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Rupatadine is a non-sedative antagonist of histamine H1-receptors with a lengthy half-life. It also inhibits platelet activating factor (PAF) (PAF). Histamine and PAF both produce broncho constriction, which increases vascular permeability and serves as a mediator in the inflammatory process.Rupatadine has a better therapeutic impact than a single antihistamine because of its dual mechanism of action. Rupatadine also inhibits mast cell degranulation triggered by immunological and non-immune stimuli, as well as the production of cytokines, including tumor necrosis factor alpha () in human mastocytes and monocytes.

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Rupadin