Brunner Martin, Derendorf Hartmut, Müller Markus
Department of Clinical Pharmacology, Division of Clinical Pharmacokinetics, Medical University of Vienna, Waehringer Guertel 18-20, A-1090 Vienna, Austria.
Curr Opin Pharmacol. 2005 Oct;5(5):495-9. doi: 10.1016/j.coph.2005.04.010.
Inadequate tissue penetration of antibiotics can lead to therapeutic failure and bacterial resistance. Pharmacokinetic evaluation of antibiotics should therefore be based on tissue rather than serum concentrations. Over several years, tissue concentration data obtained by methods such as tissue biopsies have flawed the correct interpretation of antibiotic tissue distribution. Microdialysis--a semi-invasive catheter-based sampling technique--has been employed for the in vivo measurement of antibiotic tissue pharmacokinetics. Owing to selective access to the target site for most anti-infective drugs, microdialysis satisfies regulatory requirements for pharmacokinetic distribution studies and might become a reference technique for tissue distribution studies in the near future. Furthermore, microdialysis might contribute to the definition of meaningful surrogate markers for antibiotic efficiency during drug development.
抗生素组织穿透不足可导致治疗失败和细菌耐药。因此,抗生素的药代动力学评估应基于组织浓度而非血清浓度。多年来,通过组织活检等方法获得的组织浓度数据影响了对抗生素组织分布的正确解读。微透析——一种基于半侵入性导管的采样技术——已被用于体内抗生素组织药代动力学的测量。由于大多数抗感染药物可选择性地进入靶部位,微透析满足药代动力学分布研究的监管要求,并且在不久的将来可能成为组织分布研究的参考技术。此外,微透析可能有助于在药物研发过程中定义抗生素疗效的有意义替代标志物。