Ropivacaine: Pharmacokinetics and Toxicity

DOI 2 Citations 58 References
  • ODA Yutaka
    Department of Anesthesiology, Osaka City University Graduate School of Medicine

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  • ロピバカインの薬物動態と毒性

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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.

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