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説明

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.