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Disposition kinetics and dosage regimen of levofloxacin on concomitant administration with paracetamol in crossbred calves

机译:左氧氟沙星与对乙酰氨基酚在杂种犊牛中同时给药的处置动力学和剂量方案

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摘要

The disposition kinetics of levofloxacin was investigated in six male crossbred calves following single intravenous administration, at a dose of 4 mg/kg body weight, into the jugular vein subsequent to a single intramuscular injection of paracetamol (50 mg/kg). At 1 min after the injection of levofloxacin, the concentration of levofloxacin in plasma was 17.2 ± 0.36 µg/ml, which rapidly declined to 6.39 ± 0.16 µg/ml at 10 min. The drug level above the MIC90 in plasma, was detected for up to 10 h. Levofloxacin was rapidly distributed from blood to the tissue compartment as evidenced by the high values of the distribution coefficient, α (17.3 ± 1.65 /h) and the ratio of K12/K21 (1.83 ± 0.12). The values of AUC and Vdarea were 12.7 ± 0.12 µg.h/ml and 0.63 ± 0.01 l/kg. The high ratio of the AUC/MIC (126.9 ± 1.18) obtained in this study indicated the excellent antibacterial activity of levofloxacin in calves. The elimination half-life, MRT and total body clearance were 1.38 ± 0.01 h, 1.88 ± 0.01 h and 0.32 ± 0.003 l/kg/h, respectively. Based on the pharmacokinetic parameters, an appropriate intravenous dosage regimen for levofloxacin would be 5 mg/kg repeated at 24 h intervals when prescribed with paracetamol in calves.
机译:在单次肌内注射扑热息痛(50 mg / kg)后,以4 mg / kg体重的剂量单次静脉内注射到颈静脉后,在六只雄性杂种小牛中研究了左氧氟沙星的处置动力学。注射左氧氟沙星后1分钟,血浆中左氧氟沙星的浓度为17.2±0.36 µg / ml,在10分钟时迅速下降至6.39±0.16 µg / ml。检测到血浆中MIC90以上的药物水平长达10小时。左氧氟沙星从血液迅速分布到组织区室,其分布系数α(17.3±1.65 / h)和K12 / K21之比(1.83±0.12)较高,证明了这一点。 AUC和Vdarea的值为12.7±0.12 µg.h / ml和0.63±0.01 l / kg。这项研究中获得的高AUC / MIC比(126.9±1.18)表明左氧氟沙星在犊牛中具有出色的抗菌活性。消除半衰期,MRT和全身清除率分别为1.38±0.01 h,1.88±0.01 h和0.32±0.003 l / kg / h。根据药代动力学参数,在牛犊中与扑热息痛一起开处方时,左氧氟沙星的适当静脉给药方案应为5 mg / kg,间隔24小时重复一次。

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  • 作者

    Dumka, Vinod K.;

  • 作者单位
  • 年度 2007
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  • 原文格式 PDF
  • 正文语种 {"code":"en","name":"English","id":9}
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