Matsubara N, Minami S, Muraoka T, Saikawa I, Mitsuhashi S
Antimicrob Agents Chemother. 1979 Dec;16(6):731-5. doi: 10.1128/AAC.16.6.731.
Cefoperazone, a new semisynthetic cephalosporin, has a broad spectrum of antibacterial activity. It is as active as cefazolin and cefamandole against gram-positive bacteria and is more active than cefazolin and cefamandole against such gram-negative bacilli as Escherichia coli, Klebsiella pneumoniae, Proteus species, Pseudomonas aeruginosa, Citrobacter freundii, Enterobacter cloacae, and Serratia marcescens. The superiority of cefoperazone over cefazolin and cefamandole with respect to activity against P. aeruginosa by more than 200-fold was especially remarkable. As with other beta-lactam antibiotics, there was only a small spread between the minimum inhibitory concentrations and the minimum bactericidal concentrations of cefoperazone and a significant decrease in activity with an increase in inoculum size. Activity was not altered significantly by the addition of human serum to the test medium. Cefoperazone is relatively stable to hydrolysis to beta-lactamases produced by gram-negative bacteria. Relative rates of hydrolysis of cefoperazone by cephalosporinases are 7.0 to 0.01, with reference to cephaloridine hydrolysis (base, 100). Cefoperazone is also more stable than penicillin G and cephaloridine to various types of penicillinases.
头孢哌酮是一种新型半合成头孢菌素,具有广谱抗菌活性。它对革兰氏阳性菌的活性与头孢唑林和头孢孟多相当,而对大肠杆菌、肺炎克雷伯菌、变形杆菌属、铜绿假单胞菌、弗氏柠檬酸杆菌、阴沟肠杆菌和粘质沙雷氏菌等革兰氏阴性杆菌的活性比头孢唑林和头孢孟多更强。头孢哌酮对铜绿假单胞菌的活性比头孢唑林和头孢孟多高出200多倍,这一优势尤为显著。与其他β-内酰胺类抗生素一样,头孢哌酮的最低抑菌浓度和最低杀菌浓度之间差异很小,且随着接种量的增加活性显著降低。向测试培养基中添加人血清后,活性没有明显改变。头孢哌酮对革兰氏阴性菌产生的β-内酰胺酶水解相对稳定。以头孢菌素酶水解头孢哌酮的相对速率为7.0至0.01,以头孢噻啶水解(碱,100)为参照。头孢哌酮对各种类型的青霉素酶也比青霉素G和头孢噻啶更稳定。