利奈唑胺及其耐药机制研究  

Study of linezolid and its resistance mechanism

作　　者：辛小娟[1] 黄文祥[1] 李佳俊[1] 

机构地区：[1]重庆医科大学附属第一医院,重庆400016

出　　处：《中国抗生素杂志》2013年第6期411-414,429,共5页Chinese Journal of Antibiotics

摘　　要：利奈唑胺通过抑制蛋白起始复合物的形成而抑制细菌蛋白质的合成,在体内外对革兰阳性菌,如葡萄球菌、链球菌、肠球菌等耐药菌有广谱的抗菌效果,以治疗此类细菌引起的感染。但是,近年来,由于利奈唑胺广泛用于临床、以及一定程度的滥用,国内外已发现对其耐药的葡萄球菌、肠球茵等临床耐药株。其耐药机制主要由细菌单个碱基突变和甲基转移酶的产生所介导,当然,另外一些耐药机制尚不明了。目前虽然细菌耐利奈唑胺的情况并不严重,但应该引起我们足够的重视。Linezolid is the first licenced oxazolidinone antibiotic for clinical treatment which has universal antibacterial activity both in vitro and in vivo against Gram-positive bacteria such as Staphylococcus aureus, Streptococcus, Enterococcus. It can inhibit bacterial protein synthesis by inhibiting protein amine starting complex formation. Nevertheless, with the increased wide use of linezolid and the abuse in some degree in clinical in recent years, we have found some clinical resistant strains to linezolid worldwide such as Staphylococcus aureus, Enterococcus. The mechanisms of resistance are mainly due to a single base mutation of bacteria and the generation of methyltransferase. Besides, other mechanisms of resistance are still unknown. Although it is not a very serious situation of bacterial resistance to linezolid at present, we should pay enough attention to it.

关 键 词：利奈唑胺 抗菌活性 利奈唑胺耐药 耐药机制 靶位突变 甲基转移酶 

分 类 号：R978.1[医药卫生—药品]