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Treatment of allergic rhinitis and urticaria: a review of the newest antihistamine drug bilastine.

Wang XY, Lim-Jurado M, Prepageran N, Tantilipikorn P, Wang de Y - Ther Clin Risk Manag (2016)

Bottom Line: This agent does not interact with the cytochrome P450 system and does not undergo significant metabolism in humans, suggesting that it has very low potential for drug-drug interactions, and does not require dose adjustment in renal impairment.It has also shown significant efficacy (similar to that of cetirizine) and safety in the long-term treatment of perennial allergic rhinitis.Bilastine is generally well tolerated, both at standard and at supratherapeutic doses, appears to have less sedative potential than other second-generation antihistamines, and has no cardiotoxicity.

View Article: PubMed Central - PubMed

Affiliation: Department of Allergy, Beijing Shijitan Hospital, Capital Medical University, Beijing, People's Republic of China.

ABSTRACT
Allergic rhinitis and urticaria are common allergic diseases that may have a major negative impact on patients' quality of life. Bilastine, a novel new-generation antihistamine that is highly selective for the H1 histamine receptor, has a rapid onset and prolonged duration of action. This agent does not interact with the cytochrome P450 system and does not undergo significant metabolism in humans, suggesting that it has very low potential for drug-drug interactions, and does not require dose adjustment in renal impairment. As bilastine is not metabolized and is excreted largely unchanged, hepatic impairment is not expected to increase systemic exposure above the drug's safety margin. Bilastine has demonstrated similar efficacy to cetirizine and desloratadine in patients with seasonal allergic rhinitis and, in a Vienna Chamber study, a potentially longer duration of action than fexofenadine in patients with asymptomatic seasonal allergic rhinitis. It has also shown significant efficacy (similar to that of cetirizine) and safety in the long-term treatment of perennial allergic rhinitis. Bilastine showed similar efficacy to levocetirizine in patients with chronic spontaneous urticaria and can be safely used at doses of up to fourfold higher than standard dosage (80 mg once daily). The fourfold higher than standard dose is specified as an acceptable second-line treatment option for urticaria in international guidelines. Bilastine is generally well tolerated, both at standard and at supratherapeutic doses, appears to have less sedative potential than other second-generation antihistamines, and has no cardiotoxicity. Based on its pharmacokinetic properties, efficacy, and tolerability profile, bilastine will be valuable in the management of allergic rhinitis and urticaria.

No MeSH data available.


Related in: MedlinePlus

Efficacy of increased dosages of second-generation antihistamines in chronic urticaria.Note: Adapted from Sanchez-Borges M, Ansotegui I, Jimenez JM, Rojo MI, Serrano C, Yañez A. Comparative efficacy of non-sedating antihistamine updosing in patients with chronic urticaria. World Allergy Organ J. 2014;7:33.22
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f9-tcrm-12-585: Efficacy of increased dosages of second-generation antihistamines in chronic urticaria.Note: Adapted from Sanchez-Borges M, Ansotegui I, Jimenez JM, Rojo MI, Serrano C, Yañez A. Comparative efficacy of non-sedating antihistamine updosing in patients with chronic urticaria. World Allergy Organ J. 2014;7:33.22

Mentions: A comparison of clinical trial data for second-generation antihistamines in chronic urticaria suggests that this bilastine dosage (80 mg/d) is significantly more effective than supratherapeutic dosages of desloratadine and levocetirizine (Figure 9).22 However, use of these compounds at four times higher than standard doses is certain to raise safety concerns among some physicians. For instance, the sedative potential of cetirizine, desloratadine, and loratadine will likely be markedly greater than that of bilastine, fexofenadine, and levocetirizine.5,40 Concerns at high dosage may also manifest about the potential for QTc prolongation, particularly given the unfavorable history of astemizole and terfenadine.31 However, bilastine at therapeutic and supratherapeutic doses in healthy volunteers had no significant influence on ventricular repolarization. Bilastine doses of 20 mg and 100 mg had no clinically significant effect on QTc interval. Bilastine 20 mg was also administered with ketoconazole and had no effect on QTc interval when used in combination.42


Treatment of allergic rhinitis and urticaria: a review of the newest antihistamine drug bilastine.

