Fu K P, Neu H C
Antimicrob Agents Chemother. 1978 Mar;13(3):358-67. doi: 10.1128/AAC.13.3.358.
The in vitro activity of piperacillin, a new semisynthetic piperazine penicillin derivative, was evaluated against 626 clinical isolates and compared with the activity of other beta-lactam antibiotics. At a concentration of 0.1 microgram/ml, piperacillin inhibited all streptococci except enterococci. Non-beta-lactamase-producing staphylococci were inhibited by 1.6 microgram or less per ml. Both beta-lactamase- and non-beta-lactamase-producing Haemophilus were inhibited by 0.1 microgram/ml. Piperacillin inhibited non-beta-lactamase-producing Escherichia coli, Salmonella, and Shigella at a concentration of 6.3 micrograms/ml, but 20% of strains of these species containing type III beta-lactamase were not inhibited by 100 micrograms/ml. Piperacillin at 25 micrograms/ml, inhibited 83% of Citrobacter, 58% of Klebsiella, 88% of Enterobacter, and 50% of indole-positive Proteus, Acinetobacter, and Providencia. At 25 micrograms/ml, piperacillin inhibited 95% of Pseudomonas aeruginosa and 78% of Bacteroides fragilis. The minimal inhibitory concentration of piperacillin against Pseudomonas was affected by increasing the inoculum size and by pH. Minimum bactericidal concentrations against Pseudomonas and Serratia often were eightfold greater than the minimum inhibitory concentrations. Piperacillin was equal in activity to ampicillin against enterococci. It was more active than carbenicillin against E. coli, Klebsiella, Enterobacter, and Bacteroides. It was the most active penicillin against Pseudomonas and inhibited many strains of Pseudomonas for which the MICs of carbenicillin were above 200 micrograms/ml. Piperacillin was hydrolyzed by many different beta-lactamases. Synergistic activity of piperacillin was demonstrated when it was combined with amikacin, gentamicin, and cefazolin against P. aeruginosa and members of the Enterobacteriaceae. No antagonism was observed when piperacillin was combined with aminoglycosides; however, antagonism was observed rarely against E. coli when piperacillin was combined with cefazolin.
哌拉西林是一种新型半合成哌嗪青霉素衍生物,对其体外活性进行了评估,以626株临床分离菌为研究对象,并与其他β-内酰胺类抗生素的活性进行比较。在浓度为0.1微克/毫升时,哌拉西林抑制除肠球菌外的所有链球菌。每毫升1.6微克或更低浓度可抑制不产β-内酰胺酶的葡萄球菌。产β-内酰胺酶和不产β-内酰胺酶的嗜血杆菌均被0.1微克/毫升的哌拉西林抑制。哌拉西林在浓度为6.3微克/毫升时抑制不产β-内酰胺酶的大肠杆菌、沙门氏菌和志贺氏菌,但这些菌种中含Ⅲ型β-内酰胺酶的菌株有20%在100微克/毫升时未被抑制。25微克/毫升的哌拉西林可抑制83%的柠檬酸杆菌、58%的克雷伯菌、88%的肠杆菌以及50%的吲哚阳性变形杆菌、不动杆菌和普罗威登斯菌。在25微克/毫升时,哌拉西林抑制95%的铜绿假单胞菌和78%的脆弱拟杆菌。哌拉西林对假单胞菌的最低抑菌浓度受接种量增加和pH值影响。对假单胞菌和沙雷氏菌的最低杀菌浓度通常比最低抑菌浓度高八倍。哌拉西林对肠球菌的活性与氨苄西林相当。它对大肠杆菌、克雷伯菌、肠杆菌和拟杆菌的活性比羧苄西林更强。它是对假单胞菌活性最强的青霉素,可抑制许多羧苄西林最低抑菌浓度高于200微克/毫升的假单胞菌菌株。哌拉西林可被多种不同的β-内酰胺酶水解。哌拉西林与阿米卡星、庆大霉素和头孢唑林联合应用时,对铜绿假单胞菌和肠杆菌科细菌显示出协同活性。哌拉西林与氨基糖苷类联合应用时未观察到拮抗作用;然而,哌拉西林与头孢唑林联合应用时,对大肠杆菌很少观察到拮抗作用。