Goering R V, Sanders C C, Sanders W
J Antibiot (Tokyo). 1978 Apr;31(4):363-72. doi: 10.7164/antibiotics.31.363.
The activity of BL-S786 was compared to that of cephalothin, cefamandole and cefoxitin in vitro and in treatment of experimental infections in mice. In broth dilution tests, the activity of BL-S786 was less than cephalothin or cefamandole against Staphylococcus aureus and less than cefamandole or cefoxitin against Haemophilus influenzae. BL-S786 and cefamandole were the two most active drugs against cephalothin-sensitive Enterobacteriaceae. In tests with cephalothin-resistant Enterobacteriaceae, BL-S786 was generally less active than cefamandole but more active than cefoxitin against all strains except Proteus and Providencia. Regardless of the comparative in vitro activity of the four drugs, BL-S786 was the most effective drug in treatment of mice lethally infected with Enterobacteriaceae. Protection from lethality was associated with clearance of bacteremia by each of the four drugs. In several tests where in vitro activity was not predictive of in vivo efficacy, selection of resistance in vivo was found to have occurred.
在体外以及对小鼠实验性感染的治疗中,将BL - S786的活性与头孢噻吩、头孢孟多和头孢西丁进行了比较。在肉汤稀释试验中,BL - S786对金黄色葡萄球菌的活性低于头孢噻吩或头孢孟多,对流感嗜血杆菌的活性低于头孢孟多或头孢西丁。BL - S786和头孢孟多是对头孢噻吩敏感的肠杆菌科细菌活性最强的两种药物。在对头孢噻吩耐药的肠杆菌科细菌进行的试验中,除变形杆菌和普罗威登斯菌外,BL - S786对所有菌株的活性一般低于头孢孟多,但高于头孢西丁。无论这四种药物在体外的活性比较如何,BL - S786都是治疗被肠杆菌科细菌致死性感染小鼠最有效的药物。对致死性的保护与这四种药物各自清除菌血症有关。在一些体外活性无法预测体内疗效的试验中,发现体内出现了耐药性选择。