Modak S M, Fox C L
Arch Surg. 1981 Jul;116(7):854-7. doi: 10.1001/archsurg.1981.01380190006002.
Sulfadiazine silver-resistant strains of Pseudomonas aeruginosa isolated from burned patients from several countries are sensitive to sulfadiazine silver in vitro, but in burned mice and rats resist topical therapy with sulfadiazine silver. In searching for an effective topical agent against these resistant organisms, we found that FPQC (1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7[1-piperazinyl]-quinoline-carboxylic acid) and its silver salt are effective both in vitro and in vivo. In vitro, their minimal inhibitory concentrations are ten to 20 times lower than that of sulfadiazine silver. In burned mice infected with resistant Pseudomonas strains, mortality in groups receiving topical therapy with FPQC or FPQC silver is 0%, but 80% to 100% with sulfadiazine silver and 100% without treatment. Similar results were obtained in burned rats. The efficacy of FPQC and FPQC silver in vivo may represent discovery of new agents of known low toxicity that are useful in topical burn therapy.
从几个国家的烧伤患者中分离出的对磺胺嘧啶银耐药的铜绿假单胞菌菌株,在体外对磺胺嘧啶银敏感,但在烧伤小鼠和大鼠中对磺胺嘧啶银局部治疗耐药。在寻找针对这些耐药菌的有效局部用药时,我们发现FPQC(1-乙基-6-氟-1,4-二氢-4-氧代-7-[1-哌嗪基]-喹啉羧酸)及其银盐在体外和体内均有效。在体外,它们的最小抑菌浓度比磺胺嘧啶银低10至20倍。在感染耐药铜绿假单胞菌菌株的烧伤小鼠中,接受FPQC或FPQC银局部治疗的组死亡率为0%,但接受磺胺嘧啶银治疗的组死亡率为80%至100%,未治疗组死亡率为100%。在烧伤大鼠中也获得了类似结果。FPQC和FPQC银在体内的疗效可能代表发现了已知低毒性的新型药物,可用于烧伤局部治疗。