Targeting Histamine Receptors in Irritable Bowel Syndrome: A Critical Appraisal

Abstract

Irritable bowel syndrome is a group of functional gastrointestinal disorders with not yet fully clarified etiology. Recent evidence suggesting that mast cells may play a central role in the pathogenesis of irritable bowel syndrome paves the way for agents targeting histamine receptors as a potential therapeutic option in clinical treatment. In this review, the role of histamine and histamine receptors is debated. Moreover, the clinical evidence of anti-histamine therapeutics in irritable bowel syndrome is discussed.

Editorial

“…La importancia de los receptores PAR es que pueden activarse por proteasas derivadas de células inmunitarias, mastocitos y bacterias, que pueden desencadenar inflamación de bajo grado y síntomas del SII. El artículo revisa también el papel de los mastocitos y la histamina, para los cuales agentes como el ketotifeno y el cromoglicato disódico se han estudiado para el control del dolor debido a su efecto estabilizador de la degranulación de los mastocitos 14 . Por supuesto, el artículo se refiere también al efecto del estrés y la microbiota sobre el dolor visceral.…”

Recent advances in the pathophysiology of visceral pain in irritable bowel syndrome

“…Increased mucosal MC populations have been observed in the colon and rectal biopsies from IBS patients 32 . MC stabilizers (ketotifen and disodium cromoglycate) and histamine-1 receptor antagonist have been shown to significantly ameliorate symptoms and visceral pain suffered by IBS patients 33 . More recently, it has been demonstrated that histamine-1 receptor-mediated sensitization of TRPV1 promotes visceral pain and symptoms in patients with IBS and they were able to reduce this pain with a selective histamine-1 receptor antagonist 34 .…”

Probiotics in digestive, emotional, and pain-related disorders

“…Whereas in organic diseases pain may be present, probably as a consequence of the inflammatory condition itself, in FGID pain is present but its aetiology is not so clear: it may be related to motility alterations and/or to micro-or low-grade inflammation [i.e., mastocytosis, that could be treated with anti-histamine drugs: (Fabisiak et al, 2017)] that only recently is being considered [see for example (Holtmann et al, 2016) for a recent review on IBS pathophysiology]. First, we will provide some recent examples of studies about probiotics potential to treat three main organic disorders: gastric ulcer (and infection by H. pylori); IBD; GI cancer.…”