Rupatadine – a panacea for allergies? A literature review

Abstract

Allergic diseases are one of the most common chronic diseases. The incidence of allergies is constantly increasing, and it is currently estimated that around 40% of the population suffers from at least one allergy. Current guidelines for the treatment of allergic rhinoconjunctivitis and urticaria recommend modern second-generation antihistamines. Rupatadine is the first hybrid molecule with high affinity for the H1 receptor resulting from remarkably strong binding to this receptor. It exhibits significant H1 receptor binding selectivity, greater in the lungs than in the cerebellum. It has antihistamine effect that is about 25 and 75 times stronger than that of cetirizine and loratadine, respectively. The second mechanism of its action is a strong antagonism of the platelet-activating factor (PAF) receptor. Rupatadine is rapidly absorbed, which correlates with the onset of anti-H1 and anti-PAF activity. Rupatadine is approximately 99% bound to plasma proteins, but at the same time it is very well distributed to other tissues. It undergoes metabolism in the liver through oxidative processes and glucuronide conjugation. Many studies indicate that rupatadine (10 mg) was at least as effective as desloratadine, cetirizine, loratadine and ebastine in reducing allergic symptoms in allergic rhinitis and urticaria. It has also been confirmed to be effective in relieving the symptoms of insect bite response. Rupatadine has a positive effect on the daily functioning of patients with allergic rhinitis and urticaria, and improves the quality of life of these people. At the same time, many cross-sectional studies have shown that rupatadine has a good safety and tolerability profile in adults and children and has not shown adverse cardiovascular effects.