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Cotransport of Macrolide and Fluoroquinolones, a Beneficial Interaction Reversing P-glycoprotein Efflux

Cotransport of Macrolide and Fluoroquinolones, a Beneficial Interaction Reversing P-glycoprotein... American Journal of Therapeutics 11, 433–442 (2004) Cotransport of Macrolide and Fluoroquinolones, a Beneficial Interaction Reversing P-glycoprotein Efflux Vineet Sikri, Dhananjay Pal, Ritesh Jain, Durga Kalyani, and Ashim K. Mitra* The purpose of this study was to determine the interactions of erythromycin and various fluoro- quinolones with P-glycoprotein (P-gp) and in turn assess their effects on transport kinetics across a model cell monolayer. MDCKII-MDRI cells were selected as a model monolayer to evaluate the effects of various fluoroquinolones, ie, norfloxacin, lomefloxacin, ofloxacin, enoxacin, grepafloxacin, 3 14 levofloxacin, and sparfloxacin on the P-gp–mediated efflux of H-cyclosporine (CsA) and C- erythromycin. IC values associated with grepafloxacin-, levofloxacin-, and sparfloxacin-mediated inhibition of P-gp were calculated across Caco-2 cells with erythromycin as the model P-gp sub- strate. Transport of erythromycin was then studied with P-gp saturable concentrations of fluoro- quinolones. Western blot analysis was performed on Caco-2 cells to confirm P-gp expression. Only grepafloxacin elevated the uptake of H-CsA across the MDCKII-MDRI cell monolayer, whereas norfloxacin, lomefloxacin, ofloxacin, and enoxacin did not exert any effect on H-CsA uptake. Inhibition studies indicate that grepafloxacin, levofloxacin, and sparfloxacin are potent inhibitors of P-gp–mediated efflux of C-erythromycin in the MDCKII-MDRI cell monolayer. Similar studies were conducted http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png American Journal of Therapeutics Wolters Kluwer Health

Cotransport of Macrolide and Fluoroquinolones, a Beneficial Interaction Reversing P-glycoprotein Efflux

Mitra, Ashim K
American Journal of Therapeutics , Volume 11 (6) – Nov 1, 2004
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References (33)

ISSN
1075-2765
eISSN
1536-3686
DOI
10.1097/01.mjt.0000132643.69143.64
Publisher site
See Article on Publisher Site

Abstract

American Journal of Therapeutics 11, 433–442 (2004) Cotransport of Macrolide and Fluoroquinolones, a Beneficial Interaction Reversing P-glycoprotein Efflux Vineet Sikri, Dhananjay Pal, Ritesh Jain, Durga Kalyani, and Ashim K. Mitra* The purpose of this study was to determine the interactions of erythromycin and various fluoro- quinolones with P-glycoprotein (P-gp) and in turn assess their effects on transport kinetics across a model cell monolayer. MDCKII-MDRI cells were selected as a model monolayer to evaluate the effects of various fluoroquinolones, ie, norfloxacin, lomefloxacin, ofloxacin, enoxacin, grepafloxacin, 3 14 levofloxacin, and sparfloxacin on the P-gp–mediated efflux of H-cyclosporine (CsA) and C- erythromycin. IC values associated with grepafloxacin-, levofloxacin-, and sparfloxacin-mediated inhibition of P-gp were calculated across Caco-2 cells with erythromycin as the model P-gp sub- strate. Transport of erythromycin was then studied with P-gp saturable concentrations of fluoro- quinolones. Western blot analysis was performed on Caco-2 cells to confirm P-gp expression. Only grepafloxacin elevated the uptake of H-CsA across the MDCKII-MDRI cell monolayer, whereas norfloxacin, lomefloxacin, ofloxacin, and enoxacin did not exert any effect on H-CsA uptake. Inhibition studies indicate that grepafloxacin, levofloxacin, and sparfloxacin are potent inhibitors of P-gp–mediated efflux of C-erythromycin in the MDCKII-MDRI cell monolayer. Similar studies were conducted

Journal

American Journal of Therapeutics – Wolters Kluwer Health

Published: Nov 1, 2004

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