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The quaternary lidocaine derivative QX-314 in combination with bupivacaine for long-lasting nerve block: Efficacy, toxicity, and the optimal formulation in rats  期刊论文  

  • 编号:
    3b5d3bd8-120a-45dd-8868-5c81933ba29b
  • 作者:
    Yin, Qinqin#[1]Li, Jun#[2]Zheng, Qingshan(郑青山)[3]Yang, Xiaolin[2];Lv, Rong[1];Ma, Longxiang[4];Liu, Jin[1,5];Zhu, Tao[1,5];Zhang, Wensheng*[1,5]
  • 语种:
    英文
  • 期刊:
    PLOS ONE ISSN:1932-6203 2017 年 12 卷 3 期 ; MAR 23
  • 收录:
  • 摘要:

    Objective
    The quaternary lidocaine derivative (QX-314) in combination with bupivacaine can produce long-lasting nerve blocks in vivo, indicating potential clinical application. The aim of the study was to investigate the efficacy, safety, and the optimal formulation of this combination.
    Methods
    QX-314 and bupivacaine at different concentration ratios were injected in the vicinity of the sciatic nerve in rats; bupivacaine and saline served as controls (n= 6 similar to 10). Rats were inspected for durations of effective sensory and motor nerve blocks, systemic adverse effects, and histological changes of local tissues. Mathematical models were established to reveal drug-interaction, concentration-effect relationships, and the optimal ratio of QX-314 to bupivacaine.
    Results
    0.2 similar to 1.5% QX-314 with .03 similar to 0.5% bupivacaine produced 5.8 similar to 23.8 h of effective nerve block; while 0.5% bupivacaine alone was effective for 4 h. No systemic side effects were observed; local tissue reactions were similar to those caused by 0.5% bupivacaine if QX-314 were used < 1.2%. The weighted modification model was successfully established, which revealed that QX-314 was the main active ingredient while bupivacaine was the synergist. The formulation, 0.9% QX-314 plus 0.5% bupivacaine, resulted in 10.1 +/- 0.8 h of effective sensory and motor nerve blocks.
    Conclusion
    The combination of QX-314 and bupivacaine facilitated prolonged sciatic nerve block in rats with a satisfactory safety profile, maximizing the duration of nerve block without clinically important systemic and local tissue toxicity. It may emerge as an alternative approach to post-operative pain treatment.

  • 推荐引用方式
    GB/T 7714:
    Yin Qinqin,Li Jun,Zheng Qingshan, et al. The quaternary lidocaine derivative QX-314 in combination with bupivacaine for long-lasting nerve block: Efficacy, toxicity, and the optimal formulation in rats [J].PLOS ONE,2017,12(3).
  • APA:
    Yin Qinqin,Li Jun,Zheng Qingshan,Yang Xiaolin,&Zhang Wensheng.(2017).The quaternary lidocaine derivative QX-314 in combination with bupivacaine for long-lasting nerve block: Efficacy, toxicity, and the optimal formulation in rats .PLOS ONE,12(3).
  • MLA:
    Yin Qinqin, et al. "The quaternary lidocaine derivative QX-314 in combination with bupivacaine for long-lasting nerve block: Efficacy, toxicity, and the optimal formulation in rats" .PLOS ONE 12,3(2017).
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