Experimental and clinical studies in the pediatric field on
6059-S, a newly synthesized broad spectrum parenteral
antibiotics, were carried out, and the following results were obtained. Antibacterial activities of
6059-S against S. pyogenes, S. aureus, E. coli and P. aeruginosa, recently isolated from patients, 50 strains respectively was compared with that of
cefazolin (CEZ),
cefmetazole (CMZ),
ceftizoxime (CZX),
cefotiam (CTM) and
ticarcillin (TIPC).
6059-S was less active than the other compound against S. aureus and S. pyogenes, but was about 1-5 times more active than other CEZ, CTM, CMZ and CZX against E. coli, and
6059-S had a activity against P. aeruginosa. It was equal or slightly more activity than that of TIPC. Serum concentrations were measured in 14 infants (3 y 3m-12 y) by one shot or
intravenous drip infusion with 10 mg/kg or 20 mg/kg. By one shot
intravenous infusion, the peak of serum concentrations of
6059-S with 10 mg/kg and 20 mg/kg were 40.4-44.2 mcg/ml, 79.1-90.8 mcg/ml at 30 minutes after administration respectively, and that's half life were 1.5, 1.4 hours. By
intravenous drip infusion, the peak of serum concentration was 89.9 mcg/ml at the end of administration, 13.7 mcg/ml at 5 hours after administration, and half life was 1.5 hours. The urinary recovery rate of
6059-S were 97.4, 67.4% during 6 hours in 2 cases. The cerebrospinal fluid concentration of
6059-S were 2.4-3.6 mcg/ml at 90 minutes after
intravenous infusion administration, and the CSF/serum ratio were about 7-8%. Clinical studies of
6059-S was performed in total of 27 cases (25 patients); 8 cases of
urinary tract infection, 15 cases of
respiratory tract infection, 1 case of
staphylococcal scalded skin syndrome, 1 case of
peritonitis, 2 cases of purulent
meningitis, with the dose of
6059-S 150 mg/kg/day in purulent
meningitis, 40-80 mg/kg/day in other disease. That's efficacy rate was 85.2%. Side effect observed in this
therapy were 2 cases (
exanthema 1,
diarrhea 1), and 2 cases of rise of GOT, GPT.