Arrhythmogenic mechanisms of non-sedating antihistamines

Clinical and Experimental Allergy : Journal of the British Society for Allergy and Clinical Immunology
Y G Yap, A J Camm


Antihistamines (H1-receptor antagonists) are amongst the most frequently prescribed drugs worldwide for the treatment of allergic conditions. Recently, there have been reports that certain non-sedating antihistamines, mainly terfenadine and astemizole, might be associated with the risk of rare but severe arrhythmias, namely torsades de pointes, particularly in overdosage, concomitant ingestion of imidazole or macrolide antibiotics and in patients with underlying cardiac or liver diseases. It has now been shown that the molecular target in human ventricle for the potassium channel blockade of antihistamine is HERG gene located in chromosome 7 that expresses the delayed rectifier IKr and appears to be involved in the congenital long QT syndrome. Mechanistic studies showed that blockade of IKr channels by these drugs leads to prolongation of the monophasic action potential (QT interval on surface electrocardiogram) which may then induce the development of early after-depolarization and dispersion of repolarisation leading to torsades de pointes through re-entry mechanism. There are still many questions that need to be answered such as the roles of other potassium channels (IKs, Ito, and Iped) and the relative expression of various...Continue Reading


Jan 1, 1979·The Journal of Physiology·L Cleemann, M Morad
Jul 1, 1992·European Heart Journal·M ZimmermannA Bloch
Jun 1, 1991·Journal of Molecular and Cellular Cardiology·S Kawano, M Hiraoka
Dec 15, 1990·JAMA : the Journal of the American Medical Association·B P MonahanL R Cantilena
May 1, 1991·The American Journal of Emergency Medicine·R B Vukmir
Sep 1, 1988·Progress in Cardiovascular Diseases·W M JackmanR Lazzara
Nov 1, 1983·Journal of the American College of Cardiology·G N KayA L Waldo
Sep 1, 1995·Clinical Pharmacology and Therapeutics·M D BrannanM B Affrime
Apr 15, 1995·Circulation·C I Berul, M Morad
Jan 1, 1995·Journal of Cardiovascular Pharmacology·S P PinneyR L Woosley
Sep 1, 1993·Clinical Cardiology·D M Roden
Sep 1, 1994·Otolaryngology--head and Neck Surgery : Official Journal of American Academy of Otolaryngology-Head and Neck Surgery·S J Smith
Sep 1, 1994·Clinical Pharmacology and Therapeutics·M E SaleM Chung
Aug 1, 1993·Journal of the American College of Cardiology·D M Krikler
Mar 24, 1993·JAMA : the Journal of the American Medical Association·P K HonigL R Cantilena
Mar 24, 1993·JAMA : the Journal of the American Medical Association·R L WoosleyR A Gillis
Oct 1, 1995·Clinical and Experimental Allergy : Journal of the British Society for Allergy and Clinical Immunology·J A HeyW Kreutner
Jan 1, 1996·Annual Review of Pharmacology and Toxicology·R L Woosley
May 3, 1997·Lancet·M Lindquist, I R Edwards
Jul 5, 1997·Lancet·A T Cohen
Jul 5, 1997·Lancet·M H HimmelA S Worobec

❮ Previous
Next ❯


Jun 6, 2007·Journal of Computer-aided Molecular Design·David J Diller, Doug W Hobbs
Mar 5, 2005·The Journal of Allergy and Clinical Immunology·Elizabeth F JuniperPeter H Howarth
Sep 1, 2001·Trends in Cardiovascular Medicine·R Numann, P A Negulescu
Jul 24, 2007·Nature Reviews. Drug Discovery·Jeffrey A KramerDale L Morris
Oct 24, 2012·European Heart Journal·Elijah R Behr, Dan Roden
Oct 12, 2010·American Journal of Physiology. Heart and Circulatory Physiology·Min DongHong-Sheng Wang
Jul 16, 2009·Drug Metabolism Reviews·Alan BoobisKeith Tipton
Feb 11, 2005·Current Medical Research and Opinion·Melvyn BloomJerry Herron
Nov 15, 2011·Drug Safety : an International Journal of Medical Toxicology and Drug Experience·Deborah LaytonSaad A W Shakir
Feb 25, 2009·Drug Safety : an International Journal of Medical Toxicology and Drug Experience·Deborah LaytonSaad A W Shakir
Jul 15, 2015·Journal of the Formosan Medical Association = Taiwan Yi Zhi·Jyh-Ming Jimmy JuangJiunn-Lee Lin
Nov 26, 2008·Journal of Pharmacological and Toxicological Methods·Jessica C BrimecombeArthur M Brown
Jan 21, 2004·Annals of Noninvasive Electrocardiology : the Official Journal of the International Society for Holter and Noninvasive Electrocardiology, Inc·Nenad SarapaArthur J Moss
May 19, 2004·Fundamental & Clinical Pharmacology·Christine GiudicelliJean-François Giudicelli
Jul 8, 2008·British Journal of Pharmacology·M K PugsleyM J Curtis
Sep 24, 2004·Journal of Pharmacological and Toxicological Methods·Glenn E KirschArthur M Brown
Mar 16, 2001·Expert Opinion on Pharmacotherapy·E J Schenkel
Dec 17, 2015·BMC Pharmacology & Toxicology·Yuji HaraguchiTatsuya Shimizu
Apr 19, 2011·European Journal of Pharmacology·Jing ZhaoShuangqing Peng
Jun 5, 2016·Toxicology and Applied Pharmacology·Yea Lu TayMei Lan Tan
Oct 22, 2004·Journal of Clinical Pharmacology·Samir GuptaJerry Herron
Jan 10, 2008·Journal of the European Academy of Dermatology and Venereology : JEADV·J J GrobJ P Ortonne
Jan 10, 2018·Medicinal Research Reviews·Přemysl MladěnkaUNKNOWN TOX-OER and CARDIOTOX Hradec Králové Researchers and Collaborators
Jan 16, 2002·Current Opinion in Cardiology·Robert Dumaine, Charles Antzelevitch
Aug 18, 2016·Naunyn-Schmiedeberg's Archives of Pharmacology·Jiesheng KangDavid Rampe
Nov 15, 2001·The Journal of Allergy and Clinical Immunology·J BousquetUNKNOWN World Health Organization

❮ Previous
Next ❯

Related Concepts

Related Feeds

Atrial Fibrillation

Atrial fibrillation is a common arrhythmia that is associated with substantial morbidity and mortality, particularly due to stroke and thromboembolism. Here is the latest research.


Arrhythmias are abnormalities in heart rhythms, which can be either too fast or too slow. They can result from abnormalities of the initiation of an impulse or impulse conduction or a combination of both. Here is the latest research on arrhythmias.