Fundamental and clinical studies were carried out on sulbactam/cefoperazone (SBT/CPZ) in the field of pediatrics. The following results were obtained: 1. A total of 185 clinical isolates was employed to determine the minimum inhibitory concentrations (MICs) of SBT/CPZ against various bacterial species. SBT/CPZ showed strong antibacterial potency against E. coli, Salmonella, Klebsiella and P. mirabilis, and relatively strong potency against S. marcescens, P. aeruginosa and S. aureus. 2. Antibacterial potency of SBT/CPZ was stronger than that of CPZ alone against E. coli, and it also showed strong activity against strains of Salmonella, S. marcescens and S. aureus, moderately or highly resistant to CPZ. 3. SBT/CPZ was administered by intravenous bolus infusion to pediatric patients to determine the serum concentrations of SBT and CPZ. At a dose of 10 mg/kg the mean serum levels of SBT and CPZ were as follows; 17.8 μg/ml, 40.7 μg/ml at 15 minutes and 0.3 μg/ml, 3.0 μg/ml at 6 hours, respectively. The half-lives of SBT and CPZ in the serum were 1.05 hours and 1.76 hours, respectively. Similarly, at a dose of 20 mg/kg the mean serum levels of SBT and CPZ were: 31.9 μg/ml, 81.0 μg/ml at 15 minutes and 0.5 μg/ml, 6.1 μg/ml at 6 hours, and the half-lives were 1.00 hour and 1.72 hours, respectively. At a dose of 40 mg/kg, only 1 case was determined. The serum levels of SBT and CPZ were 34.4 μg/ml, 74.8 μg/ml at 30 minutes and 0.2 μg/ml, 3.7 μg/ml at 6 hours, and the half-lives were 0.78 hour and 1.38 hours, respectively. 4. SBT/CPZ was drip-infused intravenously over a period of 1 hour, and the serum concentrations of SBT and CPZ were determined. At a dose of 10 mg/kg or 20 mg/kg, the peak serum levels of SBT and CPZ were observed at 1 hour or at the end of the drip infusion. At a dose of 10 mg/kg the mean serum levels of SBT and CPZ were 14.4 μg/ml, 33.7 μg/ml at 1 hour and 1.4 μg/ml, 4.6 μg/ml at 7 hours, respectively. The half-lives were 1.86 hours for SBT and 2.23 hours for CPZ. Similarly, at a dose of 20 mg/kg, the mean serum levels of SBT and CPZ were 22.2 μg/ml, 34.6 μg/ml at 1 hour and 0.5 μg/ml, 2.8 μg/ml at 7 hours, and the half-lives were 1.17 hours and 1.75 hours. 5. The urinary recovery rats was determined for the 6 hour period after administration. The urinary recovery rates were approximately 30~60% for SBT and 10~20% for CPZ. 6. SBT/CPZ was administered to 11 cases with bacterial infections. A good or excellent clinical effect was seen in 10 cases (91%). 7. The bacteriological effect of SBT/CPZ was investigated in 7 strains of 4 cases. All strains were eradicated, a 100% bacteriological eradication rate. A total of 7 strains comprised 1 of E. coli, 1 of P. mirabilis, 1 of P. vulgaris, 1 of P. aeruginosa, 1 of H. influenzae and 2 of S. aureus. Each one of E. coli, P. vulgaris, H. influenzae and S. aureus was a β-lactamase producing organism. 8. The following side effects of the SBT/CPZ therapy were recorded: 2 cases of diarrhea, 1 case of eosinophilia and 1 case of prolongation of PT and APTT.
|Number of pages||15|
|Journal||Japanese Journal of Antibiotics|
|Publication status||Published - 1984|
ASJC Scopus subject areas
- Molecular Medicine