Non sedating antihistamine
The effects of histamines are mediated through several receptors including H1, H2, H3, and H4 receptors that belong to the superfamily of G-protein-coupled receptors .The biological effects of histamine in the allergic reaction are mediated through H1 receptors that coexist in active and inactive forms of g-protein-coupled receptors which balance each other.Bilastine has not been derived structurally from other antihistamines.It belongs to the piperidine class of antihistamines as do loratadine, desloratadine, and fexofenadine (Figure 1).Therefore, it is recommended that bilastine is taken at least one hour before and no sooner than two hours after a meal.Clinical studies sponsored by the manufacturer have shown that bilastine 20 mg once daily is as efficacious as other nonsedating antihistamines in allergic rhinoconjunctivitis and chronic urticaria in individuals from 12 and 18 years of age, respectively.The affinity for the H1 receptor is 3 and 6 times higher than for cetirizine and fexofenadine, respectively.In vivo studies in rats have demonstrated reduction in histamine-stimulated smooth muscular contraction, bronchospasms, endothelial permeability, and microvascular extravasation .
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Important pharmacokinetic parameters for non-sedating antihistamines and recommended doses in patients ≥12 years of age are listed in Table 1 [10–13].Bilastine is efficacious in all nasal symptoms including obstruction and in eye symptoms.
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