Preclinical studies were carried out on cefotetan (CTT), together with clinical studies in the field of pediatrics. The following results were obtained. A total of 114 clinical isolates was employed to determine the minimum inhibitory concentrations (MICs) of CTT against various bacterial species. Against E. coli, Salmonella, K. pneumoniae and P. mirabilis, the MICs of CTT showed a peak at 0.78 μg/ml, and most of the strains were inhibited by a CTT concentration of 6.25 μg/ml or less. The MICs for S. marcescens strains showed a peak at 25 μg/ml, with 25% of the strains having MIDs of 3.13 μg/ml or less, and 67% having MICs of 25 μg/ml or more. All of the P. aeruginosa strains had MICs of over 100 μg/ml. Against all of the tested strains of S aureus, a Gram-positive bacterium, CTT showed MICs of 12.5 μg/ml or more, while all of the strains of S faecalis were found to have MICs of over 100 μg/ml. CTT was administered intravenously to pediatric patients as a bolus injection, and then the concentration of the antibiotic in the serum was determined as a function of time. CTT was drip-infused intravenously over a period of 1 hour, and then the serum concentration of the drug was monitored with the passage of time. CTT was administered to 3 meningitis patients, and then the concentration of the antibiotic in the cerebrospinal fluid was measured with the course of time. A single dose of CTT, ranging from 54 to 83 mg/kg, was administered, and the CSF concentration ranged from 1.1 to 4.8 μg/ml. The ratio of the concentration in the CSF to the serum concentration ranged from 0.8 to 3.6%. No cumulative effect of CTT was seen. CTT was administered intravenously to 16 cases of bacterial infection. A good clinical effect was seen in 14 of these cases (88%). The bacteriological effect of CTT was investigated in 9 patients. In all cases the causative bacteria were eliminated, for a 100% bacteriological efficacy rate. The bacterial isolates consisted of 5 strains of E. coli, 2 strains of S. pneumoniae, 1 strain of H. influenzae, and 1 strain of H. parainfluenzae. The following side effects to the CTT therapy were recorded; 4 cases of diarrhea, and elevated values of GOT and GPT in 1 patient. All of these side effect symptoms disappeared rapidly after the drug administration was stopped.
|Number of pages||15|
|Journal||Japanese Journal of Antibiotics|
|Publication status||Published - 1983|
ASJC Scopus subject areas
- Molecular Medicine