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左氧氟沙星在败血症小鼠模型中治疗全身性铜绿假单胞菌感染的体内口服疗效。

In vivo oral efficacy of levofloxacin for treatment of systemic Pseudomonas aeruginosa infections in a murine model of septicemia.

作者信息

Yagel S K, Barrett J F, Amaratunga D J, Frosco M B

机构信息

R. W. Johnson Pharmaceutical Research Institute, Raritan, New Jersey 08869, USA.

出版信息

Antimicrob Agents Chemother. 1996 Dec;40(12):2894-7. doi: 10.1128/AAC.40.12.2894.

Abstract

The in vivo efficacies of levofloxacin and ciprofloxacin in lethal, systemic Pseudomonas aeruginosa infections in mice were compared. MICs of levofloxacin and ciprofloxacin ranged from 0.5 to 2.0 micrograms/ml and from 0.12 to 1.0 microgram/ml respectively. Infecting doses ranged from 5.0 x 10(1) to 3.2 x 10(3) CFU per mouse, depending on the isolate. Test fluoroquinolones were administered orally at 1 h (single dose) or at 1 and 3 h (divided dose) postinfection, with 10 infected mice used for each of six concentrations of each fluoroquinolone tested (1 to 40 mg/kg of body weight) in each dosing regimen. Whether given in a single or a divided dose, the total daily dose was the same for each fluoroquinolone. For mice treated 1 h postinfection with levofloxacin and ciprofloxacin, the effective doses for 50% of the infected mice ranged from 2.09 to 13.80 mg/kg and from 2.34 to 11.22 mg/kg, respectively, and for those treated 1 and 3 h postinfection, the effective doses for 50% of the infected mice ranged from 3.71 to 16.98 mg/kg and from 2.95 to 13.18 mg/kg, respectively. Although the potency varied for both levofloxacin and ciprofloxacin among all strains of P. aeruginosa tested, there were small differences within the same strain for levofloxacin and ciprofloxacin when given in the same dosing regimen. Levofloxacin proved nearly as effective as ciprofloxacin against a systemic P. aeruginosa infection in mice.

摘要

比较了左氧氟沙星和环丙沙星对小鼠致死性全身性铜绿假单胞菌感染的体内疗效。左氧氟沙星和环丙沙星的最低抑菌浓度分别为0.5至2.0微克/毫升和0.12至1.0微克/毫升。感染剂量根据分离株的不同,每只小鼠为5.0×10¹至3.2×10³CFU。在感染后1小时(单剂量)或1小时和3小时(分剂量)口服给予受试氟喹诺酮类药物,每种氟喹诺酮类药物测试的六种浓度(1至40毫克/千克体重)中的每种浓度各用10只感染小鼠,每种给药方案均如此。无论单剂量还是分剂量给药,每种氟喹诺酮类药物的每日总剂量相同。对于感染后1小时用左氧氟沙星和环丙沙星治疗的小鼠,50%感染小鼠的有效剂量分别为2.09至13.80毫克/千克和2.34至11.22毫克/千克,对于感染后1小时和3小时治疗的小鼠,50%感染小鼠的有效剂量分别为3.71至16.98毫克/千克和2.95至13.18毫克/千克。尽管在所有测试的铜绿假单胞菌菌株中,左氧氟沙星和环丙沙星的效力有所不同,但在相同给药方案下,同一菌株内左氧氟沙星和环丙沙星的差异较小。左氧氟沙星在对抗小鼠全身性铜绿假单胞菌感染方面证明与环丙沙星几乎同样有效。

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本文引用的文献

1
Quinolone resistance: a practical perspective.
Arch Intern Med. 1993 Jan 11;153(1):120-1.
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Epidemiology of chronic Pseudomonas aeruginosa infections in cystic fibrosis.
J Infect Dis. 1994 Dec;170(6):1616-21. doi: 10.1093/infdis/170.6.1616.
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Mechanisms of high-level resistance to quinolones in urinary tract isolates of Pseudomonas aeruginosa.
Antimicrob Agents Chemother. 1994 Jul;38(7):1466-9. doi: 10.1128/AAC.38.7.1466.

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