JPET Assistant Professor of Medicine (Clinician-Educator)

Home Help [Feedback] [For Subscribers] [Archive] [Search] [Contents]
QUICK SEARCH:   [advanced]


     

This Article
Right arrow Full Text
Right arrow Full Text (PDF)
Right arrow Submit a response
Right arrow Alert me when this article is cited
Right arrow Alert me when eLetters are posted
Right arrow Alert me if a correction is posted
Right arrow Citation Map
Services
Right arrow Similar articles in this journal
Right arrow Similar articles in PubMed
Right arrow Alert me to new issues of the journal
Right arrow Download to citation manager
Citing Articles
Right arrow Citing Articles via HighWire
Right arrow Citing Articles via Google Scholar
Google Scholar
Right arrow Articles by Ito, T.
Right arrow Articles by Inui, K.-I.
Right arrow Search for Related Content
PubMed
Right arrow PubMed Citation
Right arrow Articles by Ito, T.
Right arrow Articles by Inui, K.-I.

Vol. 282, Issue 2, 955-960, 1997

Transport of Quinolone Antibacterial Drugs by Human P-Glycoprotein Expressed in a Kidney Epithelial Cell Line, LLC-PK11

Tatsuya Ito, Ikuko Yano, Kumiko Tanaka and Ken-Ichi Inui

Department of Pharmacy, Kyoto University Hospital, Faculty of Medicine, Kyoto University, Sakyo-ku, Kyoto 606-01, Japan

The purpose of this study was to characterize the transport mechanisms involved in the renal tubular secretion of quinolones. The contribution of P-glycoprotein to the transport of quinolones was elucidated using a kidney epithelial cell line, LLC-PK1, and its transfectant derivative cell line, LLC-GA5-COL150, which expresses human P-glycoprotein on the apical membrane. The transcellular transport of levofloxacin, a quinolone antibacterial drug, from the basolateral to apical side was increased in LLC-GA5-COL150 compared with that in LLC-PK1 monolayers. The apparent Michaelis constant and maximum velocity values for the saturable transcellular transport of levofloxacin from the basolateral to apical side in LLC-GA5-COL 150 monolayers were 3.0 mM and 45 nmol/mg protein per 15 min, respectively. The increased basolateral-to-apical transport in LLC-GA5-COL150 monolayers was completely inhibited by cyclosporin A and quinidine to the level observed in LLC-PK1 monolayers. In addition, 3 mM levofloxacin inhibited the basolateral-to-apical transport of daunorubicin in LLC-GA5-COL150 monolayers. The basolateral-to-apical transport of another quinolone antibacterial drug, DU-6859a, in LLC-GA5-COL150 monolayers greatly exceeded than that in LLC-PK1 monolayers, and was inhibited by levofloxacin. These findings suggest that quinolone antibacterial drugs are transported by P-glycoprotein, and that P-glycoprotein may contribute at least in part to the renal tubular secretion of quinolones.

Copyright © by The American Society for Pharmacology and Experimental Therapeutics


This article has been cited by other articles:


Home page
 J Clin PharmacolHome page
S. Liu, P. M. Beringer, L. Hidayat, A. P. Rao, S. Louie, G. J. Burckart, and B. Shapiro
Probenecid, but Not Cystic Fibrosis, Alters the Total and Renal Clearance of Fexofenadine
J. Clin. Pharmacol., August 1, 2008; 48(8): 957 - 965.
[Abstract] [Full Text] [PDF]

Home page
 J Clin PharmacolHome page
R. Borrows, G. Chusney, M. Loucaidou, A. James, S. Goel, S. Borrows, J. Van Tromp, T. Cairns, M. Griffith, N. Hakim, et al.
Analysis of Factors Influencing Tacrolimus Levels and Immunoassay Bias in Renal Transplantation
J. Clin. Pharmacol., August 1, 2007; 47(8): 1035 - 1042.
[Full Text] [PDF]

Home page
 ChestHome page
C. K. K. Lee, M. P. Boyle, M. Diener-West, L. Brass-Ernst, M. Noschese, and P. L. Zeitlin
Levofloxacin Pharmacokinetics in Adult Cystic Fibrosis
Chest, March 1, 2007; 131(3): 796 - 802.
[Abstract] [Full Text] [PDF]

Home page
 Nephrol Dial TransplantHome page
A. Korzets, U. Gafter, D. Dicker, M. Herman, and Y. Ori
Levofloxacin and rhabdomyolysis in a renal transplant patient
Nephrol. Dial. Transplant., November 1, 2006; 21(11): 3304 - 3305.
[Full Text] [PDF]

Home page
 J. Pharmacol. Exp. Ther.Home page
H. Sasabe, Y. Kato, T. Suzuki, M. Itose, G. Miyamoto, and Y. Sugiyama
Differential Involvement of Multidrug Resistance-Associated Protein 1 and P-Glycoprotein in Tissue Distribution and Excretion of Grepafloxacin in Mice
J. Pharmacol. Exp. Ther., August 1, 2004; 310(2): 648 - 655.
[Abstract] [Full Text] [PDF]

