新型噁唑烷酮类抗生素利奈唑胺

Pharmacology and clinical evaluation of linezolid

利奈唑胺(linezolid)是第一个应用于临床的新型噁唑烷酮类抗生素,通过抑制蛋白起始复合物的形成抑制细菌蛋白质合成,在体内、外对葡萄球菌、链球菌、肠球菌等耐药G+菌有广谱的抗菌作用,其临床疗效已经得到一系列Ⅲ期临床研究证明。现对其药理作用、抗菌活性、药动学、临床评价、药物相互作用及药物不良反应等作一综述。

Linezolid is a new class of oxazolidinones antibacterial agents that has been first used in clinical, it inhibits bacterial protein synthesis by blocking the formation of initiation complex. Linezolid has demonstrated antibacterial activity against staphylococci, streptococci, and enterococci in vitro and in vivo, its clinical curative effect has been proved by phase Ⅲ clinical research. This review summarizes the pharmacological mechanism, antibacterial potency, pharmacokinetics, drug-drug interaction, clinical research and side effects of linezolid.