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Use of Antihistamine Drugs in Colitis: A Review

Bogielski B, Gach D, Michalczyk K, Skrzep-Poloczek B, Stojko M, Zalejska-Fiolka J, Stygar D

Pharmaceuticals (Basel, Switzerland), 2026

Abstract

Background/Objectives: Colitis involves both local intestinal damage and systemic dysfunction, driven by oxidative stress and immune imbalance. Histamine, acting through its receptors, influences these processes, yet its therapeutic relevance in colitis remains unclear. This review systematically examines histamine-mediated signaling in colitic inflammation and evaluates preclinical and clinical data on antihistamines to assess their potential as a mechanism-based treatment. Methods: A structured literature search was conducted using PubMed and Google Scholar to identify studies addressing histamine signaling and the use of antihistamines in colitis, using keywords such as "colitis," "histamine," "histamine receptors," and "antihistamines." Relevant experimental and clinical studies were screened and critically analyzed to provide an integrated overview of mechanistic and therapeutic insights. This review was designed as a mechanistic narrative synthesis based on a structured search and qualitative appraisal rather than a formal systematic review with quantitative risk-of-bias grading. Results: Findings from preclinical investigations consistently indicate that pharmacological manipulation of histamine signaling-especially through H3 and H4 receptor subtypes-reduces inflammatory activity and modulates oxidative balance in animal models of colitis. Conversely, clinical evidence concerning H1 and H2 receptor antagonists remains scarce and discordant, lacking sufficient support…

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