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Sodium channel blockers are drugs which impair the conduction of sodium ions (Na +) through sodium channels.
Sodium-channel blockers comprise the Class I antiarrhythmic compounds according to the Vaughan-Williams classification scheme. These drugs bind to and block fast sodium channels that are responsible for rapid depolarization (phase 0) of fast-response cardiac action potentials.
A class of drugs that act by inhibition of sodium influx through cell membranes. Blockade of sodium channels slows the rate and amplitude of initial rapid depolarization, reduces cell excitability, and reduces conduction velocity.
Mar 2, 2024 · Sodium channel blocker toxicity is a critical aspect of clinical care given the widespread use of medications such as Vaughn Williams Class 1 antiarrhythmics, local anesthetics, and neuropathic pain treatments like tricyclic antidepressants (TCAs), anticonvulsants, and cocaine.
Brittany Norton, MFA, Sam Gillespie, BSc, Yifan Xiao, MD. Antiarrhythmic drugs help control arrhythmias or abnormal heartbeats. There are four main groups of antiarrhythmic medications: class I, sodium-channel blockers; class II, beta-blockers; class III, potassium-channel blockers; class IV, calcium-channel blockers; and miscellaneous ...
The term “sodium channel blockers” covers a wide range of naturally occurring and synthetic compounds that block the ion permeation through sodium-selective ion channels, large transmembrane proteins that control rapid membrane depolarization in electrically excitable cells.
In this article, we review the history of the use of sodium channel blockers, describe the current status of sodium channel drug discovery, highlight the challenges and hurdles to attain sodium channel subtype selectivity, and review the potential usefulness of selective sodium channel blockers in neuropathic pain.
