The stereospecific effects of isoflurane isomers in vivo

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Abstract

The anesthetic potency of racemic isoflurane and the optically pure stereoisomers was examined in rats. The (+) isomer was 53% more potent than the (−) isomer (minimum alveolar concentration (MAC) = 1.06 ± 0.07% vs. 1.62 ± 0.02%, P < 0.05). MAC for racemic isoflurane was 1.32 ± 0.03%. Both stereoisomers and the racemic isoflurane produced similar depression of arterial pressure. However, the (+) isomer blunted the cardiovascular response to a painful stimulus to a greater extent than did an equi-MAC dose of the (−) isomer. These are the first data to describe pharmacological differences between stereoisomers of a volatile anesthetic administered in vivo by the conventional route (inhaled) and measuring the clinically relevant index of anesthesia, MAC. These data are consistent with a receptor-mediated anesthetic mechanism by volatile anesthetics.

References (16)

  • B. Harris et al.

    Isoflurane anesthesia is stereoselective

    Eur. J. Pharmacol.

    (1992)
  • E.J. Moody et al.

    Stereospecific actions of the inhalation anesthetic isoflurane at the GABAA receptor complex

    Brain Res.

    (1993)
  • Z.B. Bosnjak et al.

    Lack of stereospecific effects of isoflurane isomers on isolated guinea pig hearts

    FASEB J.

    (1993)
  • D.R. Burt

    Criteria for receptor identification

  • B. Drenger et al.

    Volatile anesthetics depress calcium channel blocker binding to bovine cardiac sarcolemma

    Anesthesiology

    (1991)
  • N.P. Franks et al.

    Stereospecific effects of inhalational general anesthetic optical isomers on nerve ion channels

    Science

    (1991)
  • B. Harris et al.

    Neurochemical actions of inhalational anesthetics at the GABAA receptor complex

    J. Pharmacol. Exp. Ther.

    (1993)
  • P.J. Hoehner et al.

    Halothane depresses D600 binding to bovine heart sarcolemma

    Anesthesiology

    (1991)
There are more references available in the full text version of this article.

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    Citation Excerpt :

    Pharmacodynamic effects are site-specific. This possibility was supported by the finding that general anaesthetics were found to be enantiospecific, but this enantiospecificity cannot be accounted for by their effects on the cell membrane [29–32]. The membrane is thus unlikely to be the site of action of general anaesthetics.

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