Suppr超能文献

哌拉西林,一种新型青霉素,对许多耐其他青霉素的细菌有活性。

Piperacillin, a new penicillin active against many bacteria resistant to other penicillins.

作者信息

Fu K P, Neu H C

出版信息

Antimicrob Agents Chemother. 1978 Mar;13(3):358-67. doi: 10.1128/AAC.13.3.358.

Abstract

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.

摘要

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。

相似文献

引用本文的文献

1
Ionizable Lipid Containing Nanocarriers for Antimicrobial Agent Delivery.用于抗菌剂递送的含可电离脂质纳米载体
Small Sci. 2024 Aug 13;4(10):2400145. doi: 10.1002/smsc.202400145. eCollection 2024 Oct.
3
New Frontiers in Druggability.药物可及性的新前沿
J Med Chem. 2015 Dec 10;58(23):9063-88. doi: 10.1021/acs.jmedchem.5b00586. Epub 2015 Aug 11.
5
beta-Lactamases in laboratory and clinical resistance.实验室及临床耐药中的β-内酰胺酶
Clin Microbiol Rev. 1995 Oct;8(4):557-84. doi: 10.1128/CMR.8.4.557.
6
Piperacillin/tazobactam in complicated urinary tract infections.
Intensive Care Med. 1994 Jul;20 Suppl 3:S39-42. doi: 10.1007/BF01745250.

本文引用的文献

5
Carbenicillin and hypokalemia.羧苄青霉素与低钾血症
Ann Intern Med. 1973 May;78(5):774-5. doi: 10.7326/0003-4819-78-5-774.
6
Microiodometric determination of beta-lactamase activity.β-内酰胺酶活性的微量碘量法测定
Antimicrob Agents Chemother. 1972 Feb;1(2):94-9. doi: 10.1128/AAC.1.2.94.
7
Pharmacokinetics of ticarcillin in patients with abnormal renal function.
J Infect Dis. 1976 Jan;133(1):46-9. doi: 10.1093/infdis/133.1.46.

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验