Butts J D
University of North Carolina School of Pharmacy, Chapel Hill.
Clin Pharmacokinet. 1994 Jul;27(1):63-84. doi: 10.2165/00003088-199427010-00006.
Intracellular penetration, accumulation and disposition of antibacterial agents is crucial for effective treatment of infections caused by intracellular bacteria. Intracellular concentrations and locations of both antibacterials and bacteria remain poorly understood and further research is needed to establish the importance of these concepts. For example, concepts that have been shown to be important outcome predictors when applied to concentrations of antibacterial agents in the serum include: (i) the effect of the peak antibacterial serum concentration to minimum concentration inhibitory to 90% of organisms (MIC90) for bacteria; (ii) the effect of length of time the serum antibacterial concentration remains above the MIC90 curve; or (iii) the area under the MIC90 curve, but above the serum antibacterial concentration curve. Further research should determine whether or not these concepts have important applications in an intracellular environment. Intracellular pathogens have been increasingly contributing to respiratory infections in the community. Therefore, on the basis of intracellular activity against bacteria causing respiratory infections, macrolides are favoured as the most broad spectrum class of oral antibacterial agents available for the treatment of patients with community-acquired respiratory infections.
抗菌药物的细胞内渗透、积累和分布对于有效治疗由细胞内细菌引起的感染至关重要。抗菌药物和细菌在细胞内的浓度及位置仍了解甚少,需要进一步研究以确定这些概念的重要性。例如,当应用于血清中抗菌药物浓度时,已被证明是重要结果预测指标的概念包括:(i)抗菌血清峰值浓度对细菌最低抑菌浓度(MIC90)的影响;(ii)血清抗菌浓度保持高于MIC90曲线的时间长度的影响;或(iii)MIC90曲线下但高于血清抗菌浓度曲线的面积。进一步的研究应确定这些概念在细胞内环境中是否有重要应用。细胞内病原体在社区呼吸道感染中的作用日益增加。因此,基于对引起呼吸道感染细菌的细胞内活性,大环内酯类药物作为可用于治疗社区获得性呼吸道感染患者的最广谱口服抗菌药物而受到青睐。