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A Review on Mechanism of Histamine Mediated Allergic Reactions: Therapeutic Role, Safety, and Clinical Efficacy of Cetirizine in Modern Allergy and Other Diseases Management

Suman Ghosh, Ishita Debnath, Sobhanjan Bhunia, Supriya Hazra, Sumit Nandi, Sudip Kumar Mandal, neha Mallya, Souvik Chakraborty, A Batty Shaw, S. Patra, Rajia Khatun

2025Biomedical & Pharmacology Journal7 citationsDOIOpen Access PDF

Abstract

Histamine-mediated allergic reactions are central to the pathogenesis of various allergic disorders, involving complex molecular mechanisms. Cetirizine, a second-generation antihistamine, functions as a potent H1 receptor antagonist and is widely utilized for the management of these conditions. This review comprehensively evaluated the molecular mechanisms underlying histamine release, its interaction with H1 receptors, and the subsequent allergic responses. It also analyzed the pharmacokinetics and pharmacodynamics of cetirizine, highlighting its high selectivity for H1 receptors and its minimal sedative effects. The clinical efficacy of cetirizine was demonstrated across several allergic conditions, including food allergies, atopic dermatitis, allergic conjunctivitis, and drug-induced hypersensitivities. In these contexts, cetirizine reduced histamine-mediated symptoms, such as pruritus and inflammation, and improved patient outcomes. Additionally, combination therapies involving cetirizine with other antihistamines, corticosteroids, or biologics were discussed, particularly in refractory or severe allergic cases. Despite its overall safety, this review also highlighted the adverse effects associated with long-term cetirizine use, particularly in special populations such as pediatric, elderly, and patients with renal impairment. Future perspectives emphasize the role of future research on cetirizine in personalized allergy treatment, emerging combination therapies with biologics, and its potential in prophylactic applications.

Topics & Concepts

CetirizineHistamineAllergyMedicineMechanism (biology)Allergic reactionDesensitization (medicine)ImmunologyPharmacologyInternal medicinePhilosophyReceptorEpistemologyMast cells and histaminePhenothiazines and Benzothiazines Synthesis and ActivitiesDrug-Induced Adverse Reactions