Grunberg E, Cleeland R, Beskid G, DeLorenzo W F
Antimicrob Agents Chemother. 1976 Apr;9(4):589-94. doi: 10.1128/AAC.9.4.589.
Both an oral and a parenteral form of a 6beta-amidinopenicillanic acid derivative were found to have appreciable activity against gram-negative bacteria and poor activity against gram-positive bacteria in vivo. When administered orally or parenterally, definite synergy was demonstrated between the amidinopenicillins and ampicillin, amoxicillin, benzylpenicillin, cefazolin, or carbenicillin in infections with a number of gram-negative bacteria, including Klebsiella, Enterobacter, Escherichia, Proteus, Salmonella, and Haemophilus species in mice. Synergy was also observed between the parenteral amidinopenicillin and benzylpenicillin in the Staphylococcus aureus infection but not in infections with other gram-positive organisms. No synergy was demonstrated between the parenteral amidinopenicillin and erythromycin or oxytetracycline in infections with gram-positive or gram-negative organisms. Synergy between the parenteral amidinopenicillin and gentamicin was observed only in the case of Escherichia coli.
研究发现,一种6β-脒基青霉烷酸衍生物的口服和肠胃外给药形式在体内对革兰氏阴性菌均具有显著活性,而对革兰氏阳性菌的活性较差。当口服或肠胃外给药时,在感染多种革兰氏阴性菌(包括小鼠体内的克雷伯菌属、肠杆菌属、大肠杆菌、变形杆菌、沙门氏菌和嗜血杆菌属)的情况下,脒基青霉素与氨苄西林、阿莫西林、苄青霉素、头孢唑林或羧苄青霉素之间表现出明确的协同作用。在金黄色葡萄球菌感染中,肠胃外脒基青霉素与苄青霉素之间也观察到协同作用,但在其他革兰氏阳性菌感染中未观察到。在革兰氏阳性菌或革兰氏阴性菌感染中,肠胃外脒基青霉素与红霉素或土霉素之间未表现出协同作用。仅在大肠杆菌感染的情况下观察到肠胃外脒基青霉素与庆大霉素之间的协同作用。