The conventional antihistamine drug cyproheptadine lacks QT-interval-prolonging action in halothane-anesthetized guinea pigs: comparison with hydroxyzine

J Pharmacol Sci. 2014;124(1):92-8. doi: 10.1254/jphs.13159fp. Epub 2013 Dec 27.

Abstract

Antihistamines are known to belong to the chemical class that may induce long QT syndrome. Among them, cyproheptadine has been shown to exert multifaceted actions on the ventricular repolarization phase; namely, shortening of the action potential duration at supra-therapeutic concentrations of 2 - 8 μM and prolongation of the QT interval at ≥ 10 μM. Since information is limited regarding the in vivo electrophysiological effects of cyproheptadine, we assessed it using the halothane-anesthetized guinea-pig model, which was compared with effects of another antihistamine drug, hydroxyzine. Sub-therapeutic to therapeutic doses of hydroxyzine at 1 and 10 mg/kg, i.v. prolonged the QT interval and duration of monophasic action potential, whereas therapeutic to supra-therapeutic doses of cyproheptadine at 0.1 and 1 mg/kg, i.v. hardly affected the indices of ventricular repolarization. These results suggest that cyproheptadine may be categorized into antihistamines with little effect on the ventricular repolarization.

Publication types

  • Comparative Study

MeSH terms

  • Action Potentials / drug effects*
  • Anesthesia
  • Animals
  • Cyproheptadine / administration & dosage
  • Cyproheptadine / adverse effects*
  • Dose-Response Relationship, Drug
  • Electrocardiography / drug effects*
  • Guinea Pigs
  • Halothane
  • Heart Ventricles / drug effects
  • Heart Ventricles / physiopathology
  • Histamine Antagonists / administration & dosage
  • Histamine Antagonists / adverse effects
  • Histamine Antagonists / classification
  • Histamine Antagonists / pharmacology*
  • Hydroxyzine / administration & dosage
  • Hydroxyzine / adverse effects*
  • Hydroxyzine / pharmacology
  • Injections, Intravenous
  • Long QT Syndrome / chemically induced*

Substances

  • Histamine Antagonists
  • Cyproheptadine
  • Hydroxyzine
  • Halothane