Elsevier

Biochemical Pharmacology

Volume 32, Issue 4, 15 February 1983, Pages 621-626
Biochemical Pharmacology

Carrier-mediated transport of amino-cephalosporins by brush border membrane vesicles isolated from rat kidney cortex

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Abstract

The uptake of cephalosporin antibiotics by brush border membrane vesicles isolated from rat renal cortex has been studied by a rapid filtration technique, demonstrating a carrier-mediated transport system for amino-cephalosporins such as cephalexin and cephradine. The antibiotics were taken up into an osmotically reactive intravesicular space. The uptake of cephalexin was saturable (apparent Km 2.2 mM), was inhibited by structural analogues and sulfhydryl reagents, and was stimulated by the countertransport effect, although the Na+ gradient did not affect the uptake. This transport system was essentially different from the transport system for p-aminohippurate in brush border membranes. The uptake properties for cephradine in brush border membrane vesicles appeared to be similar to those for cephalexin. The present results suggest the existence of a carrier-mediated transport system for amino-cephalosporins in brush border membranes. This system may be a part of the mechanism of tubular reabsorption of these antibiotics.

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    The mechanism(s) underlying tubular injury include the ability of beta-lactams to actively accumulate in renal proximal tubular cells, acylate proteins [238], and/or induce lipid peroxidation (for cephaloridine) [239–241]. The side group substitutions of beta-lactams greatly affect transport rates and protein reactivity and hence contribute to the varying degrees of nephrotoxicity [242,243]. Very few cephalosporins cause tubular damage at therapeutic doses.

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