Chpt 43中 Macrolides, Lincomycins and Vancomycins.pptVIP

红霉素（erythromycin） Fig. 43-1.Mechanism of action of macrolide antibiotics 红霉素（erythromycin） Ⅴ . Linezolid 利奈唑胺 Linezolid was the first commercially available oxazolidinone噁唑烷酮antibiotic. Therapy using linezolid can be quite expensive, with prices for a course of treatment ranging up to several thousands of dollars; nonetheless, it appears to be more cost-effective than vancomycin or teicoplanin. Upjohn developed linezolid (Upjohn is now part of Pfizer) and Food and Drug Administration (FDA) approval was granted in April 2000. Mechanism of action Linezolid works on the initiation of protein synthesis. It does this by stopping the 30S and 50S subunits of the ribosome from binding together. Linezolid binds on the 23S portion of the 50S subunit close to the peptidyl transferase and chloramphenicol binding sites. This then stops the interaction with the 30S subunit. Clinical uses It is usually reserved for the treatment of serious bacterial infections where older antibiotics have failed due to antibiotic resistance. Conditions such as skin infections or nosocomial 医院的 pneumonia where methicillin or penicillin resistance is found are indicators for linezolid use. Linezolid is effective against Gram-positive pathogens, notably Enterococcus faecium 屎肠球菌, Staphylococcus aureus, Streptococcus agalactiae无乳, Streptococcus pneumoniae, and Streptococcus pyogenes化脓. It has almost no effect on gram-negative bacteria and is only bacteriostatic against most Enterococcus species. Linezolid also provides some anaerobic coverage. Rapid intravenous infusion may cause a variety of symptoms, including erythematous(红斑) or urticarial(风疹) reactions, flushing, tachycardia, and hypotension. The extreme flushing that can occur is sometimes called red-neck or redman syndrome. Adverse Reactions Vancomycin (2) Ototoxicity is associated with excessively high concentrations. (3) Nephrotoxic