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Overview
| Generic Names: | Mexiletina [INN-Spanish]; Mexiletine HCL; Mexiletinum [INN-Latin]; Mexilitine |
|---|---|
| Trade Names: | Mexitil |
| PharmGKB Accession Id: | PA450488 |
Description
Antiarrhythmic agent pharmacologically similar to lidocaine. It may have some anticonvulsant properties. PubChem (source: Drug Bank)
Indication
For the treatment of ventricular tachycardia and symptomatic premature ventricular beats, and prevention of ventricular fibrillation. (source: Drug Bank)
ATC Therapeutic Category
- C01BB:Antiarrhythmics, class Ib
Pharmacology, Interactions, and Contraindications
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 (source: Drug Bank)
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. (source: Drug Bank)
Food Interactions
Take with food to reduce irritation. (source: Drug Bank)
Absorption, Distribution, Metabolism, Elimination & Toxicity
Biotransformation
Primarily hepatic (85%) via CYP2D6 and CYP1A2 (primarily CYP2D6). (source: Drug Bank)
Protein Binding
50-60% (source: Drug Bank)
Absorption
Well absorbed (bioavailability 90%) from the gastrointenstinal tract. (source: Drug Bank)
Toxicity
Symptoms of overdose include nausea, hypotension, sinus bradycardia, paresthesia, seizures, bundle branch block, AV heart block, asystole, ventricular tachyarrythmia, including ventricular fibrillation, cardiovascular collapse, and coma. (source: Drug Bank)
Isomeric SMILES Code:
Cc1cccc(c1OCC(C)N)C (source: Drug Bank)
The following genes are in curated knowledge about this drug.
| Gene | Relationship | Evidence | |
|---|---|---|---|
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CYP2D6 |
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Publications |
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KCNH2 |
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Publications |
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SCN4A |
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Publications |
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SCN5A |
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Publications |
A list of non-curated publications that mention this drug along with other genes is available.
Drug Targets
| Gene | Description | |
|---|---|---|
| SCN5A |
|
(source: Drug Bank) |
PharmGKB Curated Pathways
A list of non-curated publications that mention this drug along with other drugs is available.
Drug Interactions
| Drug | Description | |
|---|---|---|
| aminophylline |
|
Mexiletine increases the effect and toxicity of theophylline (source: Drug Bank) |
| dyphylline |
|
Mexiletine increases the effect and toxicity of theophylline (source: Drug Bank) |
| ethotoin |
|
The hydantoin decreases the effect of mexiletine (source: Drug Bank) |
| fluvoxamine |
|
Fluvoxamine increases the effect and toxicity of mexiletine (source: Drug Bank) |
| fosphenytoin |
|
The hydantoin decreases the effect of mexiletine (source: Drug Bank) |
| mephenytoin |
|
The hydantoin decreases the effect of mexiletine (source: Drug Bank) |
| oxtriphylline |
|
Mexiletine increases the effect and toxicity of theophylline (source: Drug Bank) |
| phenytoin |
|
The hydantoin decreases the effect of mexiletine (source: Drug Bank) |
| propafenone |
|
Propafenone increases the effects/toxicity of mexiletine (source: Drug Bank) |
| rifampin |
|
Rifampin decreases the effect of mexiletine (source: Drug Bank) |
| terfenadine |
|
Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank) |
| theophylline |
|
Mexiletine increases the effect and toxicity of theophylline (source: Drug Bank) |
Curated Information
The following diseases are in curated knowledge about this drug.
| Disease | Relationship | Evidence | |
|---|---|---|---|
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Long QT Syndrome |
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Publications |
Non-Curated Information
A list of non-curated publications that mention this drug along with other diseases is available.
Additional Datasets
These datasets are minimally curated and are sorted alphabetically by title.
LinkOuts
Common Searches
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Non-Curated Publications
A list of non-curated publications that mention this drug is available.