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[Fundamental and clinical studies on cefoperazone in pediatrics, with special reference to renal toxicity]
Insights
Cefoperazone (CPZ) is an effective antibiotic for pediatric bacterial infections, showing good serum levels and minimal renal toxicity. Side effects like transient diarrhea and liver impairment were noted.
Area of Science:
- Pharmacology
- Microbiology
- Pediatrics
Context:
- Cefoperazone (CPZ) is a novel synthetic cephalosporin antibiotic.
- Pediatric bacterial infections require effective and safe therapeutic options.
Purpose:
- To evaluate the pharmacokinetic profile, clinical efficacy, and safety of cefoperazone in pediatric patients.
- To assess the antibacterial activity and potential renal toxicity of CPZ.
Summary:
- Pharmacokinetic studies in children showed dose-dependent serum levels (40.0-138.0 mcg/ml) with an average half-life of 1.55 hours.
- CPZ demonstrated high efficacy in 21 pediatric cases of bacterial infections and potent antibacterial activity against isolated pathogens.
- Transient side effects included diarrhea and mild liver function impairment; renal toxicity was minimal, with no significant disturbance of renal tubules indicated by urinary enzyme levels.
Impact:
- Cefoperazone is a promising antibiotic for treating pediatric bacterial infections with a favorable safety profile.
- The study provides valuable data on CPZ's pharmacokinetics and clinical utility in a pediatric population.
- Findings support CPZ's use, highlighting its effectiveness and low risk of renal adverse effects.
Abstract:
Fundamental, clinical studies on cefoperazone (CPZ), a new synthetic antibiotic of cephalosporins was conducted to obtain results as follows. This preparation, 11.4-50 mg/kg was administered to 11 cases of children by intravenous drip infusion for 30 minutes, and serum levels were studied. The highest serum level at the completion of infusion was 40.0-138.0 mcg/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. 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. 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. When side effects were studied, diarrhea and slight impairment of the liver were observed, but all were transient. 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 beta-D-N-acetylglucosaminidase activity in urine and variations in the urine beta 2-microglobulin levels.