Rupatadine is a long-acting, non-sedative antagonist of histamine H1-receptor. It also antagonizes the platelet-activating factor (PAF). Both histamine and PAF cause bronchoconstriction which leads to an increase in the vascular permeability and act as a mediator in the inflammatory process. Rupatadine possesses other anti-allergic properties such as the inhibition of the degranulation of mast cells induced by immunological and non-immunological stimuli and inhibition of the release of cytokines, particularly of the tumor necrosis factor alpha (TNFα) in human
mastocytes and monocytes.