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洛美沙星在药代动力学体外模型中的抗菌活性

Antibacterial activity of lomefloxacin in a pharmacokinetic in vitro model.

作者信息

Rustige C, Wiedemann B

机构信息

Pharmazeutische Mikrobiologie, Universität Bonn, Federal Republic of Germany.

出版信息

Antimicrob Agents Chemother. 1990 Jun;34(6):1107-11. doi: 10.1128/AAC.34.6.1107.

DOI:10.1128/AAC.34.6.1107
PMID:2118324
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC171766/
Abstract

An in vitro model simulating two-compartment pharmacokinetics was used to study the antibacterial activity of lomefloxacin after single oral doses of 200 and 400 mg. Lomefloxacin produced reliable bactericidal activity against gram-negative aerobic bacteria and staphylococci. Bacterial strains for which MICs were less than 0.5 microgram/ml were inhibited with both dosing schedules. Doubling the dose from 200 to 400 mg increased the bactericidal activity only against Pseudomonas aeruginosa. Against Enterococcus faecalis lomefloxacin showed no effect. Selection of resistant variants during the simulation of treatment was observed with Staphylococcus aureus and P. aeruginosa.

摘要

采用模拟双室药代动力学的体外模型,研究了单次口服200毫克和400毫克洛美沙星后的抗菌活性。洛美沙星对革兰氏阴性需氧菌和葡萄球菌具有可靠的杀菌活性。两种给药方案均能抑制最低抑菌浓度小于0.5微克/毫升的菌株。将剂量从200毫克加倍至400毫克仅增加了对铜绿假单胞菌的杀菌活性。洛美沙星对粪肠球菌无作用。在模拟治疗过程中,观察到金黄色葡萄球菌和铜绿假单胞菌出现了耐药变异株。

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本文引用的文献

1
Antibacterial effects of cefroxadine, cephalexin and cephradine in a new in vitro pharmacokinetic model.头孢沙定、头孢氨苄和头孢拉定在新型体外药代动力学模型中的抗菌作用
J Antibiot (Tokyo). 1982 Jul;35(7):843-9. doi: 10.7164/antibiotics.35.843.
2
Selection of multiple antibiotic resistance by quinolones, beta-lactams, and aminoglycosides with special reference to cross-resistance between unrelated drug classes.喹诺酮类、β-内酰胺类和氨基糖苷类药物对多重抗生素耐药性的选择,特别提及不相关药物类别之间的交叉耐药性。
Antimicrob Agents Chemother. 1984 Dec;26(6):797-801. doi: 10.1128/AAC.26.6.797.
3
Pharmacokinetics and tolerance of lomefloxacin after sequentially increasing oral doses.洛美沙星口服剂量递增后的药代动力学及耐受性
Antimicrob Agents Chemother. 1988 Oct;32(10):1503-7. doi: 10.1128/AAC.32.10.1503.
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Pharmacokinetics and tissue penetration of orally administered lomefloxacin.口服洛美沙星的药代动力学和组织穿透性。
Antimicrob Agents Chemother. 1988 Oct;32(10):1508-10. doi: 10.1128/AAC.32.10.1508.
5
In vitro activity of lomefloxacin (SC-47111; NY-198), a difluoroquinolone 3-carboxylic acid, compared with those of other quinolones.洛美沙星(SC - 47111;NY - 198),一种二氟喹诺酮3 - 羧酸,与其他喹诺酮类药物相比的体外活性。
Antimicrob Agents Chemother. 1988 May;32(5):656-62. doi: 10.1128/AAC.32.5.656.
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