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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

Affinity of bilastine to human H1 receptors expressed in HEK-293 cell.Note: Reproduced from Drugs R D, A Preclinical pharmacology of bilastine, a new selective histamine H1 receptor antagonist: receptor selectivity and in vitro antihistaminic activity, 2005;6:371–384, Corcostegui R, Labeaga L, Innerarity A, Berisa A, Orjales A,49 Copyright ©2005, With permission of Springer.
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f4-tcrm-12-585: Affinity of bilastine to human H1 receptors expressed in HEK-293 cell.Note: Reproduced from Drugs R D, A Preclinical pharmacology of bilastine, a new selective histamine H1 receptor antagonist: receptor selectivity and in vitro antihistaminic activity, 2005;6:371–384, Corcostegui R, Labeaga L, Innerarity A, Berisa A, Orjales A,49 Copyright ©2005, With permission of Springer.

Mentions: With novel antihistamines (eg, bilastine), a specific goal of in vitro studies is to confirm that the test agent has marked selectivity – high affinity for histamine H1 receptors, but minimal effects at receptors for other mediators and amines.39 Thus, bilastine (inhibition constant [Ki] 44 nM) was shown to dose-dependently inhibit 3H-pyrilamine binding to H1 receptors in the guinea pig cerebellum, with an affinity approximately threefold greater than that of cetirizine (Ki 143 nM) and fivefold greater than that of fexofenadine (Ki 246 nM).49 Similar findings were obtained in a human embryonic kidney cell line (Figure 4; Ki 64 nM).49 Additional in vitro trials demonstrated that bilastine had no significant antagonist activity at a diverse range of other receptors: H2, H3, and H4, 5-HT2A, bradykinin B1, leukotriene D4, N-type voltage-dependent calcium receptors, α1- and β2-adrenoceptors, and M1–M5 muscarinic receptors.39,49


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)

Affinity of bilastine to human H1 receptors expressed in HEK-293 cell.Note: Reproduced from Drugs R D, A Preclinical pharmacology of bilastine, a new selective histamine H1 receptor antagonist: receptor selectivity and in vitro antihistaminic activity, 2005;6:371–384, Corcostegui R, Labeaga L, Innerarity A, Berisa A, Orjales A,49 Copyright ©2005, With permission of Springer.
© Copyright Policy
Related In: Results  -  Collection

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

f4-tcrm-12-585: Affinity of bilastine to human H1 receptors expressed in HEK-293 cell.Note: Reproduced from Drugs R D, A Preclinical pharmacology of bilastine, a new selective histamine H1 receptor antagonist: receptor selectivity and in vitro antihistaminic activity, 2005;6:371–384, Corcostegui R, Labeaga L, Innerarity A, Berisa A, Orjales A,49 Copyright ©2005, With permission of Springer.
Mentions: With novel antihistamines (eg, bilastine), a specific goal of in vitro studies is to confirm that the test agent has marked selectivity – high affinity for histamine H1 receptors, but minimal effects at receptors for other mediators and amines.39 Thus, bilastine (inhibition constant [Ki] 44 nM) was shown to dose-dependently inhibit 3H-pyrilamine binding to H1 receptors in the guinea pig cerebellum, with an affinity approximately threefold greater than that of cetirizine (Ki 143 nM) and fivefold greater than that of fexofenadine (Ki 246 nM).49 Similar findings were obtained in a human embryonic kidney cell line (Figure 4; Ki 64 nM).49 Additional in vitro trials demonstrated that bilastine had no significant antagonist activity at a diverse range of other receptors: H2, H3, and H4, 5-HT2A, bradykinin B1, leukotriene D4, N-type voltage-dependent calcium receptors, α1- and β2-adrenoceptors, and M1–M5 muscarinic receptors.39,49

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