Nishi T, Tsuchiya K
Antimicrob Agents Chemother. 1980 Oct;18(4):549-56. doi: 10.1128/AAC.18.4.549.
The efficacies of several dosage schedules, productive of plasma levels of cefotiam and cefazolin of short and long duration and starting at three levels of cefotiam and cefazolin of short and long duration and starting at three different times (3, 18, and 30h) after infection, were examined in experimental pneumonia caused by Klebsiella pneumoniae DT-S in mice. With each of the multiday regimens there was a large segment of the day when plasma levels fell below assayable concentrations. In all cases, cefotiam proved about eight times as active as cefazolin, indicating that the potent in vitro antibacterial activity of cefotiam was well reflected in the therapeutic effect in this model infection. As judged by the total dose administered, the regimen of cefotiam producing a low but sustained plasma level gave better therapeutic effects than that exhibiting a high but transient plasma level. The cefotiam levels in the plasma of mice that received the regimen effective when initiated at 18 h after infection were less than the expected levels in humans after intravenous infusion of the usual clinical dose.
在小鼠由肺炎克雷伯菌DT-S引起的实验性肺炎中,研究了几种给药方案的疗效,这些方案能产生短时间和长时间的头孢替安和头孢唑林血浆水平,并在感染后三个不同时间点(3、18和30小时)开始,起始头孢替安和头孢唑林有三个水平。对于每种多日给药方案,一天中都有很长一段时间血浆水平降至可检测浓度以下。在所有情况下,头孢替安的活性约为头孢唑林的八倍,这表明头孢替安强大的体外抗菌活性在该模型感染的治疗效果中得到了很好的体现。从给药总量判断,产生低但持续血浆水平的头孢替安给药方案比产生高但短暂血浆水平的方案具有更好的治疗效果。在感染后18小时开始使用有效给药方案的小鼠血浆中,头孢替安水平低于人类静脉输注常规临床剂量后预期的水平。