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Laboratory and clinical studies of 6059-S in pediatric field



Laboratory and clinical studies of 6059-S in pediatric field



Japanese Journal of Antibiotics 34(5): 800-816



The authors have carried out the laboratory and clinical studies of 6059-S. The results were as follows: The sensitivity was estimated by the plate dilution method on 27 strains of S. aureus, 26 strains of E. coli, K. pneumoniae and P. aeruginosa, 21 strains of Salmonella sp. and 9 strains of GM resistant P. aeruginosa isolated from patients. The distribution of sensitivity of S. aureus was 6.25-12.5 micrograms/ml and the peak of distribution was 6.25 micrograms/ml. The growth of 80.8% of E. coli was inhibited at concentration of less than 0.1 microgram/ml. The growth of 88.5% of K. pneumoniae was inhibited at concentration of less than 0.2 microgram/ml. The growth of 81.0% of Salmonella sp. was inhibited at concentration of less than 1.56 microgram/ml. The distribution of sensitivity of P. aeruginosa was 12.5- greater than 100 micrograms/ml and the peak of distribution was 25.0 micrograms/ml. The distribution of sensitivity of GM-resistance P. aeruginosa (greater than or equal to 25 micrograms/ml) was 12.5-50 microgram/ml and 5 of 8 strains were inhibited at concentration of less than 25 micrograms/ml. Phagocytosis was determined by Quie's method. Phagocytosis of E. coli, K. pneumoniae, Proteus vulgaris and Enterobacter cloacae by human polymorphonuclear neutrophil was more enhanced in the presence of 1 MIC and 1/2 MIC for 6059-S than for cefazolin at 4 and 6 hours after incubation. But phagocytosis of S. aureus did not enhanced in the presence of 6059-S. 6059-S was given by intravenous administration for 5 minutes and drip infusion for one hour at a single dose of 10 mg/kg of 6059-S to 3 and 4 children respectively. After intravenous administration of 6059-S, the mean peak serum level was 76.0 +/- 2.0 micrograms/ml at 15 minutes, 36.0 +/- 2.8 micrograms/ml at one hour, 1.5 +/- 0.4 micrograms/ml at 6 hours respectively. Half-life time was 1.3 hours. And after drip infusion of 6059-S was 39.9 +/- 9.7 micrograms/ml at one hour, 11.7 +/- 4.8 micrograms/ml at 3 hours and 1.8 +/- 1.4 micrograms/ml at 7 hours respectively. Half-life time was 1.4 hours. The mean urinary excretion rate was 90.4 +/- 6.1%, 76.5 +/- 16.0% up to 6 hours after intravenous administration and drip infusion respectively. 6059-S was effective in 17 cases out of 18 cases with bacterial infections. No side effects were observed except for 4 cases with elevation of serum transaminase, each on case of eosinophilia and of anemia.

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Accession: 043505318

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PMID: 6457177


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