Mexiletine

Mexiletine (Class IB, Sodium Channel Blocker)

• Overview

  • Amine analog of lidocaine (Xylocaine), but with reduced first-pass metabolism.

  • Suitable for oral administration

  • Similar electrophysiologically to lidocaine

• Clinical Use:

  • Chronic suppression of ventricular tachyarrhythmias

  • Combination with a beta adrenergic receptor blocker or another antiarrhythmic drug (e.g. quinidine gluconate or procainamide ): synergistic effects allow:

    • reduced mexiletine dosage

    • decreased side effect incidence

  • Possibly effective: decreasing neuropathic pain when alternative medications have proven ineffective-- applications (on-label use):

    • diabetic neuropathy

    • nerve injury

• Side effects:

  • Epigastric burning: usually relieved by a taking drug with food

  • nausea (common)

  • Neurologic side effects:

    • diplopia, vertigo, slurred speech (occasionally), tremor

Category: Pharmacology Notes