Abstract
The pharmacokinetic behaviour of two aminothiazolyl cephalosporins, ceftazidime (CAZ) and cefotaxime (CTX), were compared in three studies. Doses of each antibiotic were given intravenously (500 mg, n=4; 1 g, n=4) or intramuscularly (1 g, n=8) in a cross-over manner to healthy male volunteers. Antibiotic assays were performed by HPLC and microbiological assay techniques. Both antibiotics appeared to fit a two-compartment iv kinetic model with terminal half-lives of 1.7 h (CAZ) and 0.8 h (CTX). CAZ was metabolically stable whereas there was 34% conversion of CTX to desacetyl-CTX. The 24 h urinary recovery of CAZ averaged 89% but only 51% for CTX. The protein binding of CAZ was 17% and of CTX was 47%. CTX was more painful than CAZ on im injection in seven of the eight volunteers. CAZ therefore appeared to possess a number of features more favourable than those of CTX, when assessed in healthy volunteers.
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