Correlation Engine 2.0
Clear Search sequence regions
Bookmark Forward

QuickView for Mexiletine (compound)

Name: Mexiletine
PubChem Compound ID: 180621
Description: Antiarrhythmic agent pharmacologically similar to LIDOCAINE. It may have some anticonvulsant properties.
Molecular formula: C11H17NO
Molecular weight: 179.259 g/mol
Name: Mexiletine
Name (isomeric): DB00379
Drug Type: small molecule
Description: Antiarrhythmic agent pharmacologically similar to LIDOCAINE. It may have some anticonvulsant properties.
Mexiletina [INN-Spanish]; Mexilitine; Mexiletinum [INN-Latin]; Mexiletine HCL
Brand: Mexitil
Category: Anti-Arrhythmia Agents
CAS number: 31828-71-4
Indication: For the treatment of ventricular tachycardia and symptomatic premature ventricular beats, and prevention of ventricular fibrillation.
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 decre...
show more »
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. It achieves this reduced sodium current by inhibiting sodium channels. Mexiletine decreases the effective refractory period (ERP) in Purkinje fibers in the heart. The...
show more »
Absorption: Well absorbed (bioavailability 90%) from the gastrointenstinal tract.
Protein binding: 50-60%
Biotransformation: Primarily hepatic (85%) via CYP2D6 and CYP1A2 (primarily CYP2D6).
Route of elimination: Approximately 10% is excreted unchanged by the kidney. The urinary excretion of N-methylmexiletine in man is less than 0.5%.
Half Life: 10-12 hours
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.
Affected organisms: Humans and other mammals
Food interaction:
Take with food to reduce irritation.
Drug interaction:
AminophyllineMexiletine increases the effect and toxicity of theophylline
TerfenadineIncreased risk of cardiotoxicity and arrhythmias
RamelteonMexiletine increases levels/toxicity of ramelteon
ThiothixeneThe strong CYP1A2 inhibitor, Mexiletine, may decrease the metabolism and clearance of Thiothixene, a CYP1A2 substrate. Consider alternate therapy or monitor for changes in Thiothixene therapeutic and adverse effects if Mexiletine is initiated, discontinued or dose changed.
EthotoinThe hydantoin decreases the effect of mexiletine
show more »