Acute toxicity is a dose-limiting factor for intravenous polymyxin B: A safety and pharmacokinetic study in healthy Chinese subjects.

Objectives: Polymyxin B is a last-line antibiotic for multidrug-resistant gram-negative bacterial infections. However, limited safety and pharmacokinetic information is available. We investigated the safety and pharmacokinetics of intravenous polymyxin B in healthy subjects.Methods: An open-label, s...

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Publicado en:Journal of Infection Vol. 82; no. 2; pp. 207 - 216
Autores principales: Liu, Xiaofen, Chen, Yuancheng, Yang, Haijing, Li, Jian, Yu, Jicheng, Yu, Zhenwei, Cao, Guoying, Wu, Xiaojie, Wang, Yu, Wu, Hailan, Fan, Yaxin, Wang, Jingjing, Wu, Jufang, Jin, Yi, Guo, Beining, Hu, Jiali, Bian, Xingchen, Li, Xin, Zhang, Jing
Formato: research randomized controlled trial Journal Article
Publicado: W B Saunders Feb2021
Acceso en línea:Ver este registro en EBSCOhost
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        01634453
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      jtl: Journal of Infection
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      dt: Feb2021
      vid: 82
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      pub: W B Saunders
      place: Philadelphia, Pennsylvania
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        NLM33453286
        148775248
        10.1016/j.jinf.2021.01.006
        NLM33453286
        148775248
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        atl: Acute toxicity is a dose-limiting factor for intravenous polymyxin B: A safety and pharmacokinetic study in healthy Chinese subjects.
      aug:
        au:
          Liu, Xiaofen
          Chen, Yuancheng
          Yang, Haijing
          Li, Jian
          Yu, Jicheng
          Yu, Zhenwei
          Cao, Guoying
          Wu, Xiaojie
          Wang, Yu
          Wu, Hailan
          Fan, Yaxin
          Wang, Jingjing
          Wu, Jufang
          Jin, Yi
          Guo, Beining
          Hu, Jiali
          Bian, Xingchen
          Li, Xin
          Zhang, Jing
        affil: Institute of Antibiotics, Huashan Hospital, Fudan University, 12 Wulumuqi Zhong Road, Shanghai 200040, China
      sug:
        subj:
          Antibiotics Adverse Effects
          Polymyxin B Adverse Effects
          China
          Human
          Female
          Male
          Research Subjects
          Administration, Intravenous
          Comparative Studies
          Multicenter Studies
          Evaluation Research
          Validation Studies
          Randomized Controlled Trials
          Random Assignment
          Female
          Male
      ab: Objectives: Polymyxin B is a last-line antibiotic for multidrug-resistant gram-negative bacterial infections. However, limited safety and pharmacokinetic information is available. We investigated the safety and pharmacokinetics of intravenous polymyxin B in healthy subjects.Methods: An open-label, single-dose clinical trial was conducted in healthy Chinese subjects. Polymyxin B (sulphate) was administered intravenously at 0.75 or 1.5 mg/kg (n = 10 per dose, 5 males and 5 females) to examine the safety and pharmacokinetics.Results: One female subject in the 1.5-mg/kg group discontinued due to abdominal pain during administration. The most frequently reported adverse events were perioral paraesthesia, dizziness, and numbness of extremities (7/10 subjects in the 0.75-mg/kg group, all subjects in the 1.5-mg/kg group). All neurotoxicity-related events dissipated without treatment within a maximum of 23 h. Notably, abdominal pain (3/5) and vulvar pruritus (2/5), colpitis (2/5) or abnormal uterine bleeding (1/5) were reported in female subjects receiving the 1.5-mg/kg dose. In the 0.75-mg/kg group, the total clearance, volume of distribution and half-life of polymyxin B were 0.028±0.002 L/h/kg, 0.219±0.023 L/kg and 5.44±0.741 h, respectively; similar values were observed in the 1.5-mg/kg group. Urinary recovery was 3.7 ± 1.1% and 8.1 ± 1.3% in the 0.75- and 1.5-mg/kg groups, respectively. Population pharmacokinetics of polymyxin B was consistent with a three-compartment model. The clearance and distribution of the central compartment were 0.027 L/h/kg and 0.071 L/kg, respectively.Conclusions: This study is the first to examine the safety and pharmacokinetics of polymyxin B in healthy subjects. Our results highlight that acute toxicity is a dose-limiting factor for intravenous polymyxin B.
      pubtype: Academic Journal
      doctype:
        research
        randomized controlled trial
        Journal Article
      ougenre: Article
    language: English
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