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Pharmacoepidemiology and Risk Management 2023; 15(1): 32-40

Published online March 31, 2023 https://doi.org/10.56142/perm.23.0007

Copyright © Korean Society for Pharmacoepidemiology and Risk Management.

An Overview on the Adverse Reactions of H1-Antihistamine

항히스타민제 이상반응

Kyung-Min Ahn1, Hyun Jee Kim1, Hye-Ryun Kang1,2,3

안경민1, 김현지1, 강혜련1,2,3

1Drug Safety Center, Seoul National University Hospital, Seoul, Korea
2Department of Internal Medicine, Division of Allergy and Clinical Immunology, Seoul National University Hospital, Seoul, Korea
3Institute of Allergy and Clinical Immunology, Medical Research Center, Seoul National University, Seoul, Korea

1서울대학교병원 약물안전센터, 2서울대학교병원 알레르기내과, 3서울대학교 의학연구센터, 알레르기 및 임상면역 연구소

Correspondence to:Hye-Ryun Kang
Drug Safety Center and Department of Internal Medicine, College of Medicine, Seoul National University Hospital, 101 Daehak-ro, Jongno-gu, Seoul 03080, Korea
Tel: +82-2-2072-2865
Fax: +82-2-764-2199
E-mail: helenmed@snu.ac.kr

Received: February 28, 2023; Revised: March 16, 2023; Accepted: March 17, 2023

This is an Open-Access article distributed under the terms of the Creative Commons Attribution Non-Commercial License (http://creativecommons.org/licenses/by-nc/4.0/) which permits unrestricted noncommercial use, distribution, and reproduction in any medium, provided the original work is properly cited.

Abstract

Histamine is one of the most essential biochemical molecules involved in various responses, including inflammation, neurotransmission, and cell proliferation, in diverse organs. Clinical manifestations of allergic diseases are often triggered or initiated by histamine. In order to prevent histamine reactions in allergic disease, clinicians have attempted to develop antagonist of histamine receptors. Due to its effectiveness, antihistamine has been widely used in the treatment of allergic diseases, such as allergic rhinitis and urticaria by inhibiting histamine actions. Although antihistamines are generally safe, there are patients who experience unexpected side effects, such as sedation, cardiotoxicity, hepatotoxicity, nephrotoxicity, and change of appetite. Due to their ability to penetrate through blood-brain barrier, first-generation antihistamines potentially impair alertness, cognition, and memory. The safety profiles of the second-generation antihistamines are relatively superior to the first-generation antihistamines; the second-generation antihistamines cause relatively less central nervous system adverse reactions. However, serious cardiotoxicity of early second-generation antihistamines, such as terfenadine and astemizole, was reported. Moreover, widely-used second-generation antihistamine, cetirizine and loratadine, can present hepatotoxicity. In addition, body weight gain caused by both first- and second-generation antihistamines had been reported. In recent decades, pharmacologic mechanisms that are involved in these sides effect of antihistamine have been elucidated. Understanding detailed mechanisms and consequences of commonly observed side effects may help clinicians prescribe antihistamines safely. Herein, we summarize the mechanisms of histamine action, roles of antihistamines, and their common side effects in order to provide better understanding of antihistamines in clinical practice.

KeywordsHistamine antagonist, Adverse effect, Sedation, Cardiotoxicity, Hepatotoxicity, Nephrotoxicity

Korean Society for Pharmacoepidemiology and Risk Management

Vol.16 No.2
September, 2024

eISSN 2982-5954

Frequency: Bimonthly

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