CLINICAL STUDIES ON AC-1370
1984 Volume 32 Issue Supplement9 Pages 217-230
Details
1984 Volume 32 Issue Supplement9 Pages 217-230
AC-1370, a new cephem antibiotic, was studied clinically, and the following results were obtained:
1. Antibacterial activity
MICs of AC-1370 for clinical isolates were determined and compared with those of cefoperazone, ceftizoxime, latamoxef, cefotaxime, cefmenoxime and cefpiramide. Antibacterial activity of AC-1370 against such clinical isolates as P. rnirabilis and Indole (+) Proteus was almost on the same level as those of cefpiramide, and against E. coli was its activity slightly inferior to cefpiramide. Antibacterial activity of AC-1370 against P. aeruginosa was slightly inferior to those of cefoperazone and cefpiramide, but stronger than cefotaxime, latamoxef, ceftizoxime and cefmenoxime.
2. Absorption and excretion
The serum and urinary concentrations of AC-1370 were determined in 5 healthy volunteers after 1.0g intravenous administration and were compared, in a cross-over manner, with those of cefoperazone. Influence of probenecid on the concentrations was also investigated.
The serum concentration of AC-1370 at 5 minutes after administration averaged 146.1 btgfml, and after that the concentration decreased with the half-life (β-phase) of 1.71 hours. The serum concentration of AC-1370 was slightly lower than that of cefoperazone until 15 minutes after administration, but was almostthe same as cefoperazone after such period. The urinary recovery rate up to 12 hours averaged 88.6%, which was 2.7 times as high as that of cefoperazone. The average total clearance of AC-1370 was 134.0ml/min slightly higher than that of cefoperazone, but renal clearance of 114.7ml/min was 3.0 times higher than cefoperazone.
The combination use of probenecid with AC-1370 showed no significant difference on the serum concentration, half-life and urinary recovery rate when compared with single administration of AC-1370.
3. Clinical results
AC-1370 was administered to 6 patients including 4 cases of pneumonia, I case of cholecystitis and 1 case of chronic pyelonephritis at a daily close of 2 to 4 grams for 6 to 19 days. The clinical response was excellent in 2 cases, good in 3 cases and fair in 1 case. In the course of clinical study, slight anorexia was observed in one case as a side effect but no abnormal laboratory findings were noted.
