Nishimura T, Takashima T, Hiromatsu K, Tabuki K
Jpn J Antibiot. 1982 Nov;35(11):2699-707.
Antimicrobial, pharmacokinetic and clinical evaluation of cefsulodin (CFS) was made and the following results were obtained. 1. Antimicrobial activity of CFS against P. aeruginosa was similar to a little lower than that of GM. Antimicrobial activity of CFS against S. aureus was similar to that of SBPC and against E. coli CFS showed lower antimicrobial activity. 2. Twenty or 50 mg/kg CFS was administered by 1 hour intravenous drip infusion. Average serum levels at the completion of the infusion were 35.1 +/- 8.0, 114.5 +/- 36.1 micrograms/ml and 1.6 +/- 0.7, 4.5 +/- 3.2 micrograms/ml at 6 hours afterward with the half life times of 1.50, 1.29 hours respectively. In case of 12.1 mg/kg 1 hour intravenous drip infusion, peak serum level was 13.4 micrograms/ml at the completion of infusion, and the concentration in the sputum was 1.0 micrograms/ml at 5 hours after completion of infusion. Average serum levels of CFS by one shot infusion of 20 mg/kg were 58.4 +/- 6.8 micrograms/ml, 2.7 +/- 2.5 micrograms/ml at 15 minutes and 6 hours after injection respectively. Half-life time was 1.54 hours. Average urinary excretion rates of CFS were 64.4%, 64.2% and 48.9% up to 6 hours after 1 hour intravenous drip infusion of 20 mg/kg, 50 mg/kg CFS and one shot intravenous of 20 mg/kg CFS respectively. 3. CFS was administered to 2 pneumonia cases caused by P. aeruginosa, i.e. one was 15 years and 11 months old male accompanying bronchial asthma and the another 4 years old male with LENNOX syndrome. Neither bacteriological nor clinical efficacy was, however, observed. Side effect as well as bacterial superinfection were not observed.