PHARMACOKINETICS OF CEFOPERAZONE CONCENTRATION IN HUMAN LUNG TISSUE

Abstract

A well-controlled comparative study was conducted in order to evaluate the efficacy, safety and usefulness of the monobactam antibiotic aztreonam (AZT) in complicated urinary tract infections (UTI) using cefoperazone (CPZ) as the control drug.
1. Patients with complicated UTI due to Gram-negative bacteria were examined. However, in polymicrobial infections, the cases caused by Gram-negative and Gram-positive bacteria were also examined. Both drugs were administered 1 g, twice a day by intravenous drip infusion for 5 days. Overall clinical efficacy was evaluated by the criteria proposed by the UTI committee in Japan.
2. Of the total 394 cases, the clinical efficacy was evaluated for 152 cases in the AZT group and 143 cases in the CPZ group excluding 99 cases of exclusion or dropout. There was no statistically significant difference in the back ground characteristics between the 2 groups. The overall clinical efficacy rate was 55.3% for AZT and 55.2% for CPZ with difference not significant.
As for clinical efficacy, in the monomicrobial infection after postprostatectomy (G-2), AZT was superior to CPZ (P<0.05), whereas in the polymicrobial infection without indwelling catheter (G-6), CPZ was superior to AZT (P<0.1).
3. The overall bacteriological eradication rate was 77.2% for AZT and 74.5% for CPZ. For Gram-negative bacteria only the eradication rate for AZT (83.2%) was superior to that for CPZ (74.6%). This was probably due to the stability of AZT to β-lactamase.
4. Side effects were observed in 3 cases out of 201 in the AZT group and 5 cases out of 189 in the CPZ group. No severe abnormal laboratory finding was observed in any group; there was no significant difference between the 2 groups.
Consequently, AZT was judged to be an antibiotic with clinical usefulness equal to, or even superior to that of CPZ.