Abstract
DL-8280 is an oxazine agalogue antibacterial drug for oral administration, which was first synthesized by Daiichi Seiyaku Co., Ltd. in 1980. Clinical effects and basic natures of this drug were examined in this study.
1. The antibacterial activity of DL-8280 was compared with that of NFLX and PPA. Each 25 strains of clinically separated S. aureus, E. coli, K. neumoniae, E. cloacae, S. marcescens, P. vulgaris, P. mirabilis and P. aeruginosa were inoculated at the concentration of 106 CFU/ml. DL-8280 and NFLX showed much higher antibacterial activities than PPA for all the strains studied. The comparison between DL-8280 and NFLX showed that their activities were similar, except that the former was slightly superior for S. aureus and K. pneumoniae and the latter for P. mirabilis and P. aeruginosa.
2. Serum concentrations and urinary excretion of DL-8280 were examined in the fasting state and after a meal of 600 Cal. Three hundred mg of this drug was orally administered to 6 healthy adult male volunteers. No significant difference was observed between the peak serum concentrations in the fasting (2.63 μg/ml) and fed (2.46 μg/ml), although the peak time of them was slightly different: one versus two hours on the average. Urinary excretion within 24 hours after the administration was above 90% under both the conditions.
3. Clinical effects of DL-8280 were examined in 38 patients: acute bronchopneumonia (1), acute bronchitis (18), acute tonsillitis (9), secondary infection of bronchiectasis (4), chronic bronchitis (4), acute pyelonephritis (1), and acute cystitis (1). Excepting two cases, they all received 300 mg/day of this drug, which was divided into three times a day. For the mild acute infection of the respiratory system and urinary tract, DL-8280 with the dose duration within 7 days was effective in 27 cases out of 29. For chronic respiratory infections, this drug was effective in only 3 cases out of 8, when the dose duration was between 7 and 14 days. It was not effective in one patient with acute bronchopneumonia. Bacteria were eradicated by the administration in 25 cases out of 28, in which bacteria had been detected before the administration.
4. As a side effect, anorexia was observed in three cases. No abnormality was recognized in the findings of blood examinations and hepatic functions before and after the administration.
