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Mexiletine

Name: Mexiletine
Description: Antiarrhythmic agent pharmacologically similar to lidocaine. It may have some anticonvulsant properties. (PubChem) Pharmacology: Mexiletine is a local anesthetic, antiarrhythmic agent (Class Ib), structurally similar to lidocaine, but orally active. Mexiletine has fast onset and offset kinetics, meaning that they have little or no effect at slower heart rates, and more effects at faster heart rates. It shortens the action potential duration, reduces refractoriness, and decreases Vmax in partially depolarized cells with fast response action potentials. Mexiletine either does not change the action potential duration, or decreases the action potential duration. Mechanism of action: Mexiletine, like lidocaine, inhibits the inward sodium current required for the initiation and conduction of impulses, thus reducing the rate of rise of the action potential, Phase 0. Mexiletine decreases the effective refractory period (ERP) in Purkinje fibers in the heart. The decrease in ERP is of lesser magnitude than the decrease in action potential duration (APD), which results in an increase in the ERP/APD ratio. It does not significantly affect resting membrane potential or sinus node automaticity, left ventricular function, systolic arterial blood pressure, atrioventricular (AV) conduction velocity, or QRS or QT intervals Drug type: Approved. Small Molecule. Drug category: Anti-Arrhythmia Agents
Synonym(s): Mexiletina (INN-Spanish), Mexiletine HCL, Mexiletinum (INN-Latin), Mexilitine, Mexitil
Has role: Drug
Super-category: Molecular entity
URL: http://www.drugbank.ca/drugs/DB00379
Id: DB00379
Related to: Sodium channel protein type 5 subunit alpha
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Commenttaken from DrugBank
CuratorAb  +
DefiningCitationhttp://www.drugbank.ca/drugs/DB00379  +
DefinitionAntiarrhythmic agent pharmacologically sim Antiarrhythmic agent pharmacologically similar to lidocaine. It may have some anticonvulsant properties. (PubChem) Pharmacology: Mexiletine is a local anesthetic, antiarrhythmic agent (Class Ib), structurally similar to lidocaine, but orally active. Mexiletine has fast onset and offset kinetics, meaning that they have little or no effect at slower heart rates, and more effects at faster heart rates. It shortens the action potential duration, reduces refractoriness, and decreases Vmax in partially depolarized cells with fast response action potentials. Mexiletine either does not change the action potential duration, or decreases the action potential duration. Mechanism of action: Mexiletine, like lidocaine, inhibits the inward sodium current required for the initiation and conduction of impulses, thus reducing the rate of rise of the action potential, Phase 0. Mexiletine decreases the effective refractory period (ERP) in Purkinje fibers in the heart. The decrease in ERP is of lesser magnitude than the decrease in action potential duration (APD), which results in an increase in the ERP/APD ratio. It does not significantly affect resting membrane potential or sinus node automaticity, left ventricular function, systolic arterial blood pressure, atrioventricular (AV) conduction velocity, or QRS or QT intervals Drug type: Approved. Small Molecule. Drug category: Anti-Arrhythmia Agents ule. Drug category: Anti-Arrhythmia Agents
Has roleDrug  +
IdDB00379  +
LabelMexiletine  +
ModifiedDate14 April 2014  +
RelatedToSodium channel protein type 5 subunit alpha  +
SuperCategoryMolecular entity  +
SynonymMexiletina (INN-Spanish)  +, Mexiletine HCL  +, Mexiletinum (INN-Latin)  +, Mexilitine  +, and Mexitil  +