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头孢匹罗(HR 810)是一种对葡萄球菌、肠杆菌科细菌和铜绿假单胞菌有效的吡啶头孢菌素类药物,其体外活性及对β-内酰胺酶的稳定性。

The in vitro activity and beta-lactamase stability of cefpirome (HR 810), a pyridine cephalosporin agent active against staphylococci, Enterobacteriaceae and Pseudomonas aeruginosa.

作者信息

Neu H C, Chin N X, Labthavikul P

出版信息

Infection. 1985 May-Jun;13(3):146-55. doi: 10.1007/BF01642876.

DOI:10.1007/BF01642876
PMID:3928497
Abstract

The in vitro activity of cefpirome, a new cyclopyridinium cephalosporin, was evaluated against 947 aerobic and anaerobic bacteria. Cefpirome inhibited 90% of Escherichia coli, Klebsiella spp., Citrobacter diversus, Morganella morganii, Proteus vulgaris, Proteus mirabilis, Aeromonas spp., Salmonella spp., Shigella spp. and Haemophilus and Neisseria species at less than or equal to 0.4 mg/l. It had activity comparable to that of cefotaxime, ceftizoxime, ceftazidime, aztreonam, and moxalactam against these species. Only a few Citrobacter freundii, Enterobacter spp. and Serratia marcescens had MICs above 3.1 mg/l. The activity of cefpirome against Pseudomonas aeruginosa, 90% MIC of 12.5 mg/l, was superior to piperacillin, moxalactam, cefotaxime and cefoperazone. The 90% MIC against Staphylococcus aureus was 0.8 mg/l, but methicillin-resistant staphylococci were not inhibited. Cefpirome was not significantly hydrolyzed by most plasmid beta-lactamases (TEM, SHV-1, PSE, OXA) nor by chromosomal enzymes (P99, Branhamella catarrhalis, K1). Cefpirome did not inhibit chromosomal or plasmid beta-lactamases. Mice systemically infected with E. coli, Klebsiella pneumoniae, P. aeruginosa and S. aureus were protected by concentrations of cefpirome ranging from 0.85 mg/kg for K. pneumoniae to 4.467 mg/kg for P. aeruginosa.

摘要

对一种新型环吡啶头孢菌素头孢匹罗的体外活性进行了评估,受试菌株为947株需氧菌和厌氧菌。头孢匹罗对90%的大肠杆菌、克雷伯菌属、异型枸橼酸杆菌、摩根摩根菌、普通变形杆菌、奇异变形杆菌、气单胞菌属、沙门菌属、志贺菌属以及嗜血杆菌属和奈瑟菌属的抑制浓度小于或等于0.4mg/L。它对这些菌属的活性与头孢噻肟、头孢唑肟、头孢他啶、氨曲南和拉氧头孢相当。只有少数弗氏枸橼酸杆菌、肠杆菌属和粘质沙雷菌的最低抑菌浓度高于3.1mg/L。头孢匹罗对铜绿假单胞菌的活性(90%最低抑菌浓度为12.5mg/L)优于哌拉西林、拉氧头孢、头孢噻肟和头孢哌酮。对金黄色葡萄球菌的90%最低抑菌浓度为0.8mg/L,但对耐甲氧西林葡萄球菌无抑制作用。头孢匹罗不会被大多数质粒β-内酰胺酶(TEM、SHV-1、PSE、OXA)以及染色体酶(P99、卡他莫拉菌、K1)显著水解。头孢匹罗不抑制染色体或质粒β-内酰胺酶。对全身性感染大肠杆菌、肺炎克雷伯菌、铜绿假单胞菌和金黄色葡萄球菌的小鼠,能起到保护作用的头孢匹罗浓度范围为:对肺炎克雷伯菌为0.85mg/kg,对铜绿假单胞菌为4.467mg/kg。

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The in vitro activity and beta-lactamase stability of cefpirome (HR 810), a pyridine cephalosporin agent active against staphylococci, Enterobacteriaceae and Pseudomonas aeruginosa.头孢匹罗(HR 810)是一种对葡萄球菌、肠杆菌科细菌和铜绿假单胞菌有效的吡啶头孢菌素类药物,其体外活性及对β-内酰胺酶的稳定性。
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引用本文的文献

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Drugs. 1997 Jul;54(1):117-40. doi: 10.2165/00003495-199754010-00013.
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In vitro activity of cefpirome against selected clinical enterobacterial isolates with beta-lactamase-mediated resistance.头孢匹罗对选定的具有β-内酰胺酶介导耐药性的临床肠杆菌分离株的体外活性。
Infection. 1995 Nov-Dec;23(6):384-7. doi: 10.1007/BF01713572.
3
Bactericidal activity of cefpirome (HR 810) against 513 gram-negative bacteria isolated from blood of septicemic patients.

