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Studies of local anesthetics on use-dependent block

Research Project

Project/Area Number 18591711
Research Category

Grant-in-Aid for Scientific Research (C)

Allocation TypeSingle-year Grants
Section一般
Research Field Anesthesiology/Resuscitation studies
Research InstitutionUniversity of Miyazaki

Principal Investigator

TAKASAKI Mayumi  University of Miyazaki, Director (30094212)

Co-Investigator(Kenkyū-buntansha) TANIGUCHI Masahiko  University of Miyazaki, Faculty of Medicine, Intensive Care Unit, Assistant Professor (70305085)
TATEYAMA Shingo  University of Miyazaki, Faculty of Medicine, Department of Anesthesiology & Intensive Care, Instructor (10372799)
IBUSUKI Shoichiro  University of Miyazaki, Faculty of Medicine, Surgical Division, Assistant Professor (70315381)
Project Period (FY) 2006 – 2007
Project Status Completed (Fiscal Year 2007)
Budget Amount *help
¥3,930,000 (Direct Cost: ¥3,600,000、Indirect Cost: ¥330,000)
Fiscal Year 2007: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
Fiscal Year 2006: ¥2,500,000 (Direct Cost: ¥2,500,000)
KeywordsLocal anesthetics / Use-dependent block / Intracellular concentration
Research Abstract

Clinically, lidocaine requires a large concentration than bupivacaine to block nerves. Local anesthetics access to sodium channels from the intracellular milieu. Primarily, we determined the intracellular concentrations of lidocaine and bupivacaine when a nerve was blocked in the giant axon of a crayfish. A solution of lidocaine or bupivacaine was perfused, and a nerve block was determined as the absence of an evoked action potential after tonic or phasic electrical stimulation. The intracellular lidocaine or bupivacaine concentration was measured using a lidocaine- or bupivacaine-sensitive glass microelectrode. A phasic block was more effectively and rapidly achieved with a smaller concentration of bupivacaine than with lidocaine. An 11 to 16-fold larger intracellular concentration of lidocaine than bupivacaine was observed to block a single nerve. The ratio of the intra-to extracellular concentration was significantly larger for lidocaine than for bupivacaine. These findings suggest that bupivacaine produces a more potent nerve block and a use-dependent (phasic) block at smaller concentrations than lidocaine. Secondarily, we determined the intracellular concentration of licocaine when a nerve was blocked with lidocaine alone or dimethylsulfoxide (DMSO)-containing lidocaine. The giant axon of crayfish was blocked dose-dependently with DMSO but not blocked with 0.2%DMSO. However, 0.2%DMSO-containing lidocaine produced significantly greater block than lidocaine alone. The intra- to extracellular ratio of lidocaine was similar in the 0.2%DMSO-containing lidocaine and lidocaine alone. These results demonstrate that nerve conduction block is modified by other mechanism except blocking effect of sodium channel from the axoplasma.

Report

(3 results)
  • 2007 Annual Research Report   Final Research Report Summary
  • 2006 Annual Research Report
  • Research Products

    (7 results)

All 2006

All Journal Article (6 results) (of which Peer Reviewed: 2 results) Presentation (1 results)

  • [Journal Article] ブロック発生時の細胞内リドカインとブピバカイン濃度の比較2006

    • Author(s)
      矢野 武志, ほか
    • Journal Title

      Journal of Anesthesia 20Suppl

      Pages: 193-193

    • Description
      「研究成果報告書概要(和文)」より
    • Related Report
      2007 Final Research Report Summary
    • Peer Reviewed
  • [Journal Article] A comparison of intracellular lidocaine and bupivacaine concentrations producing nerve conduction block in the giant axon of crayfish in vitro2006

    • Author(s)
      Yano, Takeshi, et. al.
    • Journal Title

      Anesthesia and Analgesia 102

      Pages: 1734-1738

    • Description
      「研究成果報告書概要(和文)」より
    • Related Report
      2007 Final Research Report Summary
    • Peer Reviewed
  • [Journal Article] A comparison of intracellular lidocaine and bupivacaine concentrations producing nerve conduction block2006

    • Author(s)
      Takeshi, Yano, Shoichiro, Ibusuki, Mayumi, Takasaki
    • Journal Title

      Journal of Anesthesia 20

      Pages: 193-193

    • Description
      「研究成果報告書概要(欧文)」より
    • Related Report
      2007 Final Research Report Summary
  • [Journal Article] A comparison of intracellular lidocaine and bupivacaine concentrations producing nerve conduction block in the giant axon of crayfish in vitro2006

    • Author(s)
      Takeshi, Yano, Shoichiro, Ibusuki, Mayumi, Takasaki
    • Journal Title

      Anesthesia and Analgesia 102 : 6

      Pages: 1734-8

    • Description
      「研究成果報告書概要(欧文)」より
    • Related Report
      2007 Final Research Report Summary
  • [Journal Article] ブロック発生時の細胞内リドカインとブピバカイン濃度の比較2006

    • Author(s)
      矢野武志, ほか
    • Journal Title

      Journal of Anesthesia 20・Suppl

      Pages: 193-193

    • Related Report
      2006 Annual Research Report
  • [Journal Article] A comparison of intracellular lidocaine and bupivacaine concentrations producing nerve conduction block in the giant axon of crayfish in vitro2006

    • Author(s)
      Takeshi Yano, et al.
    • Journal Title

      Anesthesia and Analgesia 102・6

      Pages: 1734-8

    • Related Report
      2006 Annual Research Report
  • [Presentation] ブロック発生時の細胞内リドカインとブピバカイン濃度の比較2006

    • Author(s)
      矢野 武志, ほか
    • Organizer
      日本麻酔科学会第53回学術集会
    • Place of Presentation
      神戸市
    • Description
      「研究成果報告書概要(和文)」より
    • Related Report
      2007 Final Research Report Summary

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Published: 2006-04-01   Modified: 2016-04-21  

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