Watanabe Y, Minami S, Yotsuji A, Araki H, Yasuda T, Saikawa I
Jpn J Antibiot. 1983 Dec;36(12):3437-43.
The in vitro antibacterial activities of cefoperazone (CPZ) against clinical isolates including various beta-lactamase-producing strains were studied and compared with those of cefotiam (CTM). CPZ had a broad spectrum against Gram-negative and Gram-positive bacteria. Especially, CPZ showed apparently more potent antibacterial activities than CTM against Enterobacter cloacae, Serratia marcescens, and Pseudomonas aeruginosa. However, CPZ was less active than CTM against Staphylococcus aureus and Proteus mirabilis. The stability and affinity of CPZ for various types of beta-lactamase were also studied. CPZ was more resistant to hydrolysis by typical cephalosporinase (CSase) and cefuroximase (CXase) than CTM, but was less stable to penicillinase (PCase). CPZ often showed higher affinity to beta-lactamases than CTM. The study for the inducer-activity revealed that CPZ hardly induced CSase production in E. cloacae and Proteus vulgaris while CTM highly induced in both strains. CPZ was more active against CSase-producers than CTM, especially against strains which inducibly produced the enzyme. It was speculated that this activity was responsible for the superior stability to CSase and low inducer-activity for CSase production.
研究了头孢哌酮(CPZ)对包括各种产β-内酰胺酶菌株在内的临床分离株的体外抗菌活性,并与头孢替安(CTM)进行了比较。CPZ对革兰氏阴性菌和革兰氏阳性菌具有广谱抗菌活性。特别是,CPZ对阴沟肠杆菌、粘质沙雷氏菌和铜绿假单胞菌的抗菌活性明显比CTM更强。然而,CPZ对金黄色葡萄球菌和奇异变形杆菌的活性低于CTM。还研究了CPZ对各种类型β-内酰胺酶的稳定性和亲和力。CPZ比CTM更耐典型的头孢菌素酶(CSase)和头孢呋辛酶(CXase)水解,但对青霉素酶(PCase)的稳定性较差。CPZ对β-内酰胺酶的亲和力通常高于CTM。诱导活性研究表明,CPZ在阴沟肠杆菌和普通变形杆菌中几乎不诱导CSase产生,而CTM在这两种菌株中均高度诱导。CPZ对产CSase的菌株比CTM更具活性,尤其是对可诱导产生该酶的菌株。据推测,这种活性是其对CSase具有卓越稳定性和对CSase产生低诱导活性的原因。