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氟喹诺酮类。对其作用方式、抗菌活性、药代动力学及临床疗效的综述。

Fluorinated quinolones. A review of their mode of action, antimicrobial activity, pharmacokinetics and clinical efficacy.

作者信息

Janknegt R

出版信息

Pharm Weekbl Sci. 1986 Feb 21;8(1):1-21. doi: 10.1007/BF01975473.

DOI:10.1007/BF01975473
PMID:3515312
Abstract

Quinolones, chemically related to nalidixic acid, have a strong and rapid bactericidal action against Gram-negative bacteria, including Ps. aeruginosa, some Mycobacteria, Legionella and Staphylococci. Streptococci and anaerobic bacteria are usually less sensitive. The quinolones exert their bactericidal action through inhibition of the enzyme DNA gyrase. Quinolones are absorbed for 50-100% from the gastro-intestinal tract, their volume of distribution is generally high (2 l/kg) and high concentrations are reached in almost all organs. The elimination half-lives range from 4 to 14 h. The efficacy of quinolones in urinary tract infections has been shown in many studies. They also seem to be effective in many serious infections. In animal studies their efficacy was generally equal or superior to aminoglycosides. Until now only mild and infrequent side effects have been reported.

摘要

喹诺酮类药物在化学结构上与萘啶酸相关,对革兰氏阴性菌具有强大而快速的杀菌作用,包括铜绿假单胞菌、某些分枝杆菌、军团菌和葡萄球菌。链球菌和厌氧菌通常不太敏感。喹诺酮类药物通过抑制DNA回旋酶发挥杀菌作用。喹诺酮类药物从胃肠道的吸收率为50% - 100%,其分布容积一般较高(2升/千克),几乎在所有器官中都能达到高浓度。消除半衰期为4至14小时。许多研究已表明喹诺酮类药物在尿路感染中的疗效。它们在许多严重感染中似乎也有效。在动物研究中,其疗效通常与氨基糖苷类药物相当或更优。到目前为止,仅报告了轻微且不常见的副作用。

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A preliminary report on the pharmacokinetics of ofloxacin, desmethyl ofloxacin and ofloxacin N-oxide in patients with chronic renal failure.

本文引用的文献

1
[Comparison of the antimicrobial activity of pefloxacin (1589 RB), nalidixic acid and flumequin (author's transl)].培氟沙星(1589 RB)、萘啶酸和氟甲喹抗菌活性的比较(作者译)
Pathol Biol (Paris). 1982 Jun;30(6):394-7.
2
In vitro activity of ciprofloxacin compared with those of other new fluorinated piperazinyl-substituted quinoline derivatives.环丙沙星与其他新型含氟哌嗪基取代喹啉衍生物的体外活性比较。
Antimicrob Agents Chemother. 1984 Apr;25(4):518-21. doi: 10.1128/AAC.25.4.518.
3
Comparative in vitro activity of ciprofloxacin against Campylobacter spp. and other bacterial enteric pathogens.
氧氟沙星、去甲基氧氟沙星和氧氟沙星N-氧化物在慢性肾衰竭患者体内的药代动力学初步报告。
Drugs. 1987;34 Suppl 1:56-61. doi: 10.2165/00003495-198700341-00013.
4
Steady-state kinetics of the quinolone derivatives ofloxacin, enoxacin, ciprofloxacin and pefloxacin during maintenance treatment with theophylline.茶碱维持治疗期间氧氟沙星、依诺沙星、环丙沙星和培氟沙星等喹诺酮类衍生物的稳态动力学
Drugs. 1987;34 Suppl 1:159-69. doi: 10.2165/00003495-198700341-00034.
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Effect of food on enoxacin absorption.食物对依诺沙星吸收的影响。
Antimicrob Agents Chemother. 1987 Apr;31(4):638-9. doi: 10.1128/AAC.31.4.638.
6
Ofloxacin. A review of its antibacterial activity, pharmacokinetic properties and therapeutic use.氧氟沙星。对其抗菌活性、药代动力学特性及治疗用途的综述。
Drugs. 1987 Apr;33(4):346-91. doi: 10.2165/00003495-198733040-00003.
7
Ciprofloxacin. A review of its antibacterial activity, pharmacokinetic properties and therapeutic use.环丙沙星:抗菌活性、药代动力学特性及治疗用途综述
Drugs. 1988 Apr;35(4):373-447. doi: 10.2165/00003495-198835040-00003.
8
Pharmacokinetics of ciprofloxacin.
Infection. 1988;16 Suppl 1:S3-13. doi: 10.1007/BF01650500.
9
Clinical pharmacokinetics of the newer antibacterial 4-quinolones.新型抗菌4-喹诺酮类药物的临床药代动力学
Clin Pharmacokinet. 1988 Feb;14(2):96-121. doi: 10.2165/00003088-198814020-00003.
10
In vitro susceptibility of Neisseria gonorrhoeae to RO 23-6240 and ciprofloxacin.
Eur J Clin Microbiol. 1987 Jun;6(3):315-7. doi: 10.1007/BF02017623.
环丙沙星对弯曲杆菌属及其他肠道病原菌的体外活性比较
Antimicrob Agents Chemother. 1984 Apr;25(4):504-6. doi: 10.1128/AAC.25.4.504.
4
Effect of inoculum, pH, and medium on the activity of ciprofloxacin against anaerobic bacteria.接种量、pH值和培养基对环丙沙星抗厌氧菌活性的影响。
Antimicrob Agents Chemother. 1984 Mar;25(3):342-3. doi: 10.1128/AAC.25.3.342.
5
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Antimicrob Agents Chemother. 1984 Mar;25(3):331-5. doi: 10.1128/AAC.25.3.331.
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[The antibacterial activity in vitro of ofloxacin in comparison with other orally administered antimicrobial substances on ampicillin-resistant clinical isolates].
Arzneimittelforschung. 1984;34(11):1552-4.
8
The pharmacokinetics and tissue penetration of ofloxacin.氧氟沙星的药代动力学和组织穿透性。 (注:原文中多了一个of,正确表述应该是The pharmacokinetics and tissue penetration of ofloxacin )
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J Pharm Sci. 1984 Oct;73(10):1379-82. doi: 10.1002/jps.2600731014.