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与已上市化合物(头孢噻肟、拉氧头孢和哌拉西林)相比,研究中的β-内酰胺类药物(头孢吡肟、头孢匹罗、氟氧头孢、SCE2787和哌拉西林加他唑巴坦)对新型β-内酰胺酶的体外活性和稳定性。

In vitro activity and stability against novel beta-lactamases of investigational beta-lactams (cefepime, cefpirome, flomoxef, SCE2787 and piperacillin plus tazobactam) in comparison with established compounds (cefotaxime, latamoxef and piperacillin).

作者信息

Bauernfeind A, Schweighart S, Eberlein E, Jungwirth R

机构信息

Max von Pettenkofer-Institut, München, Germany.

出版信息

Infection. 1991;19 Suppl 5:S264-75. doi: 10.1007/BF01645538.

Abstract

The therapeutic perspectives of flomoxef, SCE 2787, cefpirome, cefepime, latamoxef, cefotaxime and of piperacillin plus tazobactam were comparatively evaluated by their in vitro activity against 1119 clinical isolates of 83 bacterial species. Escherichia coli, Klebsiella spp. Enterobacter sakazakii, Proteus spp. and Shigella spp. were about equally susceptible to the cephalosporins (MIC90: 0.06 to 0.5 mg/l), while the MIC90 for piperacillin plus tazobactam was between 2 and 16 mg/l. Enterobacter cloacae, Enterobacter aerogenes and Serratia spp. were most susceptible to SCE 2787, cefpirome and cefepime (MIC90: 0.06 to 2 mg/l) followed by latamoxef, cefotaxime, flomoxef and piperacillin plus tazobactam. For Citrobacter spp., Providencia spp. and Yersinia enterocolitica MIC90 were between 0.06 and 0.5 mg/l. Flomoxef was between 2 to 4 log2 less active against these species but more active than piperacillin plus tazobactam (MIC90: 2 and 8 mg/l). Morganella morganii and Hafnia alvei were most susceptible to cefepime, cefpirome and latamoxef (MIC90: 0.13 to 0.5 mg/l) while cefotaxime (MIC90: 8 mg/l) and piperacillin plus tazobactam (MIC90: 8 and greater than 64 mg/l) were the least active compounds. SCE 2787, cefepime and cefpirome were the most potent beta-lactams against the majority of the 13 species of non-fermentative bacilli (NFB) investigated (MIC90: 0.5 to 16 mg/l). The oxacephems were the least active compounds against NFB. Cefepime was the most active of the compounds included against Pseudomonas aeruginosa (MIC90: 16 mg/l). Haemophilus spp., Neisseria gonorrhoeae and Bordetella pertussis were most susceptible to cefotaxime (MIC90: 0.03 to 0.06 mg/l). Latamoxef had the lowest activity of all compounds against gram-positive cocci. Flomoxef was the most active compound against penicillinase producing Staphylococcus aureus and about equally active as the other betalactams against methicillin susceptible staphylococci of other staphylococcal species.(ABSTRACT TRUNCATED AT 250 WORDS)

摘要

通过对1119株83种细菌临床分离株的体外活性,比较评估了氟氧头孢、SCE 2787、头孢匹罗、头孢吡肟、拉氧头孢、头孢噻肟以及哌拉西林加他唑巴坦的治疗前景。大肠埃希菌、克雷伯菌属、阪崎肠杆菌、变形杆菌属和志贺菌属对头孢菌素的敏感性大致相同(MIC90:0.06至0.5mg/L),而哌拉西林加他唑巴坦的MIC90在2至16mg/L之间。阴沟肠杆菌、产气肠杆菌和沙雷菌属对SCE 2787、头孢匹罗和头孢吡肟最敏感(MIC90:0.06至2mg/L),其次是拉氧头孢、头孢噻肟、氟氧头孢和哌拉西林加他唑巴坦。对于柠檬酸杆菌属、普罗威登斯菌属和小肠结肠炎耶尔森菌,MIC90在0.06至0.5mg/L之间。氟氧头孢对这些菌种的活性比其他药物低2至4个对数2,但比哌拉西林加他唑巴坦活性高(MIC90:2和8mg/L)。摩根摩根菌和蜂房哈夫尼亚菌对头孢吡肟、头孢匹罗和拉氧头孢最敏感(MIC90:0.13至0.5mg/L),而头孢噻肟(MIC90:8mg/L)和哌拉西林加他唑巴坦(MIC90:8和大于64mg/L)活性最低。SCE 2787、头孢吡肟和头孢匹罗是针对所研究的13种非发酵菌(NFB)中的大多数最有效的β-内酰胺类药物(MIC90:0.5至16mg/L)。氧头孢烯类药物对NFB活性最低。头孢吡肟是所包含的对铜绿假单胞菌活性最高的化合物(MIC90:16mg/L)。嗜血杆菌属、淋病奈瑟菌和百日咳博德特菌对头孢噻肟最敏感(MIC90:0.03至0.06mg/L)。拉氧头孢对革兰氏阳性球菌的活性在所有化合物中最低。氟氧头孢是对产青霉素酶金黄色葡萄球菌活性最高的化合物,对其他葡萄球菌属的甲氧西林敏感葡萄球菌的活性与其他β-内酰胺类药物大致相同。(摘要截选至250字)

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