Chemico-biological interactions
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Chem. Biol. Interact. · Sep 2007
Bupivacaine, but not lidocaine, disrupts cardiolipin-containing small biomimetic unilamellar liposomes.
Inadvertent intravenous administration of bupivacaine, unlike that of lidocaine, is associated with significant cardiotoxicity. However, the mechanism(s) underlying this phenomenon is uncertain. High concentrations of cardiolipin, an anionic phospholipid, are found in the mitochondria membrane of cardiomyocytes. ⋯ Both drugs had no significant effects on carboxyfluorescein release from liposomes devoid of cardiolipin (p>0.5). Collectively, these data indicate that bupivacaine, but not lidocaine, interacts avidly and selectively with biomimetic small unilamellar liposomes containing cardiolipin and disrupts their integrity. We suggest that these interactions underlie, in part, bupivacaine-induced cardiotoxicity.