Mizolastine was marketed in Germany and Switzerland as Mizollen for
the symptomatic relief of seasonal and perennial allergic rhinoconjunctivitis and
urticaria. Mizolastine is a new long-acting, orally active antihistaminic agent with
a rapid onset of action ; the two most recent H1 antagonists launched were
fexofenadine, metabolite of terfenadine (Sepracor, 1996) and Olopatadine
(Kyowa Hakko, 1997). Mizolastine can be prepared in 2 steps from 2-chloro 1-
(4-fluorobenzyl)benzimidazole by successive condensations of appropriate
amine and thioether. Mizolastine selectively blocks the peripheral H1 receptors
(but not the serotonergic, noradrenergic, muscarinic receptors) with a minimal
occupancy of brain receptors, and therefore does not elicit any sedative effects.
Moreover, Mizolastine does not produce cardiac rhythm disorders which have
been associated with certain non-sedating antihistamines in humans.
화학적 성질
White Solid
용도
A highly selective histamine H1-receptor antagonist (with no anticholinergic, antiadrenergic, or antiserotonin activity) for use in the treatment of allergic disorders, especially rhinitis and urticaria.
