1984 Volume 32 Issue Supplement9 Pages 300-308
The studies on antimicrobial activity, absorption, excretion and clinical evaluation of AC-1370, a new cephem, were performed, and the following results were obtained:
1) The antibacterial activity of AC-1370 was examined against each 50 clinical isolates of 7 species. AC-1370 showed the most strong activity against S. pyogenes among them, the MIC80 value being 0.39μg/ml. According to each curve of cumulative percent on MICs, the activity against the remaining 6 species was judged as in order of P. mirabilis, K. pneumoniae, E. voli, S. marcescens, E. cloacae, P. aeruginosa and S. aureus.
The MIC80 values for these species corresponded to 0.39, 1.56, 6.25, 25, 25, 25, 12.5 and 25μg/ml, respectively.
2) The peak serum concentration of 68.6μg/ml in a sepsis patient was attained at the end of intravenous drip infusion with a dose of 1.0 g over a period of 1 hour. The serum concentration was gradually decreased with the half life of 1.74 hours, and the concentration at 8 hours from administration was 1.1μg/ml.
The serum concentrations in a renal insufficient patient with Ccr of 15 ml/min. and two chronic renal insufficient patients with hemodialysis were respectively 122.0μg/ml and 121.3 126.4μg/ml at 5 minutes from a single bolus intravenous administration of 1.0 g, and 54 and 17.6 18.5μg/ml at 4 hours. The results suggested that AC-1370 was excreted by dialysis.
3) AC-1370 was administered to 6 patients with infectious diseases consisting of each one case of chronic bronchitis, localized peritonitis and urinary tract infection and of 3 cases of sepsis at a daily dose of 1 to 2 g. All the cases were evaluated clinically as good response. Neither side effects nor abnormal laboratory findings were observed.