Wang XY, Lim-Jurado M, Prepageran N, Tantilipikorn P, Wang de Y - Ther Clin Risk Manag (2016)

Efficacy of increased dosages of second-generation antihistamines in chronic urticaria.Note: Adapted from Sanchez-Borges M, Ansotegui I, Jimenez JM, Rojo MI, Serrano C, Yañez A. Comparative efficacy of non-sedating antihistamine updosing in patients with chronic urticaria. World Allergy Organ J. 2014;7:33.22
© Copyright Policy
Related In: Results  -  Collection

License 1 - License 2
Show All Figures
getmorefigures.php?uid=PMC4835134&req=5

f9-tcrm-12-585: Efficacy of increased dosages of second-generation antihistamines in chronic urticaria.Note: Adapted from Sanchez-Borges M, Ansotegui I, Jimenez JM, Rojo MI, Serrano C, Yañez A. Comparative efficacy of non-sedating antihistamine updosing in patients with chronic urticaria. World Allergy Organ J. 2014;7:33.22
Mentions: A comparison of clinical trial data for second-generation antihistamines in chronic urticaria suggests that this bilastine dosage (80 mg/d) is significantly more effective than supratherapeutic dosages of desloratadine and levocetirizine (Figure 9).22 However, use of these compounds at four times higher than standard doses is certain to raise safety concerns among some physicians. For instance, the sedative potential of cetirizine, desloratadine, and loratadine will likely be markedly greater than that of bilastine, fexofenadine, and levocetirizine.5,40 Concerns at high dosage may also manifest about the potential for QTc prolongation, particularly given the unfavorable history of astemizole and terfenadine.31 However, bilastine at therapeutic and supratherapeutic doses in healthy volunteers had no significant influence on ventricular repolarization. Bilastine doses of 20 mg and 100 mg had no clinically significant effect on QTc interval. Bilastine 20 mg was also administered with ketoconazole and had no effect on QTc interval when used in combination.42

Bottom Line: This agent does not interact with the cytochrome P450 system and does not undergo significant metabolism in humans, suggesting that it has very low potential for drug-drug interactions, and does not require dose adjustment in renal impairment.It has also shown significant efficacy (similar to that of cetirizine) and safety in the long-term treatment of perennial allergic rhinitis.Bilastine is generally well tolerated, both at standard and at supratherapeutic doses, appears to have less sedative potential than other second-generation antihistamines, and has no cardiotoxicity.

View Article: PubMed Central - PubMed

Affiliation: Department of Allergy, Beijing Shijitan Hospital, Capital Medical University, Beijing, People's Republic of China.

ABSTRACT
Allergic rhinitis and urticaria are common allergic diseases that may have a major negative impact on patients' quality of life. Bilastine, a novel new-generation antihistamine that is highly selective for the H1 histamine receptor, has a rapid onset and prolonged duration of action. This agent does not interact with the cytochrome P450 system and does not undergo significant metabolism in humans, suggesting that it has very low potential for drug-drug interactions, and does not require dose adjustment in renal impairment. As bilastine is not metabolized and is excreted largely unchanged, hepatic impairment is not expected to increase systemic exposure above the drug's safety margin. Bilastine has demonstrated similar efficacy to cetirizine and desloratadine in patients with seasonal allergic rhinitis and, in a Vienna Chamber study, a potentially longer duration of action than fexofenadine in patients with asymptomatic seasonal allergic rhinitis. It has also shown significant efficacy (similar to that of cetirizine) and safety in the long-term treatment of perennial allergic rhinitis. Bilastine showed similar efficacy to levocetirizine in patients with chronic spontaneous urticaria and can be safely used at doses of up to fourfold higher than standard dosage (80 mg once daily). The fourfold higher than standard dose is specified as an acceptable second-line treatment option for urticaria in international guidelines. Bilastine is generally well tolerated, both at standard and at supratherapeutic doses, appears to have less sedative potential than other second-generation antihistamines, and has no cardiotoxicity. Based on its pharmacokinetic properties, efficacy, and tolerability profile, bilastine will be valuable in the management of allergic rhinitis and urticaria.

No MeSH data available.


Related in: MedlinePlus