Cefuroxime: pharmacokinetics after a short infusion, and in vitro activity against hospital pathogens

Abstract

Cefuroxime is a new cephalosporin antibiotic stable to most of the β-lactamases produced by Gram-negative bacteria. The pharmacokinetics of cefuroxime have been investigated after 30-min intravenous infusions of 500 mg and 750 mg and its antibacterial activity has been compared with that of cephalothin against 104 strains of recent clinical isolates. Serum concentrations were found to be proportional to the dose: reaching 37.8 and 51.1 μg/ml after 500 and 750 mg infusions, respectively. The serum half-life was about 120 min and the apparent total volume of distribution about 191. The renal clearance rate of cefuroxime was 1.5 greater than that of creatinine. On average, 96% of the dose was excreted in the urine during the first 24 h, and it was estimated that 52% was excreted through the tubules. Urine concentrations were high. Cefuroxime was more active than cephalothin against most species of Gram-negative organisms: for 50 strains of Escherichia coli the geometric mean of the MICs was 6.4 μg/ml with cefuroxime but 12.5 μg/ml with cephalothin. Thus cefuroxime is a useful antibiotic, especially against organisms that are resistant to other cephalosporins probably because cefuroxime is not destroyed by most bacterial β-lactamase enzymes.