Modernized Classification of Cardiac Antiarrhythmic Drugs

Circulation. 2018 Oct 23;138(17):1879-1896. doi: 10.1161/CIRCULATIONAHA.118.035455.

Abstract

Background: Among his major cardiac electrophysiological contributions, Miles Vaughan Williams (1918-2016) provided a classification of antiarrhythmic drugs that remains central to their clinical use.

Methods: We survey implications of subsequent discoveries concerning sarcolemmal, sarcoplasmic reticular, and cytosolic biomolecules, developing an expanded but pragmatic classification that encompasses approved and potential antiarrhythmic drugs on this centenary of his birth.

Results: We first consider the range of pharmacological targets, tracking these through to cellular electrophysiological effects. We retain the original Vaughan Williams Classes I through IV but subcategorize these divisions in light of more recent developments, including the existence of Na+ current components (for Class I), advances in autonomic (often G protein-mediated) signaling (for Class II), K+ channel subspecies (for Class III), and novel molecular targets related to Ca2+ homeostasis (for Class IV). We introduce new classes based on additional targets, including channels involved in automaticity, mechanically sensitive ion channels, connexins controlling electrotonic cell coupling, and molecules underlying longer-term signaling processes affecting structural remodeling. Inclusion of this widened range of targets and their physiological sequelae provides a framework for a modernized classification of established antiarrhythmic drugs based on their pharmacological targets. The revised classification allows for the existence of multiple drug targets/actions and for adverse, sometimes actually proarrhythmic, effects. The new scheme also aids classification of novel drugs under investigation.

Conclusions: We emerge with a modernized classification preserving the simplicity of the original Vaughan Williams framework while aiding our understanding and clinical management of cardiac arrhythmic events and facilitating future developments in this area.

Keywords: anti-arrhythmia agents; arrhythmias, cardiac; homeostasis; ion channels.

Publication types

  • Research Support, Non-U.S. Gov't
  • Systematic Review

MeSH terms

  • Action Potentials / drug effects
  • Animals
  • Anti-Arrhythmia Agents / adverse effects
  • Anti-Arrhythmia Agents / classification*
  • Anti-Arrhythmia Agents / therapeutic use*
  • Arrhythmias, Cardiac / diagnosis
  • Arrhythmias, Cardiac / drug therapy*
  • Arrhythmias, Cardiac / metabolism
  • Arrhythmias, Cardiac / physiopathology
  • Calcium Channel Blockers / classification
  • Calcium Channel Blockers / therapeutic use
  • Heart Conduction System / drug effects*
  • Heart Conduction System / metabolism
  • Heart Conduction System / physiopathology
  • Heart Rate / drug effects*
  • Humans
  • Ion Channels / drug effects
  • Ion Channels / metabolism
  • Membrane Transport Modulators / adverse effects
  • Membrane Transport Modulators / classification*
  • Membrane Transport Modulators / therapeutic use*
  • Neurotransmitter Agents / classification
  • Neurotransmitter Agents / therapeutic use
  • Potassium Channel Blockers / classification
  • Potassium Channel Blockers / therapeutic use
  • Terminology as Topic*
  • Voltage-Gated Sodium Channel Blockers / classification
  • Voltage-Gated Sodium Channel Blockers / therapeutic use

Substances

  • Anti-Arrhythmia Agents
  • Calcium Channel Blockers
  • Ion Channels
  • Membrane Transport Modulators
  • Neurotransmitter Agents
  • Potassium Channel Blockers
  • Voltage-Gated Sodium Channel Blockers