Antihistamines (H1 receptor antagonists)

Research output: Chapter in Book/Report/Conference proceedingChapter


This chapter discusses the adverse effects of antihistamines (H1 receptor antagonists). Antihistamines act as inverse agonists that combine with H1 receptors, stabilizing them in the inactive form and shifting the equilibrium towards the inactive state. The cardiotoxic effects of antihistamines are of concern in patients with long QT syndrome who also have allergies. Fixed drug eruptions are the most frequent types of adverse cutaneous drug reaction; although fixed drug eruptions caused by systemic antihistamines are very rare, some have been previously reported with both cetirizine and levocetirizine, and another has been reported. First-generation sedating antihistamines such as dexchlorpheniramine and diphenhydramine readily cross the blood–brain barrier, resulting in blockade of histamine H1 receptors in the brain, which are responsible for maintaining a state of arousal, leading to drowsiness, fatigue, and psychomotor disturbances.
Original languageEnglish
Title of host publicationSide effects of drugs annual
Subtitle of host publicationa worldwide yearly survey of new data and trends in adverse drug reactions
EditorsJeffrey K Aronson
Place of PublicationAmsterdam, Netherlands
PublisherElsevier Science
Number of pages6
ISBN (Print)0444535500, 978-0444535504
Publication statusPublished - 21 Dec 2010

Publication series

NameMeyler's Side Effects of Drugs
PublisherElsevier Science
ISSN (Print)0378-6080


Dive into the research topics of 'Antihistamines (H1 receptor antagonists)'. Together they form a unique fingerprint.

Cite this