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Antimicrob Agents Chemother. 1976 August; 10(2): 307-317
Copyright © 1976 American Society for Microbiology. All Rights Reserved.

Comparative Pharmacokinetics and Metabolism of Cephapirin in Laboratory Animals and Humans

^a Research Division, Bristol Laboratories, Syracuse, New York 13201

ABSTRACT

Comparative drug disposition studies in mice, rats, dogs, and humans indicate that cephapirin, a new semisynthetic cephalosporin antibiotic that exhibits broad-spectrum antimicrobial activity, is metabolized to desacetylcephapirin in these species. Pharmacokinetic analyses of the concentrations of cephapirin and desacetylcephapirin in plasma and urine reveal that the rate and extent of deacetylation decreases from rodents to dogs to humans. The kinetic analyses also suggest that the kidney performs a role not only in the excretion but also in the metabolism of cephapirin to desacetylcephapirin.

¹ Present address: Division of Biopharmaceutics, Bureau of Drugs, Food and Drug Administration, Rockville, MD 20852.