Mexiletine
Mexiletine Uses, Dosage, Side Effects, Food Interaction and all others data.
Antiarrhythmic agent pharmacologically similar to lidocaine. It may have some anticonvulsant properties.
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.
| Trade Name | Mexiletine |
| Availability | Prescription only |
| Generic | Mexiletine |
| Mexiletine Other Names | Mexiletina, Mexilétine, Mexiletine, Mexiletinum |
| Related Drugs | propranolol, atenolol, amiodarone, lidocaine, verapamil, flecainide, Tenormin, Inderal, dofetilide |
| Weight | 150mg, 200mg, 250mg |
| Type | Oral capsule |
| Formula | C11H17NO |
| Weight | Average: 179.2588 Monoisotopic: 179.131014171 |
| Protein binding | 50-60% |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | United States |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Mexiletine is a class 1B antiarrhythmic agent used in the treatment of documented ventricular arrhythmias that warrant treatment.
For the treatment of ventricular tachycardia and symptomatic premature ventricular beats, and prevention of ventricular fibrillation.
Mexiletine is also used to associated treatment for these conditions: Severe Ventricular tachycardia, Severe ventricular arrhythmias
How Mexiletine works
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 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
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.
Food Interaction
- Take with food. Food reduces irritation.
Mexiletine Drug Interaction
Moderate: duloxetineMinor: ascorbic acid, ascorbic acidUnknown: aspirin, aspirin, aspirin, aspirin, apixaban, apixaban, sacubitril / valsartan, sacubitril / valsartan, atorvastatin, pregabalin, pregabalin, metoprolol, metoprolol, cyanocobalamin, cyanocobalamin, cholecalciferol, cholecalciferol
Mexiletine Disease Interaction
Major: cardiovascular dysfunction, proarrhythmic effects, AV node dysfunctionModerate: liver disease, renal dysfunction, seizures
Volume of Distribution
- 5 to 7 L/lg
Elimination Route
Well absorbed (bioavailability 90%) from the gastrointenstinal tract.
Half Life
10-12 hours
Elimination Route
Approximately 10% is excreted unchanged by the kidney. The urinary excretion of N-methylmexiletine in man is less than 0.5%.
Innovators Monograph
You find simplified version here Mexiletine
