It acts as a long-acting, non-sedative antagonist of histaminergic H1-receptors and also antagonizes the platelet-activating factor (PAF). This double mechanism of action gives Rupatadine a special isolated antihistamine action. Both histamine and PAF cause bronchoconstriction and lead to an increase in the vascular permeability, acting as a mediator in the inflammatory process, which is responsible for the bronchial
hyperactivity. Rupatadine has other anti-allergic properties, such as inhibition of
mastocytes, degranulation, induced by the immunological and non-immunological stimuli and inhibition of the release of cytokines, particularly of the tumor necrosis factor alpha
(TNF-alpha) in human mastocytes and monocytes.
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