Wise R, Lockley R, Webberly M, Adhami Z N
J Antimicrob Chemother. 1984 Sep;14 Suppl C:75-81. doi: 10.1093/jac/14.suppl_c.75.
Two new quinoline compounds, enoxacin (600 mg) and norfloxacin (400 mg) were administered consecutively to six healthy male volunteers. The levels of the two agents were measured in serum, urine and blister fluid. The mean peak serum level of enoxacin was 3.7 mg/l and attained at a mean time of 1.9 h after administration; the mean peak serum level of norfloxacin was 1.45 mg/l at a mean time of 1.5 h. The mean serum half-lives were 6.2 h for enoxacin and 3.25 h for norfloxacin. Both agents penetrated blister fluid well and reached maximum levels of 2.9 mg/l (for enoxacin) and 1.0 mg/l (for norfloxacin). The 24 h urinary recovery of enoxacin of 61% was about twice that of norfloxacin. No adverse effects of either agent were observed. The data suggest that enoxacin might be used as a once daily dose for the treatment of urinary tract infections, but twice daily for the treatment of susceptible pathogens causing systemic (as against urinary) infections.
将两种新的喹啉化合物,依诺沙星(600毫克)和诺氟沙星(400毫克)连续给予6名健康男性志愿者。在血清、尿液和水疱液中测量这两种药物的水平。依诺沙星的平均血清峰值水平为3.7毫克/升,给药后平均1.9小时达到;诺氟沙星的平均血清峰值水平为1.45毫克/升,平均时间为1.5小时。依诺沙星的平均血清半衰期为6.2小时,诺氟沙星为3.25小时。两种药物都能很好地渗透到水疱液中,依诺沙星的最高水平达到2.9毫克/升,诺氟沙星为1.0毫克/升。依诺沙星24小时尿回收率为61%,约为诺氟沙星的两倍。未观察到两种药物有不良反应。数据表明,依诺沙星可作为每日一次剂量用于治疗尿路感染,但治疗引起全身性(而非泌尿系统)感染的易感病原体时需每日两次。