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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]
Sodium channels exist in three main conformations: the resting state, the open state, and the inactive state. Phenytoin binds preferentially to the inactive form of the sodium channel. Because it takes time for the bound drug to dissassociate from the inactive channel, there is a time-dependent block of the channel.
Common side effects include abdominal pain, chest discomfort, drowsiness, headache, and nausea. It works as a non-selective voltage-gated sodium channel blocker and belongs to the Class IB group of anti-arrhythmic medications.
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 ...
Triamterene directly blocks the epithelial sodium channel [4] (ENaC) on the lumen side of the kidney collecting tubule. [5]: 127 Other diuretics cause a decrease in the sodium concentration of the forming urine due to the entry of sodium into the cell via the ENaC, and the concomitant exit of potassium from the principal cell into the forming urine.
In addition, lamotrigine shares few side effects with other, unrelated anticonvulsants known to inhibit sodium channels, which further emphasizes its unique properties. [72] It is a triazine derivate that inhibits voltage-sensitive sodium channels, leading to stabilization of neuronal membranes.
A channel blocker is the biological mechanism in which a particular molecule is used to prevent the opening of ion channels in order to produce a physiological response in a cell. Channel blocking is conducted by different types of molecules, such as cations, anions, amino acids, and other chemicals.
The effect on sodium channels could be of particular relevance for seizure protection. Although topiramate does inhibit high-voltage-activated calcium channels, its relevance to clinical activity is uncertain. Effects on specific GABA-A receptor isoforms could also contribute to the antiseizure activity of the drug.
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