Home page
 J Antimicrob ChemotherHome page
F. Van Bambeke, J.-M. Michot, and P. M. Tulkens
Antibiotic efflux pumps in eukaryotic cells: occurrence and impact on antibiotic cellular pharmacokinetics, pharmacodynamics and toxicodynamics
J. Antimicrob. Chemother., May 1, 2003; 51(5): 1067 - 1077.
[Full Text] [PDF]

Home page
 J Clin PharmacolHome page
A. W. Wallace, J. M. Victory, and G. W. Amsden
Lack of Bioequivalence When Levofloxacin and Calcium-Fortified Orange Juice Are Coadministered to Healthy Volunteers
J. Clin. Pharmacol., May 1, 2003; 43(5): 539 - 544.
[Abstract] [Full Text] [PDF]

Home page
 J Clin PharmacolHome page
A. W. Wallace, J. M. Victory, and G. W. Amsden
Lack of Bioequivalence of Gatifloxacin When Coadministered with Calcium-Fortified Orange Juice in Healthy Volunteers
J. Clin. Pharmacol., January 1, 2003; 43(1): 92 - 96.
[Abstract] [Full Text]

Home page
 J. Pharmacol. Exp. Ther.Home page
A. Fukada, H. Saito, and K.-i. Inui
Transport Mechanisms of Nicotine across the Human Intestinal Epithelial Cell Line Caco-2
J. Pharmacol. Exp. Ther., August 1, 2002; 302(2): 532 - 538.
[Abstract] [Full Text] [PDF]

Home page
 J. Pharmacol. Exp. Ther.Home page
H. Yamaguchi, I. Yano, H. Saito, and K.-i. Inui
Pharmacokinetic Role of P-Glycoprotein in Oral Bioavailability and Intestinal Secretion of Grepafloxacin in Vivo
J. Pharmacol. Exp. Ther., March 1, 2002; 300(3): 1063 - 1069.
[Abstract] [Full Text] [PDF]

Home page
 Antimicrob. Agents Chemother.Home page
K. Naruhashi, I. Tamai, N. Inoue, H. Muraoka, Y. Sai, N. Suzuki, and A. Tsuji
Involvement of Multidrug Resistance-Associated Protein 2 in Intestinal Secretion of Grepafloxacin in Rats
Antimicrob. Agents Chemother., February 1, 2002; 46(2): 344 - 349.
[Abstract] [Full Text] [PDF]

Home page
 J. Pharmacol. Exp. Ther.Home page
H. Yamaguchi, I. Yano, Y. Hashimoto, and K.-I. Inui
Secretory Mechanisms of Grepafloxacin and Levofloxacin in the Human Intestinal Cell Line Caco-2
J. Pharmacol. Exp. Ther., October 1, 2000; 295(1): 360 - 366.
[Abstract] [Full Text]

Home page
 CirculationHome page
D. R. Abernethy and D. A. Flockhart
Molecular Basis of Cardiovascular Drug Metabolism : Implications for Predicting Clinically Important Drug Interactions
Circulation, April 11, 2000; 101(14): 1749 - 1753.
[Full Text] [PDF]

Home page
 Am. J. Physiol. Gastrointest. Liver Physiol.Home page
H. Mizuuchi, T. Katsura, K. Ashida, Y. Hashimoto, and K.-I. Inui
Diphenhydramine transport by pH-dependent tertiary amine transport system in Caco-2 cells
Am J Physiol Gastrointest Liver Physiol, April 1, 2000; 278(4): G563 - G569.
[Abstract] [Full Text] [PDF]

Home page
 Antimicrob. Agents Chemother.Home page
A. Delon, S. Bouquet, F. Huguet, V. Brunet, P. Courtois, and W. Couet
Pharmacokinetic-Pharmacodynamic Contributions to the Convulsant Activity of Fluoroquinolones in Rats
Antimicrob. Agents Chemother., June 1, 1999; 43(6): 1511 - 1515.
[Abstract] [Full Text]

Home page
 J. Pharmacol. Exp. Ther.Home page
Y. Matsuo, I. Yano, T. Ito, Y. Hashimoto, and K.-I. Inui
Transport of Quinolone Antibacterial Drugs in a Kidney Epithelial Cell Line, LLC-PK1
J. Pharmacol. Exp. Ther., November 1, 1998; 287(2): 672 - 678.
[Abstract] [Full Text]

Home page
 Antimicrob. Agents Chemother.Home page
C. Østergaard, T. Klitmøller Sørensen, J. Dahl Knudsen, and N. Frimodt-Møller
Evaluation of Moxifloxacin, a New 8-Methoxyquinolone, for Treatment of Meningitis Caused by a PenicillinResistant Pneumococcus in Rabbits
Antimicrob. Agents Chemother., July 1, 1998; 42(7): 1706 - 1712.
[Abstract] [Full Text]


Home Help [Feedback] [For Subscribers] [Archive] [Search] [Contents]
All ASPET Journals Molecular Pharmacology Pharmacological Reviews
Molecular Interventions Drug Metabolism and Disposition

Copyright © 1997 by the American Society for Pharmacology and Experimental Therapeutics.