Fass R J, Prior R B
Department of Internal Medicine, Ohio State University College of Medicine, Columbus 43210.
Antimicrob Agents Chemother. 1989 Aug;33(8):1268-74. doi: 10.1128/AAC.33.8.1268.
The in vitro activities of ticarcillin, piperacillin, clavulanic acid, tazobactam, ticarcillin-clavulanate, and piperacillin-tazobactam against 819 bacterial isolates were compared. The two beta-lactamase inhibitors, clavulanic acid and tazobactam, had little useful antibacterial activity but enhanced the activities of the penicillins against beta-lactamase-producing strains of Haemophilus influenzae, Branhamella catarrhalis, and methicillin-susceptible Staphylococcus aureus; all strains were susceptible to both combinations. Both enzyme inhibitors also enhanced the activities of the penicillins against most strains of Escherichia coli, Klebsiella spp., Citrobacter diversus, Proteus spp., Providencia spp., and Bacteroides spp. and against occasional strains of Citrobacter freundii, Enterobacter spp., and Serratia marcescens. Clavulanic acid frequently enhanced the activity of ticarcillin against Xanthomonas maltophilia, and tazobactam frequently enhanced the activity of piperacillin against Morganella morganii. Enhancement was observed primarily with strains relatively resistant to the penicillins. In general, clavulanic acid was more effective than tazobactam in enhancing penicillin activity against Klebsiella spp., C. diversus, X. maltophilia, and Bacteroides spp., whereas tazobactam was more effective against Escherichia coli and Proteeae. There was little or no enhancement of activity against Enterococcus faecalis, Aeromonas hydrophila, Pseudomonas aeruginosa, Pseudomonas cepacia, or Acinetobacter anitratus. Clavulanic acid occasionally antagonized the activity of ticarcillin against ticarcillin-susceptible members of the family Enterobacteriaceae, but those strains were still considered susceptible to the combination. Tazobactam never antagonized the activity of piperacillin. In a direct comparison of the activities of ticarcillin-clavulanate and piperacillin-tazobactam, the two were equally active against H. influenzae, B. catarrhalis, and S. aureus; the latter was more active against E. faecalis. For relatively susceptible strains of members of the family Enterobacteriaceae, neither combination was predictably more active than the other, but relatively resistant strains were generally more susceptible to piperacillin-tazobactam. Piperacillin-tazobactam was more active than ticarcillin-clavulanate against A. hydrophila, P. aeruginosa, and P. cepacia, similar in activity against A. anitratus, and less active against X. maltophilia and Bacteroides spp.
比较了替卡西林、哌拉西林、克拉维酸、他唑巴坦、替卡西林-克拉维酸和哌拉西林-他唑巴坦对819株细菌分离物的体外活性。两种β-内酰胺酶抑制剂，克拉维酸和他唑巴坦，几乎没有有效的抗菌活性，但增强了青霉素对产β-内酰胺酶的流感嗜血杆菌、卡他莫拉菌和甲氧西林敏感金黄色葡萄球菌菌株的活性；所有菌株对这两种组合均敏感。两种酶抑制剂还增强了青霉素对大多数大肠杆菌、克雷伯菌属、奇异枸橼酸杆菌、变形杆菌属、普罗威登斯菌属和拟杆菌属菌株以及偶尔的弗氏枸橼酸杆菌、肠杆菌属和粘质沙雷菌菌株的活性。克拉维酸经常增强替卡西林对嗜麦芽窄食单胞菌的活性，他唑巴坦经常增强哌拉西林对摩根摩根菌的活性。增强主要在对青霉素相对耐药的菌株中观察到。一般来说，克拉维酸在增强青霉素对克雷伯菌属、奇异枸橼酸杆菌、嗜麦芽窄食单胞菌和拟杆菌属的活性方面比他唑巴坦更有效，而他唑巴坦对大肠杆菌和变形杆菌更有效。对粪肠球菌、嗜水气单胞菌、铜绿假单胞菌、洋葱伯克霍尔德菌或鲍曼不动杆菌的活性几乎没有或没有增强。克拉维酸偶尔会拮抗替卡西林对肠杆菌科中对替卡西林敏感成员的活性，但这些菌株仍被认为对该组合敏感。他唑巴坦从未拮抗哌拉西林的活性。在替卡西林-克拉维酸和哌拉西林-他唑巴坦活性的直接比较中，两者对流感嗜血杆菌、卡他莫拉菌和金黄色葡萄球菌的活性相同；后者对粪肠球菌的活性更强。对于肠杆菌科相对敏感的菌株，两种组合的活性均无明显差异，但相对耐药的菌株通常对哌拉西林-他唑巴坦更敏感。哌拉西林-他唑巴坦对嗜水气单胞菌、铜绿假单胞菌和洋葱伯克霍尔德菌的活性比替卡西林-克拉维酸更强，对鲍曼不动杆菌的活性相似，对嗜麦芽窄食单胞菌和拟杆菌属的活性较弱。
