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Med Monatsschr Pharm. 2015 Jan;38(1):4-11.
Fosfomycin is a bactericidal phosphonic acid derivative, which engages by inhibiting pyruvyltransferase at an early stage in the peptidoglycan synthesis. It shows a broad spectrum of activity that includes many multidrug-resistant gram-negative and gram-positive bacteria. Fosfomycin is active against most strains of Pseudomonas aeruginosa and several multidrug-resistant Enterobacteriaceae, e.g., Escherichia coli strains expressing extended spectrum beta-lactamases (ESBL) and Klebsiella pneumoniae strains with decreased susceptibilities to carbapenems. Most methicillin-resistant Staphylococcus aureus (MRSA) strains as well as enterococci with and without vancomycin resistance are also sensitive to fosfomycin. During the last decade, a variety of studies showed that fosfomycin is not only suitable for treating uncomplicated urinary tract diseases, but also for the treatment of many other diseases caused by bacterial pathogens with and without multidrug resistance. However, large controlled studies demonstrating the efficacy of the drug to treat diseases caused by multidrug-resistant bacteria are still missing. Considering the low number of antibacterial agents with good activity against multidrug-resistant bacteria, fosfomycin should be evaluated as an important antibiotic for the treatment of several severe illnesses due to these pathogens. However, because some multidrug-resistant bacteria are also resistant to fosfomycin, this agent should only be applied if the pathogen is sensitive to this drug. In addition, because rapid development of resistance cannot be excluded if fosfomycin will be applied alone, this drug should only be given in combination with other effective drugs for the treatment of serious systemic diseases due to multidrug-resistant bacterial pathogens.
磷霉素是一种杀菌性膦酸衍生物,它通过在肽聚糖合成的早期抑制丙酮酸转移酶来发挥作用。它具有广泛的活性谱,包括许多耐多药革兰氏阴性菌和革兰氏阳性菌。磷霉素对大多数铜绿假单胞菌菌株以及几种耐多药肠杆菌科细菌具有活性,例如表达超广谱β-内酰胺酶(ESBL)的大肠杆菌菌株和对碳青霉烯类药物敏感性降低的肺炎克雷伯菌菌株。大多数耐甲氧西林金黄色葡萄球菌(MRSA)菌株以及有或没有耐万古霉素的肠球菌对磷霉素也敏感。在过去十年中,各种研究表明,磷霉素不仅适用于治疗单纯性泌尿系统疾病,还适用于治疗由有或没有耐多药的细菌病原体引起的许多其他疾病。然而,仍缺乏大型对照研究来证明该药物治疗耐多药细菌引起的疾病的疗效。考虑到对耐多药细菌具有良好活性的抗菌剂数量较少,磷霉素应被评估为治疗由这些病原体引起的几种严重疾病的重要抗生素。然而,由于一些耐多药细菌也对磷霉素耐药,只有在病原体对该药物敏感时才应使用这种药物。此外,由于单独使用磷霉素不能排除耐药性的快速产生,因此该药物仅应与其他有效药物联合使用,以治疗由耐多药细菌病原体引起的严重全身性疾病。