A new semisynthetic 1-oxa-beta-lactam derivative,
6059-S, was evaluated for its safety and efficacy in children. Twenty-five patients were treated with 10 to 274 mg/kg per day of
6059-S by
intravenous administrations. The diagnosis of the patients were acute
pharyngitis (2), acute
bronchitis (2),
pneumonia (4),
pertussis (4), acute
enterocolitis (2), recurrent
urinary tract infection (2), suspected
septicemia (3), and acute purulent
meningitis (1); and the remaining 5 patients were considered to have nonbacterial
infections. The pathogens recovered were Streptococcus pneumoniae (1), Haemophilus influenzae (4), Haemophilus parainfluenzae (1), Enterobacter cloacae (1), Enterobacter aerogenes (1), Proteus morganii (1), Psuedomonas aeruginosa (2) and Salmonella typhimurium (1). All the patients of
bacterial infections were cured after the
6059-S therapy. However, Pseudomonas aeruginosa and Salmonella typhimurium were not eradicated after the
6059-S therapy, and the rate of bacterial disappearance was 75%.
Diarrhea (3), precordial
pain (2, only in cases with high-dose
therapy), transient elevation of GOT and GPT (2), and transient
eosinophilia (2) were found to be associated with the
6059-S therapy. However, no severe adverse reactions were encountered. Half life of the serum
6059-S level was 1.34 +/- 0.16 hours. CSF concentrations in a case with Haemophilus influenzae
meningitis ranged 4.0 to 9.7 mcg/ml after an
intravenous injection of 34.3 to 75 mg/kg of
6059-S. From the present study,
6059-S appears to be a safe and effective
antibiotic when used in children with susceptible
bacterial infections. It remains to be further determined whether
6059-S is superior to ABPC in the treatment of Haemophilus influenzae
meningitis.