Abstract
Intraperitoneally administered cephalothin-14C is rapidly metabolized and excreted in the rat with about 70% of a radioactive dose appearing in urine in 4 hours. The major metabolite is desacetylcephalothin which forms by hydrolysis of the ester group. Some in vivo side chain hydrolysis at position 7 also occurs as indicated by the excretion of thienylacetylglycine, a metabolite of thiophene acetic acid. A long-lived minor metabolite occurs in blood and appears to be an albumin-cephalothin complex. A similar complex forms from cephaloglycin, 7-phenylacetamidocephalosporanic acid and 6-thienylacetamidopenicillanic acid but not from desacetylcephalothin, cephalexin, penicillin G or penicillin V. The complex was formed in vitro by incubation of radiocephalothin with rat serum.
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