Abstract
This chapter provides an overview of the pharmacological profile of mizolastine. Mizolastine is a novel histamine H1 receptor antagonist. It inhibits histamine release from activated mast cells and shows additional unique antiallergic properties at similar doses in vivo. The selectivity of mizolastine for the histamine H1receptor was determined by the pharmacological characteristics of [3H] mizolastine binding sites. Mizolastine at low doses exhibits a powerful and long-lasting anti-inflammatory action against AA-induced paw oedema. Based on the existing experimental data, the mechanism of the anti-inflammatory effect of mizolastine appears to involve the 5-LO pathway, and would exclude direct antagonism of histamine H1 receptors as terfenadine, loratadine, and pyrilamine were ineffective. Mizolastine has been shown to inhibit histamine-mediated reactions such as histamine-induced oedema, bronchoconstriction and capillary permeability. It also shows anti-allergic activity, inhibits anaphylactic reactions, prevents lethal shock, inhibits clinical signs of bronchospasm and inhibits release of histamine from activated mast cells in animals.
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