Effects of Bepotastine and Fexofenadine on Histamine-Induced Flare, Wheal and Itch

Abstract

Background: Urticaria is mainly caused by mast cell-derived histamine through the histamine H₁ receptor. Antihistamines are occasionally used on demand upon a recurrence of urticaria; therefore, rapidly acting agents should be explored. The onset of action is assumed to depend on time to maximum concentration (T_max), but the speed of action needs to be evaluated not only through blood concentration analysis but also by measuring in vivo effectiveness. Methods: In this study, we chose two representative second-generation antihistamines (bepotastine and fexofenadine) with relatively short T_max values and evaluated their effects on histamine-induced skin responses using both visual and laser Doppler imaging scales. Results: Suppression of histamine-induced flare and itch was observed 3 and 6 h after administration of both antihistamines. Attenuation of itch was seen 30 min after the administration of each drug and thereafter until 6 h. In addition, bepotastine suppressed flare formation after only 30 min following application. Conclusion: These results suggest that antihistamines suppress histamine-induced itch and flare, followed by wheal formation, and that bepotastine suppresses skin symptoms sooner after administration than fexofenadine does, which is relatively consistent with the T_max results.

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

“…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 ]. Other studies of H 1 -antihistamines with slightly different methodologies confirmed similar results regarding the efficacy of fexofenadine HCl in the suppression of the induced wheal [ 67 , 68 ].…”

Randomized Controlled Study Comparing the Efficacy and Tolerance of Bepotastine, a New 2nd Generation Antihistamine, to Fexofenadine, in Symptomatic Relief of Patients with Pruritic Cutaneous Disorders

“…Though, till date to our knowledge there is no published study which compares the clinical symptomatic improvement of Bepotastine in patients with cutaneous pruritic disorders to Fexofenadine, the following comparative studies with Fexofenadine are available. The first compares Bepotastine to Fexofenadine to evaluate the attenuation of histamine induced itch at 30 min after the administration of each drug and thereafter until 6 h. Bepotastine suppressed flare formation after only 30 min following drug administration which was sooner than Fexofenadine [12]. A double-blind, placebo-controlled, crossover study to compare the inhibitory effects of Bepotastine, Cetirizine, Fexofenadine, and Olopatadine yielded significant reduction of histamine-induced wheal-and flare response compared to placebo (P<0.01) with the strongest suppression with Olopatadine.…”

A Double Dose of Levocetirizine Leads to Better Control of Histamine-Induced Flare, Wheal and Itch in Healthy Donors

“…The maximum (r 1 ) and orthogonal diameters (r 2 ) were visually measured and the flare and wheal areas were calculated as r 1 /2 × r 2 /2 × 3.14. In addition, changes in skin blood flow were assessed using a moorLDI2 imager (Moor Instruments Ltd., Axminster, UK), and flare areas were calculated from the calibrated images using the manufacturer's software [7]. Responses to the test stimuli were assessed before and 1, 3, 6, 12 and 24 h after administration of the medication.…”