Comparative wheal and flare study of mizolastine vs terfenadine, cetirizine, loratadine and placebo in healthy volunteers.
1. Mizolastine, a new benzimidazole derivative with potent selective, non-sedative H1-histamine antagonist activity was compared with terfenadine, cetirizine and loratadine using the histamine-induced wheal and flare model in healthy volunteers. 2. Study design was a five way double-blind crossover design using a single dose of mizolastine 10 mg, terfenadine 120 mg, cetirizine 10 mg, loratadine 10 mg and placebo. 3. Histamine tests were performed on 10 occasions up to +24 h after dosing using an intradermal injection of histamine 2 micrograms with concommittant contralateral injection of a saline control. 4. Mizolastine, terfenadine, cetirizine and loratadine significantly (P < 0.001 vs placebo) inhibited the wheal and flare formation starting 1 to 2 h after dosing up to 24 h after dosing. 5. Mizolastine was significantly more active than loratadine on the wheal (P < 0.01) and flare (P < 0.05) inhibition from 3 up to 6 and 8 h respectively, as active as terfenadine on both parameters and as active as cetirizine on wheal inhibition while less active (P < 0.01) than cetirizine on flare inhibition at 2 and 12 h post-dosing.
Rosenzweig
P
P
Synthélabo Recherche (LERS), Bagneux, France.
Caplain
H
H
Chaufour
S
S
Ulliac
N
N
Cabanis
M J
MJ
Thebault
J J
JJ
D000328:Adult; D001562:Benzimidazoles / Q000494:pharmacology*; D017332:Cetirizine / Q000494:pharmacology; D018592:Cross-Over Studies; D004311:Double-Blind Method; D006634:Histamine H1 Antagonists / Q000494:pharmacology*; D006801:Humans; D006969:Hypersensitivity, Immediate / Q000188:drug therapy*; D017336:Loratadine / Q000494:pharmacology; D008297:Male; D016593:Terfenadine / Q000494:pharmacology
D001562:Benzimidazoles; D006634:Histamine H1 Antagonists; C076170:mizolastine; D017336:Loratadine; D016593:Terfenadine; D017332:Cetirizine