评估的细菌杀死当造型支气管肺的莫西沙星与左氧氟沙星的药动学特征parC-containing肺炎链球菌的分离。

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Deryke CA, Du X,尼克洛DP

评估的细菌杀死当造型支气管肺的莫西沙星与左氧氟沙星的药动学特征parC-containing肺炎链球菌的分离。

J Antimicrob Chemother。2006年9月,58 (3):601 - 9。Epub 2006年7月19日。

PubMed ID

16857688 (在PubMed

]

文摘

目标:第一步帕洛阿尔托研究中心的患病率正日益认识到突变体在肺炎链球菌和新创的发展阻力在氟喹诺酮类治疗的问题。之前的工作由我们小组展示了莫西沙星的能力,但不是左氧氟沙星,根除parC突变体。这个实验的目的是确定是否这些氟喹诺酮类抗生素提供等价的细菌杀死当类似的AUC /麦克风被检查。方法:体外药效学模型被用来模拟上皮衬里流体(精灵)浓度后口服左氧氟沙星的每天500毫克一次,莫西沙星在老年人400毫克每日一次。此外,一系列的AUC /中等收入国家也效仿,包括左氧氟沙星750毫克每日一次。包含第帕洛阿尔托研究中心五个不同的肺炎链球菌突变和一个隔离没有突变检测48 h和time-kill曲线建立了。收集样本(0)24和48 h表型和基因型分析。高效液相色谱法是用于验证目标暴露。结果:分离没有帕洛阿尔托研究中心突变4日志显示降低cfu与左氧氟沙星治疗后500毫克,没有选择抵抗。在所有5个隔离包含第帕洛阿尔托研究中心突变,电阻出现在48 h >或= 16倍增加麦克风和收购gyrA突变。 Increasing the exposure of levofloxacin to approximately 750 mg dose still led to > or =16-fold increase in MIC at 48 h in two of the four isolates containing parC mutations. On the other hand, moxifloxacin 400 mg sustained bacterial killing against the two isolates tested without the selection of resistant mutants. It appears that the critical AUC/MIC necessary to prevent the acquisition of resistance for levofloxacin is 200 and approximately 400 for moxifloxacin. CONCLUSIONS: Due to suboptimal exposures, once-daily oral regimens of levofloxacin at both 500 and 750 mg inconsistently led to bactericidal activity and the frequent acquisition of a second-step gyrA mutation in S. pneumoniae isolates already containing a first-step parC mutation. Conversely, once-daily moxifloxacin 400 mg provides exposures that vastly exceed the apparent efficacy breakpoint and did not select for second-step mutants until exposures were decreased 4-fold. As a result of these data and the emerging literature involving mutations in the pneumococcus, caution should be exercised when the respiratory fluoroquinolones are used to treat patients infected with S. pneumoniae suspected of having parC mutations.

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药物靶点

药物	目标	类	生物	药理作用	行动
莫西沙星	DNA拓扑异构酶4单元	蛋白质	流感嗜血杆菌(写明ATCC 51907株/ DSM 11121 / KW20 / Rd)	是的	抑制剂	细节