FUNDAMENTAL AND CLINICAL STUDIES ON CEFOPERAZONE IN PEDIATRICS

WITH SPECIAL REFERENCE TO RENAL TOXICITY

Abstract

Fundamental, clinical studies on cefoperazone (CPZ), a new synthetic antibiotic of cephalosporins was conducted to obtain results as follows.
1. This preparation, 11.4-50mg/kg was administered to 11 cases of children by intravenous drip infusion for 30minutes, and serum levels were studied. The highest serum level at the completion of infusion was 40.0-138.0mcg/ml. A dose response was observed. The half-life in serum averaged 1.55 hours except 2.4 hours observed with 1 case of liver dysfunction.
2. When the urinary excretion during 30 minutes drip infusion was examined, the urinary recovery rate at 0-6 hours in 2 cases of children averaged 17.2% and was low at 5.3% in 1 case of membranoproliferative glomerulonephritis.
3. In terms of the clinical effect on bacterial infections in pediatric field, CPZ proved effective in all of the 21 cases in which it was used alone. And it showed an excellent antibacterial activity against all the bacteria isolated from cases used as the subjects.
4. When side effects were studied, diarrhea and slight impairment of the liver were observed, but all were transient.
5. As a result of a study on the renal toxicity of CPZ, CPZ was deemed as being a drug which hardly causes disturbance of renal tubules judging from the aspect of the β-D-N-acetylglucosaminidase activity in urine and variations in the urine β₂2-microglobulin levels.