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左氧氟沙星和莫西沙星对不同氟喹诺酮敏感性肺炎球菌菌株的体外和体内活性之间的相关性

Correlation between in vitro and in vivo activity of levofloxacin and moxifloxacin against pneumococcal strains with different susceptibilities to fluoroquinolones.

作者信息

Huelves Lorena, Sevillano David, Martínez-Marín Carmina, López-Casla María Teresa, Gracia Matilde, Alou Luis, del Carmen Ponte María, Prieto José, Soriano Francisco

机构信息

Unit for Research in Medical Microbiology and Antimicrobial Chemotherapy, Fundación Jiménez Díaz-UTE, Avenida de Reyes Católicos 2, 28040 Madrid, Spain.

出版信息

Int J Antimicrob Agents. 2006 Apr;27(4):294-9. doi: 10.1016/j.ijantimicag.2005.10.022. Epub 2006 Mar 9.

Abstract

In vitro and in vivo models were developed to evaluate the efficacy of levofloxacin and moxifloxacin against three serotype 3 pneumococcal strains with different susceptibilities to fluoroquinolones (wild-type, parC mutant, and parC, parE and gyrA mutant). Levofloxacin and moxifloxacin reduced the bacterial burden in the in vitro pharmacodynamic and animal models for the wild-type strain but had very little activity against the fully resistant strain (parC, parE and gyrA mutant). Levofloxacin showed very little activity both in the in vitro pharmacodynamic model and in the animal model for the strain having a mutation in parC (levofloxacin and moxifloxacin minimum inhibitory concentrations, 2mg/L and 0.25mg/L, respectively). However, moxifloxacin still had a significant in vitro and in vivo activity against this strain.

摘要

建立了体外和体内模型,以评估左氧氟沙星和莫西沙星对三种对氟喹诺酮类药物敏感性不同的3型肺炎球菌菌株(野生型、parC突变体以及parC、parE和gyrA突变体)的疗效。在体外药效学和动物模型中,左氧氟沙星和莫西沙星降低了野生型菌株的细菌载量,但对完全耐药菌株(parC、parE和gyrA突变体)几乎没有活性。对于parC发生突变的菌株(左氧氟沙星和莫西沙星的最低抑菌浓度分别为2mg/L和0.25mg/L),左氧氟沙星在体外药效学模型和动物模型中均显示出极低的活性。然而,莫西沙星对该菌株仍具有显著的体外和体内活性。

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