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Pharmacological studies of the enantiomer of bupivacaine

Research Project

Project/Area Number 08671755
Research Category

Grant-in-Aid for Scientific Research (C)

Allocation TypeSingle-year Grants
Section一般
Research Field Anesthesiology/Resuscitation studies
Research InstitutionMiyazaki Medical College

Principal Investigator

TAKASAKI Mayumi  Miyazaki Medical College, Department of Anesthesiology, Professor, 医学部, 教授 (30094212)

Co-Investigator(Kenkyū-buntansha) KATSUKI Hiroshi  Miyazaki Medical College, Department of Anesthesiology, Instructor, 医学部, 助手 (80194786)
Project Period (FY) 1996 – 1997
Project Status Completed (Fiscal Year 1997)
Budget Amount *help
¥2,200,000 (Direct Cost: ¥2,200,000)
Fiscal Year 1997: ¥1,100,000 (Direct Cost: ¥1,100,000)
Fiscal Year 1996: ¥1,100,000 (Direct Cost: ¥1,100,000)
Keywordsbupvacaine / ropivacaine / enantiomer / intracellular concentration / 細胞内濃度 / レボブピバカイン / 神経細胞内濃度
Research Abstract

Background : Levobupivacaine and ropivacaine are both single S(-)-enantiomers that have less cardiotoxic and convulsant effects than racemic bupivacaine. The anesthetic action of S(-)-bupivacaine, R(+)-bupivacaine and ropivacaine was directly compared in vitro by studying their effects on action potential and the maximum value of dV/dt (dV/dt max) in crayfish giant axon. To clarify the difference of intracellular anesthetic concentration, the intracellular ionized anesthetic concentration was measured.
Methods : Desheathed crayfish axons were perfused with 1 mM of each anesthetic agent at a stimulation frequency of either 0.1 or 5 Hz. Intracellular anesthetic concentration was measured using local anesthetic-sensitive microelectrodes.
Results : At 0.1-Hz stimulation, no differences were observed in either model. In crayfish giant axon at 5 Hz stimulation, the order of magnitude of the mean percentage decrease in dV/dt max was S(-)-bupivacaine > R(+)-bupivacaine> ropivacaine. Intracellular local anesthetic concentration did not differ among three agents.
Conclusion : Compared with ropivacaine, S(-)-bupivacaine has potent phasic blocking effect in crayfish giant axon. The equivalent intracellular local anesthetic concentration among three agents suggests that intracellular protonated local anesthetic concentration are not directly correlated with blocking effects.

Report

(3 results)
  • 1997 Annual Research Report   Final Research Report Summary
  • 1996 Annual Research Report
  • Research Products

    (4 results)

All Other

All Publications (4 results)

  • [Publications] 金井祐子: "ブピバカインとロピバカインの麻酔効果の比較" Journal of Anesthesia. 12 Suppl. 177 (1998)

    • Description
      「研究成果報告書概要(和文)」より
    • Related Report
      1997 Final Research Report Summary
  • [Publications] Kanai Yuko, Katsuki Hiroshi and Takasaki Mayumi: "Comparison of anesthetic effect of bupivacaine and ropivacaine." Journal of Anesthesia. 12 Suppl. 177 (1998)

    • Description
      「研究成果報告書概要(欧文)」より
    • Related Report
      1997 Final Research Report Summary
  • [Publications] 金井 裕子: "ブピバカインとロピバカインの麻酔効果の比較" Journal of Anesthesia. 1998 (12Suppl)

    • Related Report
      1997 Annual Research Report
  • [Publications] 金井 裕子: "ブピバカインとロピバカインの麻酔効果の比較" Journal of Anesthesia. 1998 (12Suppl)177:

    • Related Report
      1997 Annual Research Report

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Published: 1996-04-01   Modified: 2016-04-21  

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