Article
The opioid methadone induces a local anaesthetic-like inhibition of the cardiac Na⁺ channel, Na(v)1.5.
British journal of pharmacology - 1 Jan 2014
Schulze V, Stoetzer C, O'Reilly A O, Eberhardt E, Foadi N, Ahrens J, Wegner F, Lampert A, de la Roche J, Leffler A
Abstract excerpt
BACKGROUND AND PURPOSE: Treatment with methadone is associated with severe cardiac arrhythmias, a side effect that seems to result from an inhibition of cardiac hERG K⁺ channels. However, several other opioids are inhibitors of voltage-gated Na⁺ channels. Considering the common assumption that an inhibition of the cardiac Na⁺ channel Na(v)1.5, is the primary mechanism for local anaesthetic (LA)-induced...
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