中文摘要：

利奈唑胺是第一个嘿唑烷酮类抗菌药物，通过与细菌核糖体50S亚单位作用，抑制起始复合物的形成，而抑制细菌蛋白质合成。对葡萄球菌、链球菌、肠球菌等革兰阳性菌有很强的抗菌作用。目前，国内外已出现耐药葡萄球菌，耐药情况且呈上升趋势，特别是凝固酶阴性的葡萄球菌值得重视。耐药机制主要是细菌核糖体23SrRNA第v功能区基因突变，CFR基因的获得，编码50S核糖体蛋白L3、L4、L22的rpIC、rpID、rpIV的基因突变，23SrRNA修饰改变导致的耐药，LmrS多药外排泵，ABC蛋白过度表达等。

英文摘要：

Linezolid is the first oxazolidinone antibiotic. It inhibits protein synthesis through binding to the 50S ribosomal subunit and imperiling the formation of initial complex. It has antibacterial function to many Grmn-positive bacteria, including Staphylococci, Streptococci and Enterococci. Now, the Staphylococci resistant to Linezolid have been reported all over the world and the trend of resistance is increasing, especially for coagulase- negative Staphylococci. The resismlace mechanisms have been mainly characterized： mutations in the domain V region of 23S rRNA genes, acquisition of the ribosomal methyltransferase gene CFR, mutations in the rplC, rpID, rplV gene encoding the 50S ribosomal protein L3, L4, L22 modifications of 23S rRNA multidrug efftux pump LmrS and overexpression of an ABC transporter and so on.