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Sodium channel blockers are also used as local anesthetics and anticonvulsants. [5] Sodium channel blockers have been proposed for use in the treatment of cystic fibrosis, [6] but current evidence is mixed. [7] It has been suggested that the analgesic effects of some antidepressants may be mediated in part via sodium channel blockade. [8]
It is a sodium channel blocker and is classified as a Class 1a anti-arrhythmic agent. [3] [4] Disopyramide has a negative inotropic effect on the ventricular myocardium, significantly decreasing the contractility. [5] [6] Disopyramide also has general anticholinergic effects which contribute to unwanted adverse effects. Disopyramide is ...
For example, TTX can bind and inactivate voltage-gated sodium channels, despite the fact that TTX is much larger and chemically different than sodium ions. Given the disparities in size and chemical properties between TTX and a sodium ion, this is an example of structure being used to block usually specific channels.
Procainamide (PCA) is a medication of the antiarrhythmic class used for the treatment of cardiac arrhythmias.It is a sodium channel blocker of cardiomyocytes; thus it is classified by the Vaughan Williams classification system as class Ia.
Carbamazepine is a sodium channel blocker. [37] It binds preferentially to voltage-gated sodium channels in their inactive conformation, which prevents repetitive and sustained firing of an action potential. Carbamazepine has effects on serotonin systems but the relevance to its antiseizure effects is uncertain.
[13] [14] Inhibition of the Na v 1.5 channel is specifically involved in its antiarrhythmic effects as a class I antiarrhythmic agent. [15] Quinidine also blocks certain voltage-gated potassium channels (e.g., K v 1.4 , K v 4.2 , hERG , among others), [ 16 ] [ 17 ] acts as an antimuscarinic and alpha-1 blocker , [ 18 ] and is an antimalarial ...
Cenobamate is a voltage-gated sodium channel (VGSC) blocker. [15] It is a selective blocker of the inactivated state of VGSCs, preferentially inhibiting persistent sodium current. [15] It has been proposed that cenobamate additionally enhances presynaptic release of γ-aminobutyric acid (GABA), thereby increasing inhibitory GABAergic ...
Phencyclidine: a dissociative anesthetic previously used in medicine, but its development was discontinued in the 1960s in favor of its successor ketamine due to its relatively high incidence of psychotomimetic effects. Abused recreational and legally controlled in most countries. Remacemide: a low affinity antagonist also a sodium-channel blocker.