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[Overall clinical evaluation of cefprozil against infections in pediatric fields. Pediatric Study Group for
1Research Institute of Chemotherapy for Mother and Child, Teikyo University.
Insights
Cefprozil (CFPZ) demonstrates dose-dependent serum concentrations and urinary excretion in pediatric patients. This antibiotic shows high clinical efficacy rates in treating various pediatric infections, with excellent bacteriological eradication for Gram-positive organisms.
Area of Science:
- Pharmacology
- Pediatric Infectious Diseases
- Antibiotic Therapy
Background:
- Cefprozil (CFPZ) is a cephalosporin antibiotic used for treating bacterial infections.
- Understanding its pharmacokinetic and clinical profile in pediatric populations is crucial for effective treatment.
- Granule preparations offer a suitable dosage form for pediatric administration.
Purpose of the Study:
- To evaluate the pharmacokinetic properties of Cefprozil (CFPZ) granules in pediatric patients.
- To assess the bacteriological and clinical efficacy of CFPZ in treating various pediatric infections.
- To investigate the influence of food intake on CFPZ pharmacokinetics.
Main Methods:
- Pediatric patients received single oral doses of CFPZ granules at 4.0, 7.5, and 15.0 mg/kg.
- Serum concentrations, urinary excretion, Cmax, AUC, and T1/2 (beta) were measured.
- Clinical efficacy was assessed in 804 cases, with bacteriological eradication rates also determined.
Main Results:
- Cefprozil (CFPZ) exhibited dose-dependent Cmax and AUC, with stable T1/2 (beta) across doses (0.94-1.03 hours).
- Food intake caused a slight delay in Tmax and a minor decrease in Cmax, but did not significantly alter AUC or T1/2.
- High clinical efficacy rates (96.0-97.2%) were observed across various infection types, with a 97.2% efficacy in cases with isolated bacteria. Bacteriological eradication rates were 83.3% overall, with higher rates for Gram-positive (95.8%) than Gram-negative organisms (64.2%).
Conclusions:
- Cefprozil (CFPZ) demonstrates favorable pharmacokinetics and high clinical efficacy in pediatric patients with various infections.
- The granule formulation is suitable for pediatric use, with minimal impact of food on its absorption.
- CFPZ is effective against common pediatric pathogens, including Haemophilus influenzae, with good bacteriological eradication rates, particularly for Gram-positive bacteria.
Abstract:
Cefprozil (CFPZ, BMY-28100) granule preparation was studied for pharmacokinetic, bacteriological and clinical aspects in the pediatric infections. The results obtained are summarized as follows: 1. Serum concentrations and urinary excretion. The pharmacokinetics of CFPZ in pediatrics was investigated by single oral administration of fine granules at doses of 4.0, 7.5 and 15.0 mg/kg. Peak blood levels of CFPZ were 3.06, 4.62 and 9.65 micrograms/ml, respectively, at 1.00-1.30 hours after each dose and AUCs were 7.44, 12.50 and 27.01 micrograms.hr/ml, respectively. These data showed that Cmax and AUC depended on dose levels. T 1/2 (beta) at these dose levels were 1.03, 0.94 and 1.01 hours, respectively. There were no differences related to dose. Urinary recovery rates in the first 6 hours after administration were 51.5-57.1%. The pharmacokinetics of CFPZ before or after meals were also investigated at a dose of 7.5 mg/kg. Peak blood levels were 4.88 micrograms/ml at 1.17 hours after administration in the fasting state, and 4.30 micrograms/ml at 1.54 hours after administration in the non-fasting state. Delay of Tmax and slight decrease of Cmax were observed in the non-fasting state, but T 1/2 and AUC were 0.91 hour and 12.96 micrograms.hr/ml, respectively, in the non-fasting state, and were similar to those in the fasting state, 0.93 hour and 12.82 micrograms.hr/ml, respectively. Urinary recovery rates in the first 6 hours after administration were 63.8% in the fasting state and 50.7% in the non-fasting state. 2. Clinical results. Clinical efficacies of CFPZ granules in various infectious diseases were studied in 804 cases. Twenty nine cases, mostly viral or mycoplasmal infections, were excluded from the statistical analysis. The clinical efficacy rate in 527 cases with causative bacteria isolated was 97.2%; and in 248 cases from whom no significant isolate had been obtained was 96.0%. The clinical efficacy rate in 475 cases with monobacterial infections (proven by culture of isolates) was 97.3%, and that in 52 case with polybacterial infections was 96.2%. Haemophilus influenzae was isolated mostly from acute respiratory infections. In 88 cases from whom H. influenzae was isolated, clinical efficacy rate was 95.5%. In cases from whom H. influenzae was found concomitant by with Staphylococcus aureus, Streptococcus pyogenes or Streptococcus pneumoniae, the clinical efficacy rates were also high. The bacteriological eradication rate in cases with 582 strains was 83.3%; the eradication rate for Gram-positive organisms was 95.8%; and for Gram-negative organisms, it was 64.2%.(ABSTRACT TRUNCATED AT 400 WORDS)