ロピバカインの薬物動態と毒性  [in Japanese] Ropivacaine : Pharmacokinetics and Toxicity  [in Japanese]

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Author(s)

    • 小田 裕 ODA Yutaka
    • 大阪市立大学大学院医学研究科麻酔科学講座 Department of Anesthesiology, Osaka City University Graduate School of Medicine

Abstract

  長時間作用型局所麻酔薬ロピバカイン (商品名: アナペイン<sup>®</sup>) は主として肝臓で代謝を受けるため, 肝機能が低下している場合は血中濃度の上昇や作用時間の延長が生ずる可能性がある. ロピバカインの半減期はラセミ体ブピバカイン (以下, ブピバカイン) よりも短く, 硬膜外投与後の半減期は約5.5時間である. 実験動物においてくも膜下腔に直接投与した場合の神経毒性はリドカインやブピバカインに比べて低く, 硬膜外麻酔や伝達麻酔に安全に用いることができると考えられる. 血中濃度の上昇によって生ずる中枢神経症状はリドカインやロピバカインの場合と類似しているが, 中枢神経毒性, 心毒性はいずれもブピバカインよりも低く, レボブピバカインとほぼ同程度である.

  Ropivacaine, the S (-) -enantiomer of 1-propyl-2',6'-pipecoloxylidide, is a long-acting local anesthetic with a structure homologous to that of bupivacaine. Ropivacaine is metabolized by hepatic cytochrome P4501A and 3A to produce the aromatic rings 3'-hydroxylated ropivacaine and 2',6'-pipecoloxylidide. Systemic clearance of ropivacaine is predominantly dependent on hepatic P4503A activity, and is decreased in subjects with impaired liver function. Plasma half-life of ropivacaine is shorter than bupivacaine after epidural infusion. Neuronal toxicity of ropivacaine after intrathecal infusion is lower than lidocaine and racemic bupivacaine in experimental animals, suggesting that ropivacaine is able to be safely used for regional anesthesia in the clinic. Symptoms induced by inadvertent intravascular injection are similar to those of other local anesthetics such as lidocaine and bupivacaine. Both central nervous system and cardiovascular toxicity of ropivacaine are lower than racemic bupivacaine, and comparable with levobupivacaine.

Journal

  • THE JOURNAL OF JAPAN SOCIETY FOR CLINICAL ANESTHESIA

    THE JOURNAL OF JAPAN SOCIETY FOR CLINICAL ANESTHESIA 29(4), 519-527, 2009-07-15

    THE JAPAN SOCIETY FOR CLINICAL ANESTHESIA

References:  30

Cited by:  2

Codes

  • NII Article ID (NAID)
    10025382951
  • NII NACSIS-CAT ID (NCID)
    AN00330159
  • Text Lang
    JPN
  • Article Type
    Journal Article
  • ISSN
    02854945
  • Data Source
    CJP  CJPref  J-STAGE 
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