Suppression of wheal and flare in histamine test by the main H1 antihistamines commercialized in Brazil

Abstract

BackgroundSeveral dermatoses are mediated by histamine, such as urticaria, angioedema, and papular urticaria. There are no Brazilian studies comparing the potency of antihistamines.ObjectivesTo evaluate the tolerability and efficacy of the main commercial brand and generic H1 antihistamines, regarding the suppression of the wheal and flare to the histamine test.MethodsA quasi-experimental, open study with 10 healthy adults submitted to the histamine test on the ventral aspect of the forearms. After 20 minutes, wheal and flares were measured. The tests were performed after two hours of intake of dexchlorpheniramine, hydroxyzine, levocetirizine, fexofenadine, cetirizine, loratadine, ebastine, desloratadine, epinastine and rupatadine, as well as generics of loratadine, cetirizine and fexofenadine.ResultsAll antihistamines presented a reduction in the wheal compared to the control (p <0.02), as well as in the flare, except for rupatadine (p = 0.70). In the internal comparison, cetirizine, fexofenadine, epinastine, levocetirizine, dexchlorpheniramine and hydroxyzine were the most potent, with no difference between them (p > 0.1). As for halo, cetirizine, epinastine, hydroxyzine and fexofenadine were the most potent, with no difference between them (p > 0.1). The most common adverse effect was drowsiness, which was more prevalent among first-generation drugs (p < 0.01). Generic loratadine, fexofenadine and cetirizine halos were higher than their controls (p <0.03)..Study limitationsA single-center study evaluating only aspects related to histamine.ConclusionsBrazilian commercial antihistamines presented different profiles of inhibition of wheal and flares in the histamine test, as well as adverse effects. Generic loratadine, fexofenadine and cetirizine presented larger flares than brand drugs.

Insights into urticaria in pediatric and adult populations and its management with fexofenadine hydrochloride

“…A recent meta-analysis performed by Huang et al, found that antihistamine effect of fexofenadine HCl was significantly higher than that of placebo (p < 0.00001, both flare and wheal), and non-inferior to other second-generation antihistamines (flare, p = 0.84; wheal, p = 0.21) based on the analysis of five studies on healthy subjects [ 64 ]. In a recent study conducted in Brazil, 10 healthy adults were subjected to the histamine test to compare the effect of the H 1 -antihistamines most used in the local clinical practice (dexchlorpheniramine, hydroxyzine, levocetirizine, fexofenadine HCl, cetirizine, loratadine, ebastine, desloratadine, epinastine and rupatadine) [ 65 ]. Two hours after intake, all antihistamines including fexofenadine HCl resulted in a significant reduction in the wheal (p < 0.02) as well as in the flare compared to control [ 65 ].…”

“…In a recent study conducted in Brazil, 10 healthy adults were subjected to the histamine test to compare the effect of the H 1 -antihistamines most used in the local clinical practice (dexchlorpheniramine, hydroxyzine, levocetirizine, fexofenadine HCl, cetirizine, loratadine, ebastine, desloratadine, epinastine and rupatadine) [ 65 ]. Two hours after intake, all antihistamines including fexofenadine HCl resulted in a significant reduction in the wheal (p < 0.02) as well as in the flare compared to control [ 65 ]. Fexofenadine HCl 180 mg compared with desloratadine 5 mg significantly reduced histamine-induced flares (61% versus + 2%, respectively: p < 0.05) and wheals (p < 0.05) at 2 h after treatment in adults and adolescents [ 66 ].…”

“…It has been shown that treatment with fexofenadine HCl improves health-related QoL and does not interfere with work productivity or performance of daily activities in patients with chronic urticaria [ 73 , 74 ]. Table 4 summarizes the studies investigating the efficacy and QoL of fexofenadine HCl [ 65 – 71 , 73 – 76 ].…”

Ameliorating Effects of Delphinol&#174;, Anthocyanin Standardized Maqui Berry Extract, on Skin Brightness and Redness in Japanese Females: A Randomized Double-Blind Placebo-Controlled Pilot Study

“…The anti-oxidant effects are most likely related, in addition to the photoprotective effects of Delphinol® [26] because anthocyanins can suppress allergic inflammatory responses in mast cells [40]. Released histamine induces skin flare [41]. The anti-oxidant effects of Del-phinol® are involved because oxidative stress induces skin inflammation [42] and redness.…”

Angioedema and Fatty Acids

“…Histamine plays important physiological roles mediated through three histamine receptors, H1, H2 and H3, which belong to G protein-coupled receptors [19]. The H1 receptor is a representative histamine receptor that causes urticaria, and mediates wheal formation and vascular permeability [20,21]. Histamine is a relevant vasoactive derived from mast-cell degranulation, and the H1 receptor leads to vasodilatation and enhances blood flow [22].…”