Introduction: Rupatadine is a second-generation H1-antihistamine with dual affinity for histamine H1 and PAF receptors. Rupatadine is indicated for the treatment of allergic rhinitis and urticaria.
Areas covered: A Medline search was conducted to identify preclinical and clinical studies of rupatadine. This was supplemented with additional articles obtained from online sources. The focus of this review is on the safety profile of rupatadine.
Expert opinion: The review of these data indicates that rupatadine is highly selective for histamine H1-receptors, exhibits additional PAF antagonism in in vitro and in vivo studies, does not cross the blood-brain barrier, and has similar adverse events comparable with other second-generation antihistamines. Rupatadine is a safe and well tolerated drug in patients over 2 years old, with no central nervous system or cardiovascular effects and it can be taken with or without foods.
Keywords: H1-antihistamine; H1-receptor antagonist; PAF antagonist; Rupatadine; allergic rhinitis; chronic spontaneous urticaria; intermittent; perennial; persistent; pharmacodynamics; pharmacokinetics; safety; seasonal; second-generation antihistamine; therapeutic use; urticaria.