Pharmacokinetic Study of Cefazaflur Compared to Cephalothin and Cefazolin

Abstract

A single 1-g dose of cefazaflur, a new semisynthetic cephalosporin derivative, was compared in a crossover study to the same dose of cephalothin and cefazolin by i.m. injection in 7 healthy volunteers. Serum concentrations were measured at several time intervals during 6 h following each administration. The mean peak serum levels obtained after 30 min were 25.2, 17.2 and 62.3 .mu.g/ml, respectively, for cefazaflur, cephalothin and cefazolin. In each of the 7 subjects, serum concentrations were higher at each sampling time with cefazolin than with the other 2 cephalosporins. The percentage of total administered dose recovered in urine in a microbiologically active form for the 0-24-h collection was, respectively, 92.7, 59.2 and 94.9% with cefazaflur, cephalothin and cefazolin, the largest part being excreted during the first 6 h. Neither drug appeared to have any pronounced effect on various laboratory tests. Local reactions at the site of i.m. injection were minor with cefazaflur and cefazolin, but were more pronounced with cephalothin.