Perry C M, Jarvis B
Adis International Limited, Auckland, New Zealand.
Drugs. 2001;61(4):525-51. doi: 10.2165/00003495-200161040-00008.
Linezolid is the first of a new class of antibacterial drugs, the oxazolidinones. It has inhibitory activity against a broad range of gram-positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA), glycopeptide-intermediate S. aureus (GISA), vancomycin-resistant enterococci (VRE) and penicillin-resistant Streptococcus pneumoniae. The drug also shows activity against certain anaerobes, including Clostridium perfringens, C. difficile, Peptostreptococcus spp. and Bacteroidesfragilis. In controlled phase III studies, linezolid was as effective as vancomycin in the treatment of patients with infections caused by methicillin-resistant staphylococci and also demonstrated efficacy against infections caused by VRE. Further phase III studies have demonstrated that linezolid is an effective treatment for patients with nosocomial pneumonia, for hospitalised patients with community-acquired pneumonia, and for patients with complicated skin or soft tissue infections (SSTIs). In these studies, linezolid was as effective as established treatments, including third-generation cephalosporins in patients with pneumonia, and oxacillin in patients with complicated SSTIs. Oral linezolid 400 or 600mg twice daily was as effective as clarithromycin 250mg twice daily or cefpodoxime proxetil 200mg twice daily in the treatment of patients with uncomplicated SSTIs or community-acquired pneumonia. Linezolid is a generally well tolerated drug. The most frequently reported adverse events in linezolid recipients were diarrhoea, headache, nausea and vomiting. Thrombocytopenia was also documented in a small proportion (about 2%) of patients treated with the drug.
Linezolid has good activity against gram-positive bacteria, particularly multidrug resistant strains of S. aureus (including GISA), Enterococcus faecium and E. faecalis (including VRE). In controlled clinical trials, linezolid was as effective as vancomycin in eradicating infections caused by methicillin-resistant Staphylococcus spp. and has demonstrated efficacy against infections caused by VRE. As the level of resistance to vancomycin increases among S. aureus and enterococci, linezolid is poised to play an important role in the management of serious gram-positive infections.
利奈唑胺是新型抗菌药物恶唑烷酮类中的首个药物。它对多种革兰氏阳性菌具有抑制活性，包括耐甲氧西林金黄色葡萄球菌（MRSA）、糖肽中介金黄色葡萄球菌（GISA）、耐万古霉素肠球菌（VRE）以及耐青霉素肺炎链球菌。该药物对某些厌氧菌也有活性，包括产气荚膜梭菌、艰难梭菌、消化链球菌属以及脆弱拟杆菌。在对照的III期研究中，利奈唑胺在治疗耐甲氧西林葡萄球菌引起的感染方面与万古霉素疗效相当，并且对VRE引起的感染也显示出疗效。进一步的III期研究表明，利奈唑胺对医院获得性肺炎患者、社区获得性肺炎住院患者以及复杂性皮肤或软组织感染（SSTIs）患者是一种有效的治疗药物。在这些研究中，利奈唑胺与既定治疗方法疗效相当，在肺炎患者中与第三代头孢菌素相当，在复杂性SSTIs患者中与苯唑西林相当。每日两次口服400或600mg利奈唑胺在治疗非复杂性SSTIs或社区获得性肺炎患者时与每日两次口服250mg克拉霉素或每日两次口服200mg头孢泊肟酯疗效相当。利奈唑胺是一种总体耐受性良好的药物。接受利奈唑胺治疗的患者中最常报告的不良事件是腹泻、头痛、恶心和呕吐。在一小部分（约2%）接受该药物治疗的患者中也记录到了血小板减少症。
利奈唑胺对革兰氏阳性菌，特别是金黄色葡萄球菌（包括GISA）、粪肠球菌和屎肠球菌（包括VRE）的多重耐药菌株具有良好活性。在对照临床试验中，利奈唑胺在根除耐甲氧西林葡萄球菌属引起的感染方面与万古霉素疗效相当，并且对VRE引起的感染也显示出疗效。随着金黄色葡萄球菌和肠球菌对万古霉素的耐药水平增加，利奈唑胺在严重革兰氏阳性感染的管理中有望发挥重要作用。
