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Antimicrob Agents Chemother. 1973 February; 3(2): 270-273
Copyright © 1973 American Society for Microbiology. All Rights Reserved.

Comparison of the Chemotherapeutic and Pharmacodynamic Activities of Cephradine, Cephalothin, and Cephaloridine in Mice

Gennaro J. Miraglia, Kathleen J. Renz and Hans H. Gadebusch

Squibb Institute for Medical Research, Princeton, New Jersey 08540

ABSTRACT

Cephradine, a new semisynthetic cephalosporin derivative, is 7[D(–)-2-amino-2-(1,4-cyclohexadien-1-yl) acetamido]-3-methyl-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid hydrate. The compound has a broad spectrum of antimicrobial activity in vitro. When given subcutaneously to mice, cephradine was appreciably more effective than cephalothin against infections induced by penicillinase-producing Staphylococcus, Escherichia coli, Klebsiella pneumoniae, or Enterobacter cloacae strains. Cephradine and cephaloridine possessed equivalent activity in treating infections caused by these same three gram-negative bacteria. The mean total bioactivity of cephradine in the serum of mice peaked within 30 min (59 µg/ml) after parenteral administration and was approximately threefold that of cephalothin (20 µg/ml), but less than that of cephaloridine (83 µg/ml). Nearly all of the administered cephradine (84%) and cephaloridine (70%) were excreted in the urine as the parent compounds. In contrast, only 47% (total bioactivity) of administered cephalothin was recovered, an amount that represented only 15 to 20% of the parent substance.

Antimicrob Agents Chemother. 1973 February; 3(2): 270-273
Copyright © 1973 American Society for Microbiology. All Rights Reserved.





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