Arai S, Gohara Y, Akashi A, Kuwano K, Nishimoto M, Yano T, Oizumi K, Takeda K, Yamaguchi T
Department of Microbiology, Kurume University School of Medicine, Japan.
Antimicrob Agents Chemother. 1993 Feb;37(2):287-92. doi: 10.1128/AAC.37.2.287.
The efficacies of the new quinolones temafloxacin, ofloxacin, and ciprofloxacin were investigated against Mycoplasma pneumoniae in an experimental hamster pneumonia model. Hamsters were infected intratracheally with M. pneumoniae and sacrificed 18 h after the final medication, and their lungs were aseptically removed, homogenized, and cultured quantitatively. The efficacies of these drugs were determined by the CFU of M. pneumoniae in lungs. Temafloxacin and ofloxacin, but not ciprofloxacin, were active when the oral administration of 200 mg/kg of body weight per day (once per day) for 5 days was initiated 24 h after infection. Although no effect on the elimination of M. pneumoniae was observed after the administration of these drugs at 200 mg/kg/day at 5 days after infection, the continuous administration for 15 days of temafloxacin, but not ofloxacin or ciprofloxacin, significantly reduced viable M. pneumoniae in the lungs. These results suggest that temafloxacin and ofloxacin are effective in the acute phase of infection and, moreover, that temafloxacin is effective in the late stage of infection during which progressive lung alterations and continuous increases in mycoplasmal growth occurred. The peak levels of temafloxacin in sera and lungs after oral administration were similar to those of ofloxacin and higher than those of ciprofloxacin. The areas under the curve of temafloxacin in the lung tissue, however, were higher than those of ofloxacin and ciprofloxacin. On the basis of these results, temafloxacin and ofloxacin might be promising antimicrobial agents for the treatment of mycoplasmal infection.
在实验性仓鼠肺炎模型中研究了新型喹诺酮类药物替马沙星、氧氟沙星和环丙沙星对肺炎支原体的疗效。仓鼠经气管内感染肺炎支原体,并在末次给药后18小时处死,无菌取出肺脏,匀浆并进行定量培养。通过肺中肺炎支原体的菌落形成单位(CFU)来确定这些药物的疗效。当在感染后24小时开始每天口服200mg/kg体重(每天一次),持续5天时,替马沙星和氧氟沙星有活性,但环丙沙星无活性。虽然在感染后5天给予这些药物200mg/kg/天时未观察到对肺炎支原体清除的影响,但替马沙星连续给药15天可显著降低肺中存活的肺炎支原体,而氧氟沙星和环丙沙星则无此作用。这些结果表明,替马沙星和氧氟沙星在感染急性期有效,此外,替马沙星在感染后期也有效,此时肺部出现进行性改变且支原体生长持续增加。口服给药后,替马沙星在血清和肺中的峰值水平与氧氟沙星相似,且高于环丙沙星。然而,替马沙星在肺组织中的曲线下面积高于氧氟沙星和环丙沙星。基于这些结果,替马沙星和氧氟沙星可能是治疗支原体感染的有前景的抗菌药物。