[Experimental and clinical studies on 6059-S (author's transl)].

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.