Bilastine: a guide to its use in the treatment of symptomatic allergic rhinoconjunctivitis and urticaria
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Bilastine: a guide to its use in the treatment of symptomatic allergic rhinoconjunctivitis and urticaria Katherine A. Lyseng-Williamson and Natalie J. Carter Adis, Auckland, New Zealand
Bilastine, a new antihistamine, is indicated for the symptomatic treatment of seasonal or perennial allergic rhinoconjunctivitis and urticaria in many European countries. In clinical trials, the efficacy of bilastine in these indications was similar to that of other second-generation antihistamines. Bilastine is well tolerated, with an overall tolerability profile similar to that of placebo.
What is the rationale for developing the drug? Allergic rhinoconjunctivitis (characterized by rhinitis and conjunctivitis) and urticaria (characterized by wheals and angioedema) are common allergic disorders.[1,2] The activity of histamine at histamine H1 receptors plays an important role in the pathophysiology of these conditions.[1,2] Antihistamines, which are functionally classified as first- or second-generation antihistamines, are the mainstay of treatment of allergic disorders.[1-3] Because first-generation antihistamines are readily transported across the blood-brain barrier, these drugs are frequently associated with CNS adverse effects (e.g. drowsiness, sedation, somnolence, and impaired cognitive function and psychomotor performance). Moreover, first-generation antihistamines have poor receptor selectivity and may act on other receptor types to cause adverse effects (e.g. antimuscarinic and antiserotonin effects).[1] In contrast, second-generation antihistamines have limited penetration across the blood-brain barrier, as a result of P-glycoprotein-mediated efflux of the drug from the CNS and low lipid solubility.[1] As a result, second-generation agents are less sedating than the first-generation agents. Adis Evaluation What are the key clinical benefits of bilastine in symptomatic allergic rhinoconjunctivitis and urticaria? Reduces the symptoms of allergic rhinoconjunctivitis and chronic idiopathic urticaria Improves disease-related quality of life Overall tolerability profile is similar to that of placebo Incidence of somnolence is similar to that of placebo and significantly lower than that of cetirizine Does not affect CNS function or the ability to drive Not associated with cardiac adverse effects Does not interfere with the cytochrome P450 enzyme system
Second-generation agents are also more selective for H1 receptors and, hence, are not associated with adverse events arising from interactions at other receptor types. For these reasons, treatment guidelines recommend the use of secondgeneration antihistamines as first-line treatment for symptomatic control in allergic rhinoconjunctivitis[3] and urticaria.[2] However, some new adverse events have been observed in patients receiving certain second-generation antihistamines, including potentially life-threatening cardiotoxicity.[1,2] In addition, some second-generation agents, particularly when administered at high doses, may still penetrate the blood-brain barrier and cause some
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