Hospital General Universitario de Elche, Universidad Miguel Hernández, Spain.
APMIS. 2011 Apr;119(4-5):304-8. doi: 10.1111/j.1600-0463.2011.02735.x. Epub 2011 Mar 22.
As linezolid is emerging as a useful alternative in the treatment of multi-resistant tuberculosis, we developed an in vitro model to elucidate certain aspects of the interaction that takes place between the microorganism and the antibiotic. We found that the drug does not generate resistant mutants following repeated exposure at subinhibitory concentrations and that it exhibits bactericidal activity against most of the susceptible strains in vitro at high concentrations (83.3% of the strains at concentrations of 50 μg/mL) in the exponential growth phase. This bactericidal activity is much less if the microorganism is in nonreplicating phase, even in the case of susceptible strains in vitro. Therefore, linezolid appears to be an alternative as far as generation of resistance is concerned in the treatment of multi-resistant tuberculosis. However, it has limited bactericidal capacity against strains in nonreplicant phase, which makes it necessary to use linezolid in combination with other drugs that act on these microorganisms.
由于利奈唑胺在治疗多重耐药结核病方面的应用日益广泛，我们开发了一种体外模型来阐明微生物和抗生素之间相互作用的某些方面。我们发现，该药物在亚抑菌浓度下反复暴露时不会产生耐药突变体，并且在对数生长期高浓度（50μg/mL 时为 83.3%的菌株）下对大多数体外敏感株具有杀菌活性。如果微生物处于非复制阶段，即使是体外敏感株，这种杀菌活性也会大大降低。因此，利奈唑胺在治疗多重耐药结核病方面似乎是一种替代药物，不会产生耐药性。然而，它对非复制阶段的菌株的杀菌能力有限，这使得有必要将利奈唑胺与其他作用于这些微生物的药物联合使用。
