IR@PKUHSC  > 北京大学第一临床医学院
学科主题临床医学
Pharmacokinetics/pharmacodynamics of antofloxacin hydrochloride in a neutropenic murine thigh model of Staphylococcus aureus infection
Xiao, Xiu-mei2; Xiao, Yong-hong1
关键词Antofloxacin Hydrochloride Pk/pd Murine Thigh Infection Model Staphylococcus Aureus Auc(24h)/mic
刊名ACTA PHARMACOLOGICA SINICA
2008-10-01
DOI10.1111/j.1745-7254.2008.00872.x
29期:10页:1253-1260
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Chemistry, Multidisciplinary ; Pharmacology & Pharmacy
研究领域[WOS]Chemistry ; Pharmacology & Pharmacy
关键词[WOS]STREPTOCOCCUS-PNEUMONIAE ; MOUSE MODEL ; PHARMACODYNAMICS ; CIPROFLOXACIN ; LEVOFLOXACIN ; FLUOROQUINOLONES ; PARAMETERS
英文摘要

Aim: Antofloxacin hydrochloride is a new fluoroquinolone antibiotic with broad-spectrum in vitro activity. Using the neutropenic murine thigh infection model, we defined the pharmacodynamic profile and property of antofloxacin hydrochloride against Staphylococcus aureus. Methods: Single-dose pharmacokinetic studies of antofloxacin hydrochloride were carried out in thigh infected mice. Therapy was initiated at 2 h postinoculation with 5-640 mg/kg per d fractionated for different dosing regimens. The thighs were removed for bacterial measurement after 24 h of therapy, the best pharmacokinetic/pharmacodynamic (PK/PD) index correlated with the efficacy was determined by nonlinear regression analysis. A sigmoid E-max dose-response model was used to estimate the daily dose and AUC(24 h)/MIC (minimal inhibitory concentration) required to achieve a static effect. Results: The PK was linear with similar elimination half-life over the dose range studied. The AUC(24 h)/MIC ratio was the PK/PD parameter that best correlated with efficacy (R-2=923%, 90.8% for the two organisms, compared with C-max/MIC and T > MIC [%], respectively). The 24 h static dose ranged from 34.3 to 153.7 mg/kg per d for all S aureus strains, the total AUC(24 h)/MIC ratio to achieve bacteriostatic effect varied from 31.7 to 122.5 (mean, 65.7 +/- 30.6). Conclusion: Antofloxacin hydrochloride showed powerful antibacterial activity against the S aureus isolates used in our neutropenicinfected mice model. Our data suggested that the AUC/MIC ratio appeared to be most closely linked to the bacterial outcome (R-2 > 90%), and a total AUC(24 h)/MIC ratio of 65.7 appears to be the target value to achieve a net bactericidal activity against S aureus, similar to the results of other fluoroquinolones.

语种英语
WOS记录号WOS:000259937500016
引用统计
被引频次:6[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/51110
专题北京大学第一临床医学院
作者单位1.Peking Univ, Hosp 1, Beijing 100083, Peoples R China
2.Peking Univ, Hosp 3, Dept Lab Med, Beijing 100083, Peoples R China
推荐引用方式
GB/T 7714
Xiao, Xiu-mei,Xiao, Yong-hong. Pharmacokinetics/pharmacodynamics of antofloxacin hydrochloride in a neutropenic murine thigh model of Staphylococcus aureus infection[J]. ACTA PHARMACOLOGICA SINICA,2008,29(10):1253-1260.
APA Xiao, Xiu-mei,&Xiao, Yong-hong.(2008).Pharmacokinetics/pharmacodynamics of antofloxacin hydrochloride in a neutropenic murine thigh model of Staphylococcus aureus infection.ACTA PHARMACOLOGICA SINICA,29(10),1253-1260.
MLA Xiao, Xiu-mei,et al."Pharmacokinetics/pharmacodynamics of antofloxacin hydrochloride in a neutropenic murine thigh model of Staphylococcus aureus infection".ACTA PHARMACOLOGICA SINICA 29.10(2008):1253-1260.
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