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利奈唑胺(linezolid,PNU-100766)系第一个应用于临床的新型(口恶)唑烷酮类(oxazolidinone)抗菌药,在英、美等国已相继获准上市。利奈唑胺在体内、外对可能引起社区和院内感染的各类革兰阳性球菌均具高度抗菌活性。有关该药治疗社区获得性肺炎、院内获得性肺炎以及皮肤和软组织感染等疾病的一系列Ⅲ期临床实验研究表明,利奈唑胺的临床疗效优于或等同于常规抗菌药物,对甲氧西林耐药葡萄球菌(MRSA)、糖肽类耐药肠球菌、青霉素耐药肺炎链球菌等引起的感染也有显著疗效,而且毒性很小。因利奈唑胺的结构和作用机制独特,故细菌不易对其产生耐药性[1-3]。本文着重综述利奈唑胺的临床研究进展。
Linezolid (linezolid, PNU-100766) is the first new (oral) oxazolidinone antimicrobial used clinically in the United States and other countries. Linezolid has a high degree of antibacterial activity both in vitro and in vivo against a wide range of Gram-positive cocci that may cause community and nosocomial infections. A series of phase III clinical trials of the drug in the treatment of community-acquired pneumonia, nosocomial pneumonia, and skin and soft tissue infections have shown that the clinical efficacy of linezolid is better than or equal to that of conventional antibacterials and that of methicillin- Staphylococcus aureus (MRSA), glycopeptide-resistant enterococci, penicillin-resistant Streptococcus pneumoniae and other infections caused by a significant effect, but little toxicity. Linezolid because of its unique structure and mechanism of action, so the bacteria are not easy to produce resistance [1-3]. This article focuses on the clinical research progress of linezolid.