Bozdogan Bülent, Appelbaum Peter C
Department of Pathology, Penn State University Hershey Medical Center, H083, 500 University Drive, PO Box 850 Hershey, PA 17033, USA.
Int J Antimicrob Agents. 2004 Feb;23(2):113-9. doi: 10.1016/j.ijantimicag.2003.11.003.
Oxazolidinones are a new group of antibiotics. These synthetic drugs are active against a large spectrum of Gram-positive bacteria, including methicillin- and vancomycin-resistant staphylococci, vancomycin-resistant enterococci, penicillin-resistant pneumococci and anaerobes. Oxazolidinones inhibit protein synthesis by binding at the P site at the ribosomal 50S subunit. Resistance to other protein synthesis inhibitors does not affect oxazolidinone activity, however rare development of oxazolidinone resistance cases, associated with 23S rRNA alterations during treatment have been reported. Linezolid, the first oxazolidinone available, has already taken its place in the clinic for treatment of Gram-positive infections. Pharmacokinetic properties as well as its good penetration and accumulation in the tissue including bone, lung, vegetations, haematoma and cerebrospinal fluid, allow its use for surgical infections.
恶唑烷酮类是一类新型抗生素。这些合成药物对多种革兰氏阳性菌具有活性,包括耐甲氧西林和耐万古霉素的葡萄球菌、耐万古霉素的肠球菌、耐青霉素的肺炎球菌和厌氧菌。恶唑烷酮类通过与核糖体50S亚基的P位点结合来抑制蛋白质合成。对其他蛋白质合成抑制剂的耐药性并不影响恶唑烷酮类的活性,不过已有报道称,在治疗期间出现了罕见的与23S rRNA改变相关的恶唑烷酮类耐药病例。利奈唑胺是首个可用的恶唑烷酮类药物,已在临床上用于治疗革兰氏阳性菌感染。其药代动力学特性以及在包括骨骼、肺、赘生物、血肿和脑脊液在内的组织中的良好渗透和蓄积,使其可用于外科感染的治疗。