Prolongation in QT interval is not predictive of Ca2+-dependent arrhythmias: implications for drug safety

Expert Opin Drug Saf. 2009 Jan;8(1):57-72. doi: 10.1517/14740330802655454.

Abstract

Background: Voltage-gated ion channels are the main providers of drug-induced delayed repolarization and, therefore, first line targets in cardiac safety assessments.

Objectives/methods: We review mechanisms of drug-induced ventricular arrhythmias that may be associated with sudden cardiac death. We focus on Ca(2+)-dependent mechanisms with drug safety concerns.

Results: Early afterdepolarizations occur during abnormally prolonged action potential repolarization. QT interval measurement is commonly used to assess the proarrhythmic risk of a drug. However, delayed afterdepolarizations are triggered by intracellular Ca(2+) overload and/or abnormal spontaneous openings of ryanodine receptors in diastole. A drug promoting alterations of Ca(2+) handling may be pro-arrhythmogenic without QT interval change at rest.

Conclusion: Ca(2+)-dependent arrhythmia should be investigation matter in drug safety evaluation.

Publication types

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

MeSH terms

  • Action Potentials
  • Arrhythmias, Cardiac / chemically induced*
  • Arrhythmias, Cardiac / physiopathology
  • Calcium / physiology*
  • Death, Sudden, Cardiac / etiology
  • Drug-Related Side Effects and Adverse Reactions*
  • Humans
  • Ion Channel Gating
  • Long QT Syndrome / chemically induced
  • Long QT Syndrome / physiopathology
  • Ryanodine Receptor Calcium Release Channel / physiology
  • Torsades de Pointes / chemically induced
  • Torsades de Pointes / physiopathology
  • Ventricular Function / drug effects
  • Ventricular Function / physiology

Substances

  • Ryanodine Receptor Calcium Release Channel
  • Calcium