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β-内酰胺酶抑制剂YTR 830、克拉维酸和舒巴坦与广谱青霉素联合应用对耐替卡西林肠杆菌科细菌和假单胞菌的比较活性

Comparative activities of the beta-lactamase inhibitors YTR 830, clavulanate and sulbactam combined with extended-spectrum penicillins against ticarcillin-resistant Enterobacteriaceae and pseudomonads.

作者信息

Jacobs M R, Aronoff S C, Johenning S, Yamabe S

出版信息

J Antimicrob Chemother. 1986 Aug;18(2):177-84. doi: 10.1093/jac/18.2.177.

Abstract

The in-vitro synergistic activity of YTR 830, a new beta-lactamase inhibitor, combined with four extended-spectrum penicillins (ticarcillin, piperacillin, mezlocillin and apalcillin) against ticarcillin-resistant clinical isolates of Gram-negative enteric bacilli was compared with that of clavulanate and sulbactam. Synergy testing was performed with fixed concentrations of beta-lactamase inhibitors (8 mg/l) combined with doubling dilutions of beta-lactams in microdilution trays. Synergy was defined as a four-fold or greater decrease of beta-lactam MIC in the combination compared with the beta-lactam alone. For 79 ticarcillin-resistant Enterobacteriaceae, ticarcillin-YTR 830 and ticarcillin-clavulanate were synergistic against 90% of strains; for ticarcillin-sulbactam, 70% showed synergy. The synergistic activity of all three inhibitors was similar against strains resistant only to ticarcillin; for strains resistant to all four extended-spectrum penicillins, the activity of ticarcillin with YTR 830 and clavulanate was similar (synergy against 79% of strains) and superior to ticarcillin-sulbactam (synergy against 39% of strains). YTR 830 was more active than clavulanate against Serratia, Citrobacter, Proteus and Providencia spp. Piperacillin, mezlocillin and apalcillin susceptible strains, with MICs of 8-16 mg/l, showed synergy with inhibitors against 37-87% of strains. Amongst pseudomonads, no synergy was demonstrated against Pseudomonas aeruginosa; ticarcillin produced synergy with the inhibitors against Ps. maltophilia, while piperacillin-YTR 830 and apalcillin-YTR 830 were synergistic against Ps. cepacia. YTR 830 appears to have comparable in-vitro activity to that of clavulanate, and further development of this compound is warranted.

摘要

将新型β-内酰胺酶抑制剂YTR 830与四种广谱青霉素(替卡西林、哌拉西林、美洛西林和阿帕西林)联合应用,针对耐替卡西林的革兰氏阴性肠道杆菌临床分离株进行体外协同活性研究,并与克拉维酸和舒巴坦进行比较。在微量稀释板中,使用固定浓度的β-内酰胺酶抑制剂(8mg/L)与成倍稀释的β-内酰胺类药物进行协同试验。协同作用定义为联合用药时β-内酰胺类药物的最低抑菌浓度(MIC)相较于单独使用β-内酰胺类药物降低四倍或更多。对于79株耐替卡西林的肠杆菌科细菌,替卡西林-YTR 830和替卡西林-克拉维酸对90%的菌株具有协同作用;替卡西林-舒巴坦则对70%的菌株显示出协同作用。三种抑制剂对仅耐替卡西林的菌株的协同活性相似;对于对所有四种广谱青霉素均耐药的菌株,替卡西林与YTR 830及克拉维酸的活性相似(对79%的菌株具有协同作用),且优于替卡西林-舒巴坦(对39%的菌株具有协同作用)。YTR 830对沙雷氏菌属、柠檬酸杆菌属、变形杆菌属和普罗威登斯菌属的活性高于克拉维酸。对哌拉西林、美洛西林和阿帕西林敏感的菌株(MIC为8 - 16mg/L),与抑制剂联合使用时,对37% - 87%的菌株具有协同作用。在假单胞菌中,未发现对铜绿假单胞菌有协同作用;替卡西林与抑制剂联合对嗜麦芽窄食单胞菌有协同作用,而哌拉西林-YTR 830和阿帕西林-YTR 830对洋葱伯克霍尔德菌有协同作用。YTR 830的体外活性似乎与克拉维酸相当,因此有必要对该化合物进行进一步研发。

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