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Transport of cephalosporin antibiotics in rat renal basolateral membranes

Abstract— Transport mechanisms of cephalosporin antibiotics in rat renal basolateral membranes have been studied in isolated membrane vesicles. Uptake of [14C]p‐aminohippurate, a typical organic anion, by basolateral membrane vesicles was enhanced when membrane vesicles were preloaded with unlabelled p‐aminohippur‐ate (counter‐transport). Cephalosporins such as cephradine, cephalexin, and cefazolin inhibited the counter‐transport of [14C]p‐aminohippurate, as did unlabelled p‐aminohippurate and probenecid. In contrast, cephalexin did not affect the uptake of [3H]tetraeth‐ylammonium, an organic cation, by basolateral membrane vesicles. These results suggest that most cephalosporins are transported via organic anion transport systems in rat renal basolateral membranes.