Desloratadine: A new, nonsedating. oral antihistamine

Desloratadine is a new, selective, H-1-receptor antagonist that also has an ti-inflammatory activity. In vitro studies have shown that desloratadine in hibits the release or generation of multiple inflammatory mediators, includ ing IL-4, IL-6, IL-8, IL-13, PGD(2), leukotriene C-4, tryptase, histamine, and the TNF-alpha -induced chemokine RANTES, Desloratadine also inhibits th e induction of cell adhesion molecules, platelet-activating factor-induced eosinophil chemotaxis, TNF-alpha -induced eosinophil adhesion, and spontane ous and phorbol myristate acetate-induced superoxide generation in vitro. I n animals desloratadine had no effect on the central nervous, cardiovascula r. renal, or gastrointestinal systems. Desloratadine is rapidly absorbed, h as dose-proportional pharmacokinetics, and has a half-life of 27 hours, The absorption of desloratadine is not affected by food, and the metabolism an d elimination are not significantly affected by the subject's age, race, or sex, There are no clinically relevant interactions between desloratadine a nd erythromycin, ketoconazole, or grapefruit juice. Desloratadine is not a significant substrate of the P-glycoprotein transport system, Once daily ad ministration of desloratadine rapidly reduces the nasal and nonnasal sympto ms of seasonal allergic rhinitis, including congestion. In patients with se asonal allergic rhinitis and concomitant asthma, desloratadine treatment wa s also associated with significant reductions in total asthma symptom score and use of inhaled Pz-agonists, Use of desloratadine in patients with chro nic idiopathic urticaria was associated with significant reductions in prur itus, number of hives, size of the largest hive, and interference with slee p and daily activities. Clinical experience in over 2300 patients has shown that the adverse event profile of desloratadine is similar to that of plac ebo; desloratadine has no clinically relevant effects on electrocardiograph ic parameters, does not impair wakefulness or psychomotor performance, and does not exacerbate the psychomotor impairment associated with alcohol use.