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

Autor: Lindsey Ingleby‐Talecki, Sven C. van Dijkman, Sean P. Oosterholt, Oscar Della Pasqua, Christina Winter, Marianne Cunnington, Linda Rebar, Sergio Forero‐Schwanhaeuser, Vickas Patel, James A. Cooper, Anthony Bahinski, Khuram W. Chaudhary
Rok vydání: 2022
Předmět:
Zdroj: Clinical and Translational Science. 15:1978-1989
ISSN: 1752-8062
1752-8054
DOI: 10.1111/cts.13311
Popis: 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
Databáze: OpenAIRE
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