Cellular pharmacodynamics and pharmacokinetics of antibiotics: current views and perspectives.
Cellular pharmacodynamics and pharmacokinetics of antibiotics: current views and perspectives.
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发表时间：
2006-03
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通讯作者：
F. Van Bambeke;Maritza Barcia-Macay;S. Lemaire;P. Tulkens
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作者：
F. Van Bambeke;Maritza Barcia-Macay;S. Lemaire;P. Tulkens
细胞内感染的治疗需要使用具有适当细胞药代动力学和药效学特性的抗生素。然而，这些特性不能简单地根据细胞药物积累和肉汤中最低抑制浓度来预测。在大多数情况下，细胞内活性实际上低于细胞外活性，尽管所有抗生素的细胞内浓度至少与细胞外浓度相等，而且往往高于细胞外浓度。这种差异可能是由于抗生素活性表达的损害或细胞内细菌反应性的改变。因此，在适当的模型中评估抗生素的细胞内活性显得很重要。
The treatment of intracellular infections requires the use of antibiotics presenting appropriate cellular pharmacokinetic and pharmacodynamic properties. These properties, however, cannot be predicted on the simple basis of cellular drug accumulation and minimum inhibitory concentration in broth. In most cases, intracellular activity is actually lower than extracellular activity, despite the fact that all antibiotics reach intracellular concentrations that are at least equal to, and more often higher than the extracellular concentrations. This discrepancy may result from impairment of the expression of antibiotic activity or a change in bacterial responsiveness inside the cells. It therefore appears important to evaluate the intracellular activity of antibiotics in appropriate models.