本文引用的文献

1
Trapping of nonhydrolyzable cephalosporins by cephalosporinases in Enterobacter cloacae and Pseudomonas aeruginosa as a possible resistance mechanism.阴沟肠杆菌和铜绿假单胞菌中的头孢菌素酶截留不可水解头孢菌素作为一种可能的耐药机制。
Antimicrob Agents Chemother. 1982 May;21(5):711-7. doi: 10.1128/AAC.21.5.711.
2
Susceptibility of gram-positive aerobic cocci to the new cephalosporin HR 810.革兰氏阳性需氧球菌对新型头孢菌素HR 810的敏感性
Eur J Clin Microbiol. 1983 Aug;2(4):354-5. doi: 10.1007/BF02019468.
3
In vitro evaluation of HR810, a new wide-spectrum aminothiazolyl alpha-methoxyimino cephalosporin.
头孢匹罗(HR 810)对从败血症患者血液中分离出的513株革兰氏阴性菌的杀菌活性。
Infection. 1994 Jul-Aug;22(4):299-305. doi: 10.1007/BF01739925.
4
In vitro activity of E-1040, a novel cephalosporin with potent activity against Pseudomonas aeruginosa.新型头孢菌素E-1040对铜绿假单胞菌的体外活性,该头孢菌素对铜绿假单胞菌具有强效活性。
Antimicrob Agents Chemother. 1988 Nov;32(11):1666-75. doi: 10.1128/AAC.32.11.1666.
5
Comparative in vitro activity of cefpirome and cefepime, two new cephalosporins.
Eur J Clin Microbiol Infect Dis. 1990 Sep;9(9):677-85. doi: 10.1007/BF01964272.
新型广谱氨噻唑基α-甲氧基氨基头孢菌素HR810的体外评价
Antimicrob Agents Chemother. 1984 Jun;25(6):710-8. doi: 10.1128/AAC.25.6.710.
4
HR 810, a cephalosporin with low affinity for Enterobacter cloacae beta-lactamase.HR 810,一种对阴沟肠杆菌β-内酰胺酶亲和力较低的头孢菌素。
Eur J Clin Microbiol. 1983 Aug;2(4):352-4. doi: 10.1007/BF02019467.
5
The Antibacterial activity in vitro and beta-lactamase stability of the new cephalosporin HR 810 in comparison with five other cephalosporins and two aminoglycosides.新型头孢菌素HR 810与其他五种头孢菌素及两种氨基糖苷类药物相比的体外抗菌活性及β-内酰胺酶稳定性
Infection. 1983 Sep-Oct;11(5):275-9. doi: 10.1007/BF01641262.
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HR 810, a new parenteral cephalosporin with a broad antibacterial spectrum.HR 810,一种新型的具有广谱抗菌活性的肠胃外使用的头孢菌素。
Arzneimittelforschung. 1983;33(8):1084-6. doi: 10.1002/chin.198350201.
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In vitro activity of HR 810, a new broad-spectrum cephalosporin.新型广谱头孢菌素HR 810的体外活性
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The in vitro activity, human pharmacology, and clinical effectiveness of new beta-lactam antibiotics.新型β-内酰胺类抗生素的体外活性、人体药理学及临床疗效
Annu Rev Pharmacol Toxicol. 1982;22:599-642. doi: 10.1146/annurev.pa.22.040182.003123.
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Indirect method for assessing the penetration of beta-lactamase-nonsusceptible penicillins and cephalosporins in Escherichia coli strains.评估β-内酰胺酶不敏感青霉素和头孢菌素在大肠杆菌菌株中渗透性的间接方法。
Antimicrob Agents Chemother. 1976 Aug;10(2):215-8. doi: 10.1128/AAC.10.2.215.
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Dissociated resistance among cephalosporins.头孢菌素之间的分离耐药性。
Antimicrob Agents Chemother. 1979 Apr;15(4):497-503. doi: 10.1128/AAC.15.4.497.