Cardiac sodium channel inhibition by lamotrigine: In vitro characterization and clinical implications.

ABSTRACT: Lamotrigine, approved for use as an antiseizure medication as well as the treatment of bipolar disorder, inhibits sodium channels in the brain to reduce repetitive neuronal firing and pathological release of glutamate. The shared homology of sodium channels and lack of selectivity associated with channel blocking agents can cause slowing of cardiac conduction and increased proarrhythmic potential. The Vaughan-Williams classification system differentiates sodium channel blockers using biophysical properties of binding. As such, Class Ib inhibitors, including mexiletine, do not slow cardiac conduction as measured by the electrocardiogram, at therapeutically relevant exposure. Our goal was to characterize the biophysical properties of Na_V 1.5 block and to support the observed clini

SUBMITTER: Ingleby-Talecki L 

PROVIDER: S-EPMC9372421 | biostudies-literature | 2022 Aug

REPOSITORIES: biostudies-literature