A study comparing the inhibitory effects of single and repeated oral doses of ebastine and fexofenadine against histamine-induced skin reactivity.
OBJECTIVE
The aim of this double-blind, randomized, crossover, placebo-controlled clinical trial was to compare the inhibition of the histamine-induced skin reaction induced by ebastine 20 mg with respect to that induced by fexofenadine 120 mg or placebo.


METHODS
Eighteen volunteers (10 males, 8 females) received the three treatments once daily for 5 days, with a mean 7-day washout period between treatments. Intradermal tests, using 0.05 ml from a solution containing 100 microg/ml of histamine, were performed at baseline and at 1, 1.5, 2, 3, 10 and 24 h after a single dose and repeated 5-day dose, and in addition after 34, 48, 58 and 72 h after repeated 5-day dose.


RESULTS
After 24 h of acute administration, ebastine 20 mg was significantly more effective than fexofenadine 120 mg in reducing the wheal and flare induced by histamine challenge (p<0.001). Although fexofenadine 120 mg had the shortest onset of action (1.5 vs. 3 h in ebastine 20 mg), the duration of its antihistamine effect was the shortest (24 vs. 58 h in ebastine 20 mg) and wheal reduction after 24 h was not significantly different from placebo. The overall effect after single and repeated 5-day dose, expressed as the AUC of reduction of wheal and flare area (%/h), showed the following order of magnitude: ebastine 20 mg>fexofenadine 120 mg>placebo. No significant differences in the incidence of adverse events were found between the three treatments.


CONCLUSIONS
The present results clearly show a superior and long-acting effect of ebastine 20 mg compared with fexofenadine 120 mg on the skin response to histamine 24 h after dosing.
Barbanoj
M J
MJ
Centre d'Investigació de Medicaments, Institut de Recerca; Servei de Farmacologia Clínica, Hospital de la Santa Creu i Sant Pau, Departament de Farmacologia i Terapèutica, Universitat Autònoma de Barcelona, Barcelona, España. mbarbanoj@hsp.santpau.es
Antonijoan
R M
RM
García-Gea
C
C
Morte
A
A
Gich
I
I
Gispert
J
J
Garcia
E
E
Esbrí
R
R
Luria
X
X
D000284:Administration, Oral; D000293:Adolescent; D000328:Adult; D002090:Butyrophenones / Q000008:administration & dosage / Q000009:adverse effects / Q000494:pharmacology*; D004311:Double-Blind Method; D005260:Female; D006633:Histamine Antagonists / Q000494:pharmacology*; D006801:Humans; D008297:Male; D008875:Middle Aged; D010880:Piperidines / Q000008:administration & dosage / Q000009:adverse effects / Q000494:pharmacology*; D012867:Skin / Q000187:drug effects* / Q000276:immunology; D016593:Terfenadine / Q000008:administration & dosage / Q000009:adverse effects / Q000031:analogs & derivatives* / Q000494:pharmacology*
D002090:Butyrophenones; D006633:Histamine Antagonists; D010880:Piperidines; D016593:Terfenadine; C093230:fexofenadine; C058249:ebastine