Tocainide

• Tocainide (Class I, Sodium Channel Blocker)

  • Amine analog of lidocaine, similar to mexiletine, orally active --but with reduced first-pass metabolism.

  • Used for chronic suppression of ventricular tachyarrhythmias

  • Electrophysiologically similar to lidocaine

  • Similar to mexiletine: tocainide + if beta-adrenergic receptor blocker or another antiarrhythmic drug: synergism

    • e.g.--Combination with quinidine may increase efficacy and diminish adverse effects.

  • Side Effects:

    • Profile similar to mexiletine

    • suitable for oral administration, but RARELY USED due to possibly fatal bone marrow aplasia and pulmonary fibrosis.

    • tremor and nausea are major dose-related adverse side effects

  • Excreted by the kidney, accordingly dose should be reduced in patients with renal disease

Stoelting, R.K., "Cardiac Antidysrhythmic Drugs", in Pharmacology and Physiology in Anesthetic Practice, Lippincott-Raven Publishers, 1999, 331-343

Category: Pharmacology Notes