Journal of Antimicrobial Chemotherapy, Vol 40, 263-268, Copyright © 1997 by The British Society for Antimicrobial Chemotherapy
E Memin, G Panteix and A Revol
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.
ORIGINAL ARTICLES
Carrier-mediated system for pefloxacin uptake in human monocytes
Centre Hospitalier Lyon Sud, Service de Biochimie, Pierre Benite, France.
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