In a review of
rupatadine published in 2008, the primary focus was on its role as an
antihistamine, with a thorough evaluation of its pharmacology and interaction with
histamine H1 -receptors. At the time, however, evidence was already emerging of a broader mechanism of action for
rupatadine involving other mediators implicated in the inflammatory cascade. Over the past few years, the role of
platelet-activating factor (PAF) as a potent mediator involved in the
hypersensitivity-type
allergic reaction has gained greater recognition.
Rupatadine has dual affinity for
histamine H1 -receptors and
PAF receptors. In view of the
Allergic Rhinitis and its Impact on
Asthma group's call for oral
antihistamines to exhibit additive
anti-allergic/anti-inflammatory properties, further exploration of
rupatadine's anti-PAF effects was a logical step forward. New studies have demonstrated that
rupatadine inhibits PAF effects in nasal airways and produces a greater reduction in nasal symptoms than
levocetirizine. A meta-analysis involving more than 2500 patients has consolidated the clinical evidence for
rupatadine in allergic rhinoconjunctivitis in adults and children (level of evidence Ia, recommendation A). Other recent advances include observational studies of
rupatadine in everyday clinical practice situations and approval of a new formulation (1 mg/ml oral
solution) for use in children. In this reappraisal, we revisit some key properties and pivotal clinical studies of
rupatadine and examine new clinical data in more detail including studies that measured health-related quality of life and studies that investigated the efficacy and safety of
rupatadine in other indications such as acquired
cold urticaria, mosquito
bite allergy and
mastocytosis.