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Desloratadine
See also Antihistamines
General information
Desloratadine is the primary metabolite of loratadine, with superior H1 receptor binding, potent antihistaminic activity compared with the parent compound, and proven efficacy in allergic disease [ ]. It is effective and well tolerated in seasonal allergic rhinitis, including relief of nasal congestion [ ].
In a randomized, open, four-way, crossover study in 20 healthy men desloratadine was given as single doses (5, 7.5, 10, and 20 mg) in four different treatment periods with 14 days between each dose. The C max for all doses occurred at 4 hours after administration, with a half-life of 21–24 hours. There were no dose-related differences in drug absorption rate, and even the 20 mg dose was well tolerated [ ]. The systemic availability of desloratadine was unaffected by food in healthy adult volunteers [ ].
Organs and systems
Cardiovascular
In a large, multicenter, double-blind, placebo-controlled, parallel-group study of the efficacy and tolerability of desloratadine in 346 patients with seasonal allergic rhinitis, the symptoms improved significantly and there was no significant effect on the QT c interval [ ].
In a multicenter, randomized, double-blind, placebo-controlled study in 190 patients, desloratadine was effective in the treatment of moderate to severe chronic idiopathic urticaria, with no adverse electrocardiographic effects [ ].
In healthy volunteers, 12 men and 12 women, there was no prolongation of the QT c interval after co-administration of desloratadine with erythromycin [ ].
Nervous system
Desloratadine appears to be minimally sedative, given that several studies, published in abstract, have shown no impairment in terms of wakefulness or psychomotor performance [ ]. Moreover, in a study in which desloratadine was effective and well tolerated in patients with seasonal allergic rhinitis there were no clinically significant sedative effects [ ].
Psychological, psychiatric
The results of several studies suggest that desloratadine has minimal or no effects on cognitive functions and psychomotor performance [ ].
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