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[Laboratory and clinical studies of cefoperazone in children (author's transl)]
Insights
Cefoperazone (CPZ) shows promising pediatric efficacy against common bacteria like S. aureus and E. coli, with favorable serum concentrations and a high clinical response rate in infections. Studies indicate CPZ is well-tolerated in infants, with no observed clinical side effects.
Area of Science:
- Pediatric infectious diseases
- Pharmacokinetics and pharmacodynamics of antibiotics
- Clinical microbiology
Background:
- Evaluation of cefoperazone (CPZ), a novel synthetic cephalosporin, in pediatric applications.
- Comparison of CPZ's Minimum Inhibitory Concentrations (MICs) against clinically isolated bacteria (S. aureus, E. coli, K. pneumoniae, H. influenzae) with existing antibiotics (CEZ, ABPC).
- Assessment of CPZ's pharmacokinetic profile and clinical effectiveness in pediatric patients.
Observation:
- CPZ demonstrated potent activity against most tested strains, with MICs below 6.25 mcg/ml for 88-100% of S. aureus, E. coli, K. pneumoniae, and H. influenzae isolates.
- Pharmacokinetic studies in infants showed a serum half-life of 1.29 hours and a urinary recovery rate of 14.5% after intravenous administration.
- Clinical trials in pediatric patients with pneumonia, bronchitis, and urinary tract infections reported effective to markedly effective responses.
Findings:
- CPZ exhibited superior or comparable MICs against E. coli, K. pneumoniae, and H. influenzae compared to CEZ and ABPC, and was superior to ABPC against S. aureus.
- Bacteriological eradication was observed for multiple pathogens, including S. pneumoniae, S. faecalis, H. influenzae, E. coli, and K. pneumoniae.
- No significant clinical side effects were noted, with minor laboratory abnormalities (elevated GOT, eosinophilia) resolving post-therapy.
Implications:
- Cefoperazone (CPZ) presents a viable therapeutic option for treating various pediatric bacterial infections.
- The favorable pharmacokinetic profile and high clinical efficacy support CPZ's use in pediatric populations.
- Further research may explore CPZ's role in combating antibiotic-resistant strains and its long-term safety in children.
Abstract:
Experimental and clinical studies on cefoperazone (CPZ), a new synthetic cephalosporin, were performed in the field of pediatrics. 1) The MICs of CPZ against 26 strains of S. aureus, 21 strains of E. coli, 20 strains of K. pneumoniae and 15 strains of H. influenzae which were clinically isolated were estimated and compared with those of CEZ and ABPC. Some strains were found to be high in the MIC of CPZ against S. aureus, E. coli and K. pneumoniae by original inoculation but 88% of S. aureus, 95% of E. coli, 95% of K. pneumoniae and 100% of H. influenzae were under 6.25 mcg/ml by 100 times dilution inoculation. The MIC of CPZ against S. aureus was inferior to CEZ and superior to ABPC, and that against E. coli, K. pneumoniae and H. influenzae was superior to CEZ and ABPC. 2) The serum concentration, urinary concentration and recovery rate from urine were measured in two healthy infants and one infant in the stage of convalescence from cholangiohepatitis after a single intravenous administration of 25 mg/kg of CPZ. The mean serum concentration in the two healthy infants was 88.0 mcg/ml at 30 minutes, 63.0 at 1 hour, 31.4 at 2 hours, 12.2 at 4 hours and 4.2 at 6 hours; the half-life was 1.29 hours, and the recovery rate from urine was 14.5%. 3) The clinical effect of CPZ was examined in 16 cases of acute lobar pneumonia or acute bronchopneumonia, 1 case of acute bronchitis and 4 cases of acute urinary tract infections. All of the cases responded effectively or markedly effectively. Among the causative bacteria in those cases, 2 strains of S. pneumoniae, 1 strain of S. faecalis, 1 strain of H. influenzae and 2 strains of E. coli and 1 strain of K. pneumoniae disappeared following the administration of CPZ. The bacteriological effect against 1 strain of P. aeruginosa was unknown, but clinical effectiveness was observed in this case. No clinical side effects were observed. Laboratory examination carried out before and after the administration revealed a rise of GOT and eosinophilia in each one case, but in both abnormality returned to normal after termination of therapy.