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[Experimental and clinical evaluation of cefotetan in pediatrics]
Insights
Cefotetan (CTT) demonstrates broad-spectrum antibacterial activity against common pathogens like E. coli and S. aureus. Clinical trials show CTT is effective in treating bacterial infections with a high response rate and minimal side effects.
Area of Science:
- Pharmacology
- Microbiology
- Clinical Medicine
Background:
- Cefotetan (CTT) is a novel cephalosporin antibiotic.
- Assessing the in vitro antibacterial spectrum and in vivo pharmacokinetics of CTT is crucial for its clinical application.
Observation:
- CTT exhibits potent in vitro activity against Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae, Serratia marcescens, and Salmonella species.
- Pharmacokinetic studies reveal CTT's serum concentration, half-life, and urinary excretion patterns following intravenous bolus injection and drip infusion.
- Clinical evaluation in 15 patients with bacterial infections demonstrated an 80% success rate with CTT treatment.
Findings:
- The minimum inhibitory concentrations (MICs) for susceptible bacteria ranged from <0.1 to 12.5 µg/ml.
- Following a 20 mg/kg intravenous dose, peak serum levels reached 175.0 µg/ml with a half-life of 3.53 hours (bolus) and 2.41 hours (infusion).
- Urinary excretion rates were 49.4% (infusion) and 64.2% (bolus) within 8 hours.
Implications:
- Cefotetan (CTT) shows promise as an effective antibiotic for treating various bacterial infections.
- The pharmacokinetic profile supports the potential for convenient dosing regimens.
- Further investigation into CTT's safety and efficacy is warranted, although initial results indicate a favorable safety profile with minor elevations in liver enzymes and eosinophilia observed in a small percentage of patients.
Abstract:
The authors have carried out the laboratory and clinical studies of cefotetan (CTT), and obtained the following results. The antibacterial activities of CTT were measured by the plate dilution method against the clinical isolates of S. aureus, E. coli, K. pneumoniae, S. marcescens and Salmonella sp. The susceptibility distribution of S. aureus to CTT was at concentration of 6.25-12.5 micrograms/ml and the peak of that was obtained at 6.25 micrograms/ml with an inoculum size of 10(6) cells/ml. And the peaks of susceptibility distribution of E. coli and K. pneumoniae to CTT were obtained at less than 0.1 microgram/ml respectively, and that of S. marcescens was obtained at 6.25-12.5 micrograms/ml with an inoculum size of 10(6) cells/ml. The growth of all strains of Salmonella sp. was inhibited at concentration of less than 0.1 microgram/ml. As for pharmacokinetic study, CTT was given by intravenous bolus injection and drip infusion for 30 minutes at a single dose of 20 mg/kg. After intravenous bolus injection of 20 mg/kg of CTT, the mean peak serum level was 175.0 +/- 7.0 micrograms/ml at 15 minutes after injection, and half-life time was 3.53 hours. After 30 minutes drip infusion of 20 mg/kg of CTT, the mean serum concentration was 106.0 +/- 6.0 micrograms/ml at end of infusion, half-life time was 2.41 hours. The mean urinary excretion rates were 49.4% and 64.2% up to 8 hours after drip and bolus injection of 20 mg/kg of CTT, respectively. CTT was given 15 cases with bacterial infection. Daily doses of CTT were from 15.0 to 107.0 mg/kg. Clinical results obtained were excellent and good responses in 12 of 15 cases (80.0%). No side effects were obtained except for 2 cases with elevation of GOT and GPT, and 1 case with eosinophilia.