Res (NY) 20:1595-1599.
16. Nicholson AN (1983) Antihistamines and sedation. Lancet 2:211-212.
17. Nozawa T, Imai K, Nezu J, Tsuji A, and Tamai I (2004) Functional characterization of pH-sensitive organic anion transporting polypeptide OATP-B in human. J Pharmacol Exp Ther 308:438-445.
18. Ohashi R, Tsukimoto M, Nakamura S, Ohtsuka M, Hayashi K, Nishiyama S, Hanawa S, Mitsugi K, and Esumi Y (1997) Pharmacokinetic study of betotastine besilate (TAU-284) (I): absorption, distribution, metabolism and excretion after a single oral administration. Xenobio Metab Dispos 12:417-438.
19. Polli JW, Baughman TM, Humphreys JE, Jordan KH, Mote AL, Salisbury JA, Tippin TK, and Serabjit-Singh CJ (2003) P-glycoprotein influences the brain concentrations of cetirizine (Zyrtec), a second-generation non-sedating antihistamine. J Pharm Sci 92:2082-2089.
20. Sakai A, Kikuchi M, Yato N, Kikkawa S, Saito N, and Narita H (1997) Inhibitory effect of betotastine besilate on antigen-induced airway eosinophil infiltration and peripheral blood eosinophilia in mice. Arzneim-forsch 47:954-958.
21. Schinkel AH, Smit JJ, van Tellingen O, Beijnen JH, Wagenaar E, van Deemter L, Mol CA, van der Valk MA, Robanus-Mandaag EC, te Riele HPJ, et al. (1994) Disruption of the mouse mdr1a P-glycoprotein gene leads to a deficiency in the blood-brain barrier and to increased sensitivity to drugs. Cell 77:491-502.
22. Tagawa M, Kano M, Okamura N, Higuchi M, Matsuda M, Mizuki Y, Arai H, Iwata R, Fujii T, Komemushi S, et al. (2001) Neuroimaging of histamine H1-receptor occupancy in human brain by positron emission tomography (PET): a comparative study of ebastine, a second-generation antihistamine and (+)-chlorpheniramine, a classical antihistamine. Br J Clin Pharmacol 52:501-509.
23. Tahara H, Kusuhara H, Fuse E, and Sugiyama Y (2005) P-glycoprotein plays a major role in the efflux of fexofenadine in the small intestine and blood-brain barrier, but only a limited role in its biliary excretion. Drug Metab Dispos 33:963-968.
24. Takara K, Ohnishi N, Horibe S, and Yokoyama T (2003) Expression profiles of drug-metabolizing enzyme CYP3A and drug efflux transporter multidrug resistance 1 subfamily mRNAs in small intestine. Drug Metab Dispos 31:1235-1239.
25. Tamai I, Kido Y, Yamashita J, Sai Y, and Tsuji A (2000) Blood-brain barrier transport of H1-antagonist ebastine and its metabolite carebastine. J Drug Target 8:383-393.
26. Tamura S, Ohike A, Ibuki R, Amidon GL, and Yamashita S (2002) Tacrolimus is a class II low-solubility high-permeability drug: the effect of P-glycoprotein efflux on regional permeability of tacrolimus in rats. J Pharm Sci 91:719-729.
27. Tamura S, Tokunaga Y, Ibuki R, Amidon GL, Sezaki H, and Yamashita S (2003) The site-specific transport and metabolism of tacrolimus in rat small intestine. J Pharmacol Exp Ther 306:310-316.
28. Tanigawara Y, Okamura N, Hirai M, Yasuhara M, Ueda K, Kioka N, Komano T, and Hori R (1992) Transport of digoxin by human P-glycoprotein expressed in a porcine kidney epithelial cell line (LLC-PK1). J Pharmacol Exp Ther 263:840-845.
29. Toyobuku H, Tamai I, Ueno K, and Tsuji A (2003) Limited influence of P-glycoprotein on small-intestinal absorption of cilostazol, a high absorptive permeability drug. J Pharm Sci 92:2249-2259.
30. Tsuji A, Terasaki T, Takabatake Y, Tenda Y, Tamai I, Yamashima T, Moritani S, Tsuruo T, and Yamashita J (1992) P-glycoprotein as the drug efflux pump in primary cultured bovine brain capillary endothelial cells. Life Sci 51:1427-1437.
31. Ueda K, Okamura N, Hirai M, Tanigawara Y, Saeki T, Kioka N, Komano T, and Hori R (1992) Human P-glycoprotein transports cortisol, aldosterone and dexamethasone, but not progesterone. J Biol Chem 267:24248-24252.
32. Valenzuela B, Nacher A, Ruiz-Carretero P, Martin-Villodre A, Lopez-Carballo G, and Barettino D (2004) Profile of P-glycoprotein distribution in the rat and its possible influence on the salbutamol intestinal absorption process. J Pharm Sci 93:1641-1648.
33. Varma MV, Sateesh K, and Panchagnula R (2005) Functional role of P-glycoprotein in limiting intestinal absorption of drugs: contribution of passive permeability to P-glycoprotein mediated efflux transport. Mol Pharm 2:12-21.
34. Yamazaki M, Terasaki T, Yoshioka K, Nagata O, Kato H, Ito Y, and Tsuji A (1994a) Carrier-mediated transport of H1-antagonist at the blood-brain barrier: mepyramine uptake into bovine brain capillary endothelial cells in primary monolayer cultures. Pharm Res (NY) 11:975-978.
35. Yamazaki M, Terasaki T, Yoshioka K, Nagata O, Kato H, Ito Y, and Tsuji A (1994b) Carrier-mediated transport of H1-antagonist at the blood-brain barrier: a common transport system of H1-antagonists and lipophilic basic drugs. Pharm Res (NY) 11:1516-1518.
36. Yanai K, Okamura N, Tagawa M, Itoh M, and Watanabe T (1999) New findings in pharmacological effects induced by antihistamines: from PET studies to knock-out mice. Clin Exp Allergy 29(Suppl 3):29-36.
37. Yato N, Murata T, Saito N, Sakai A, Kikuchi M, Tsuzurahara K, and Narita H (1997) Anti-allergic activity of betotastine besilate (TAU-284), new anti-allergic drug. Folia Pharmacol Jpn 110:19-29.
38. Zimmermann C, Gutmann H, Hruz P, Gutzwiller JP, Beglinger C, and Drewe J (2005) Mapping of multidrug resistance gene 1 and multidrug resistance- associated protein isoform 1 to 5 mRNA expression along the human intestinal tract. Drug Metab Dispos 33:219-224.