1984 Volume 32 Issue Supplement9 Pages 630-637
For the studies of absorption and excretion, AC-1370 was given to 5 healthy volunteers at a dose of 1g or 4g in a cross-over manner by 1 hour intravenous drip infusion. The Cmax and T 1/2 of AC-1370 were 117.4 μg/ml and 1.45 hours for 1g injection, and 278.9 μg/ml and 1.63 hours for 4g injection. The urinary recovery rates within 8 hours were 90.8% for 1g injection, and 94.4% for 4g injection. AC-1370 was also administered to each two dehydrated and hydrated rabbits at a dose of 500mg/3 kg by a single intravenous injection, and the levels in serum and various organ tissues were measured. The every level for dehydrated rabbits was higher than the corresponding level for hydrated ones.
For clinical evaluation, AC-1370 was given to 9 patients with urinary tract infections at a daily dose of 2 to 4g twice a day. Six of these 9 cases were evaluated by the criteria of UTI committee, and the clinical response to AC-1370 treatment was excellent in 3 cases and poor in 3 cases with 50% of effectiveness rate.
No remarkable side effect was observed except for one case that showed slight elevation of BUN and serum creatinine with slight decrease of WBC. This was transient, but could not be denied to be due to the AC-1370 treatment.
When considering the report that in vivo antimicrobial activity of AC-1370 is more potent than in vitro, AC-1370 is expected to be useful against pyelonephritis rather than chronic complicated cystitis.
