The pharmacokinetic and bactericidal characteristics of oral cefixime

Abstract

The pharmacokinetics of cefixime (FK 027), a broad-spectrum cephalosporin, were assessed in 12 normal subjects after single oral doses of 50, 100, 200, and 400 mg. Mean peak serum concentrations were 1.02, 1.46, 2.63, and 3.85 micrograms/ml after the four respective doses. Respective mean serum levels at 12 hours were 0.16, 0.33, 0.72, and 1.13 micrograms/ml. Volumes of distribution averaged 0.1 L/kg body weight, and the elimination t1/2 was 3 hours for all doses. The AUC was 7.01, 11.4, 22.5, and 36.4 micrograms X hr/ml for the four doses, respectively. Serum clearance averaged 0.4 mg/min/kg and mean 24-hour urinary recovery was 21%, 19%, 20%, and 16% for the four respective doses. Serum bactericidal titers at 4 hours exceeded 1:16 for Streptococcus pneumoniae, S. pyogenes, Hemophilus influenzae, and Branhamella catarrhalis. Urine bactericidal titers exceeded 1:8 for Escherichia coli, Klebsiella pneumoniae, and Enterobacter cloacae resistant to the available oral cephalosporins.