Wilcox Mark H
Department of Microbiology, University of Leeds and The General Infirmary, Leeds LS2 9JT, UK.
J Antimicrob Chemother. 2003 May;51 Suppl 2:ii27-35. doi: 10.1093/jac/dkg251.
Treatment of Gram-positive bacterial infections is currently a therapeutic challenge because many of these pathogens are now resistant to standard antimicrobial agents. The emergence of multidrug-resistant, Gram-positive pathogens emphasizes the need for new antimicrobial therapy. Linezolid is an oxazolidinone antibiotic with a novel mechanism of action that works by inhibiting bacterial protein synthesis by blocking formation of the initiation complex. It is active against Gram-positive organisms resistant to other antibiotics, including methicillin-resistant Staphylococcus aureus (MRSA), penicillin-resistant Streptococcus pneumoniae and vancomycin-resistant enterococci (VRE). Results are encouraging from several large-scale, randomized, Phase III trials comparing the efficacy and safety of linezolid with standard comparator agents for the treatment of nosocomial pneumonia, community-acquired pneumonia, skin and skin structure infections, and infections due to MRSA and VRE. Intravenous/oral linezolid is a promising antimicrobial agent and provides the clinician with an additional treatment option, particularly among the limited therapies for resistant Gram-positive bacterial infections.
目前，革兰氏阳性菌感染的治疗是一项治疗挑战，因为许多这类病原体现在对标准抗菌药物具有耐药性。多重耐药革兰氏阳性病原体的出现凸显了新型抗菌疗法的必要性。利奈唑胺是一种恶唑烷酮类抗生素，其作用机制新颖，通过阻断起始复合物的形成来抑制细菌蛋白质合成。它对耐其他抗生素的革兰氏阳性菌有效，包括耐甲氧西林金黄色葡萄球菌（MRSA）、耐青霉素肺炎链球菌和耐万古霉素肠球菌（VRE）。几项大规模、随机、III期试验比较了利奈唑胺与标准对照药物治疗医院获得性肺炎、社区获得性肺炎、皮肤及皮肤结构感染以及由MRSA和VRE引起的感染的疗效和安全性，结果令人鼓舞。静脉注射/口服利奈唑胺是一种很有前景的抗菌药物，为临床医生提供了额外的治疗选择，尤其是在耐药革兰氏阳性菌感染的有限治疗方法中。
