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Journal of Antimicrobial Chemotherapy, Vol 40, 263-268, Copyright © 1997 by The British Society for Antimicrobial Chemotherapy


ORIGINAL ARTICLES

Carrier-mediated system for pefloxacin uptake in human monocytes

E Memin, G Panteix and A Revol
Centre Hospitalier Lyon Sud, Service de Biochimie, Pierre Benite, France.

Protein transporters present in cellular membranes can influence the intracellular concentration of a variety of drugs. Pefloxacin is a fluoroquinolone which is commonly used in systemic infections. Its transport mechanisms have never been described. In the present study, we demonstrated that pefloxacin uptake is carrier-mediated. Pefloxacin crosses the membrane in zwitterionic form. The transport seems to differ from that of other fluoroquinolones which use amino acid or organic anion transporters. Pefloxacin uptake is not influenced by the presence of hexose in the incubation medium. It does not use a nucleoside transport system to penetrate the cells but adenosine increases the uptake. The carrier is inhibited by verapamil at 60 min and is activated by a Ca2+-dependent system.
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