Nakamura T, Hashimoto I, Sawada Y, Mikami J, Bekki E
Jpn J Antibiot. 1985 Aug;38(8):2057-67.
Fosfomycin (FOM) is a synthetic antibiotic having a unique structural formula and bactericidal mechanism and a broad spectrum of antimicrobial activity against various bacterial species. It has higher activity in vivo than in vitro. As therapy, FOM-Na in a daily dose of 4 g (2 g X 2) was given by intravenous drip infusion for 5 to 10 days to 6 cases with infectious diseases (2 cases of acute cholecystitis, 3 cases of acute localized peritonitis due to phlegmonous appendicitis and 1 case of acute diffuse peritonitis due to perforative appendicitis). The clinical response was rated as "excellent" in 1 case, "good" in 4 cases, "fair" in 1 case and "poor" in none. No adverse effects were observed in any of the patients. Six clinical isolates were obtained, and these consisted of 4 strains of Escherichia coli and 1 strain each of Klebsiella pneumoniae, and Bacteroides fragilis. The MICs of FOM were from 6.25 to 12.5 micrograms/ml for E. coli, 50 micrograms/ml for K. pneumoniae, and 100 micrograms/ml for B. fragilis. FOM-Na was administered to the 6 cases intravenously in a dose of 2 g before surgery, and tissue specimens and body fluid samples were taken during the operation. The FOM concentration was determined by bioassay with a Proteus sp. (MB 838) as the test organism. The mean FOM concentration in bile from the common bile duct was 61.85 +/- 17.13 micrograms/ml (n = 5) at 95 to 108 minutes after FOM-Na intravenous bolus injection. The mean FOM concentration in the gall bladder bile was 80.06 +/- 92.36 micrograms/ml, while that in the gall bladder wall was 146.65 +/- 39.10 micrograms/g. The mean FOM concentration in purulent ascites was 58.20 +/- 13.29 micrograms/ml, 36.22 +/- 14.63 micrograms/g in the appendix wall and 12.64 +/- 11.34 micrograms/ml in pus in the appendix. The FOM concentrations in the infected tissues and body fluids thus exceeded the MICs of FOM for the pathogenic bacteria. Therefore, FOM-Na appears to be a very useful drug when used for chemotherapy of infections encountered in the surgical field.
磷霉素（FOM）是一种具有独特结构式和杀菌机制的合成抗生素，对多种细菌具有广谱抗菌活性。它在体内的活性高于体外。作为治疗方法，对6例传染病患者（2例急性胆囊炎、3例蜂窝织炎性阑尾炎所致急性局限性腹膜炎、1例穿孔性阑尾炎所致急性弥漫性腹膜炎）静脉滴注给予每日剂量4g（2g×2）的磷霉素钠，持续5至10天。临床反应评定为“优”1例，“良”4例，“中”1例，无“差”的病例。所有患者均未观察到不良反应。获得6株临床分离菌，其中包括4株大肠杆菌、1株肺炎克雷伯菌和1株脆弱拟杆菌。磷霉素对大肠杆菌的MIC为6.25至12.5微克/毫升，对肺炎克雷伯菌为50微克/毫升，对脆弱拟杆菌为100微克/毫升。对这6例患者在手术前静脉给予2g剂量的磷霉素钠，并在手术期间采集组织标本和体液样本。以变形杆菌属（MB 838）作为测试菌通过生物测定法测定磷霉素浓度。在静脉推注磷霉素钠后95至108分钟，胆总管胆汁中磷霉素的平均浓度为61.85±17.
