1988 Volume 36 Issue Supplement2-Clinical Pages 803-825
We performed basic and clinical studies on NY-198, a new antimicrobial agent of pyridonecarboxylic acid derivation. The results were as follows.
1) Pharmacokinetics
NY-198 was given orally to 5 patients with chronic renal failure (3 mild cases: Ccr=58.8-72.8ml/min; 1 moderate: Ccr=30.0ml/min; 1 severe: Ccr=9.8ml/min) in a single dose of 200mg. The peak mean serum level of NY-198 was 1.50μg/ml at 4h after oral administration in the mild cases, 1.63μg/ml after 4h in the moderate, and 1.35μg/ml after 8h in the severe case. The 24-h urinary recovery rate was 59.08% in the mild cases, 16.56% in the moderate and 5.78% in the severe case.
2) Antibacterial activity
The antibacterial activities of NY-198, norfloxacin, ofloxacin, enoxacin, ciprofloxacin and cefaclor against Gram-negative bacteria isolated from urinary tract infections were compared, and the activity of NY-198 was decidedly superior to that of cefaclor, almost equal to those of norfloxacin, ofloxacin and enoxacin and slightly inferior to that of ciprofloxacin.
3) Clinical effect
Thirty-one cases with various types of urinary tract infection were treated with NY-198. According to the criteria of the Japanese UTI Committee, the overall clinical efficacy rate was 100%(3/3) in acute simple cystitis when treated with a daily oral dose of 3×200mg of NY-198 for 3 days and 77.8%(14/18) in chronic complicated cystitis when treated with 3×200mg for 5 days. Clinical efficacy in chronic prostatitis proved good in 1 case and fair in 4.
4) Side-effects
No side-effects or abnormal changes in laboratory examinations were observed.
