SK&F 75073，一种新型肠胃外使用的广谱头孢菌素，血清浓度高且持续时间长。
SK&F 75073, new parenteral broad-spectrum cephalosporin with high and prolonged serum levels.
作者信息
Actor P, Uri J V, Zajac I, Guarini J R, Phillips L, Pitkin D H, Berges D A, Dunn G L, Hoover J R, Weisbach J A
出版信息
Antimicrob Agents Chemother. 1978 May;13(5):784-90. doi: 10.1128/AAC.13.5.784.
Abstract
SK&F 75073, a new parenteral cephalosporin, was found to have broad in vitro and in vivo antibacterial activity including isolates usually resistant to cephalothin and cefazolin. This activity included indole-positive Proteus and Enterobacter species and some Serratia isolates. Proteus mirabilis strains were particularly susceptible, as were Haemophilus influenzae and Neisseria species. The activity of SK&F 75073 against gram-positive bacteria was poorer than that of the control cephalosporins. This cephalosporin is highly bound to serum proteins, and a loss in in vitro activity was observed in the presence of serum. Parenteral administration of SK&F 75073 to experimental animals (mice, dogs, squirrel monkeys) resulted in high and prolonged serum levels when compared with cefazolin and other injectable cephalosporins. This favorable serum profile was reflected in the excellent protection observed in mice infected with pathogenic bacteria.
摘要
SK&F 75073是一种新型胃肠外用头孢菌素，体外和体内均有广泛抗菌活性，包括通常对头孢噻吩和头孢唑林耐药的菌株。这种活性包括吲哚阳性变形杆菌和肠杆菌属菌种以及一些沙雷氏菌属分离株。奇异变形杆菌菌株尤其敏感，流感嗜血杆菌和奈瑟菌属菌种也是如此。SK&F 75073对革兰氏阳性菌的活性比对照头孢菌素差。这种头孢菌素与血清蛋白高度结合，在有血清存在时观察到体外活性丧失。与头孢唑林和其他注射用头孢菌素相比，给实验动物（小鼠、狗、松鼠猴）胃肠外注射SK&F 75073会导致血清水平升高且持续时间长。这种良好的血清特征反映在感染病原菌的小鼠中观察到的极佳保护作用上。
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