Efficacy and Safety of H1-Antihistamines: An Update

ISSN: 1875-614X (Online)
ISSN: 1871-5230 (Print)

Volume 15, 3 Issues, 2016

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Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Inflammatory and Anti-Allergy Agents

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Claudiu T. Supuran
Neurofarba Department
University of Florence

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Efficacy and Safety of H1-Antihistamines: An Update

Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry, 11(3): 230-237.

Author(s): Fusun Kalpaklioglu and Ayse Baccioglu.

Affiliation: Department of Immunology and Allergic Diseases, Faculty of Medicine, Kirikkale University, Kirikkale, Turkey.


H1-antihistamines are inverse agonists that combine with and stabilize inactive conformation of H1-receptors. Thus they interfere with actions of histamine at H1-receptors. They are widely used for treatment of allergic rhinitis, allergic conjunctivitis, urticaria, coughs, colds and insomnia. H1-antihistamines are classified as older ‘first generation’ and newer ‘second generation’. First generation H1-antihistamines have poor receptor H1-receptor selectivity, and cross blood-brain-barrier. They have a lot of adverse events such as anti-muscarinic, anti-α-adrenergic, anti-serotonin, and sedative effects. In contrast, second generation H1-antihistamines were highly selective for the histamine H1-receptor, do not cross the blood brain barrier, and have minimal adverse events. The risks of first-generation H1-antihistamines have been clearly underestimated, particularly when purchased as nonprescribed over the counter medications by public. This review summarizes curent literature to evaluate antihistamines including their mechanism, indications and side-effects.


Adverse events, antihistamine(s), allergic rhinitis, atopic dermatitis, cardiotoxicity, histamine, pharmacology, receptor, sleep, urticaria.

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Article Details

Volume: 11
Issue Number: 3
First Page: 230
Last Page: 237
Page Count: 8
DOI: 10.2174/1871523011202030230
Price: $58

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