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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

Intracellular signaling processes mediated by G-proteins after interaction of histamine with each receptor subtype.Abbreviations: AC, adenylate cyclase; Akt, protein kinase B; cAMP, cyclic adenosine monophosphate; CREB, cAMP response element-binding protein; DAG, diacyl glycerol; IP3, inositol triphosphate; MAPK, mitogen-activated protein kinase; PI3K, phosphoinositide 3-kinase; PKA, protein kinase A; PKC, protein kinase C; PLC, phospholipase C.
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f1-tcrm-12-585: Intracellular signaling processes mediated by G-proteins after interaction of histamine with each receptor subtype.Abbreviations: AC, adenylate cyclase; Akt, protein kinase B; cAMP, cyclic adenosine monophosphate; CREB, cAMP response element-binding protein; DAG, diacyl glycerol; IP3, inositol triphosphate; MAPK, mitogen-activated protein kinase; PI3K, phosphoinositide 3-kinase; PKA, protein kinase A; PKC, protein kinase C; PLC, phospholipase C.

Mentions: Four principal histamine receptor subtypes exist: H1, H2, H3, and H4. These are G-protein-coupled receptors that transfer extracellular signals via G proteins, which act as intermediaries between cell surface receptors and intracellular second messengers (Figure 1).5,30 H1 and H2 receptors are widely distributed throughout the body, but the H3 subtype is mainly located in the central nervous system (CNS) and the H4 subtype in hematopoietic tissues.30 The allergic response is primarily mediated by the H1 receptor subtype.


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)

Intracellular signaling processes mediated by G-proteins after interaction of histamine with each receptor subtype.Abbreviations: AC, adenylate cyclase; Akt, protein kinase B; cAMP, cyclic adenosine monophosphate; CREB, cAMP response element-binding protein; DAG, diacyl glycerol; IP3, inositol triphosphate; MAPK, mitogen-activated protein kinase; PI3K, phosphoinositide 3-kinase; PKA, protein kinase A; PKC, protein kinase C; PLC, phospholipase C.
© Copyright Policy
Related In: Results  -  Collection

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

f1-tcrm-12-585: Intracellular signaling processes mediated by G-proteins after interaction of histamine with each receptor subtype.Abbreviations: AC, adenylate cyclase; Akt, protein kinase B; cAMP, cyclic adenosine monophosphate; CREB, cAMP response element-binding protein; DAG, diacyl glycerol; IP3, inositol triphosphate; MAPK, mitogen-activated protein kinase; PI3K, phosphoinositide 3-kinase; PKA, protein kinase A; PKC, protein kinase C; PLC, phospholipase C.
Mentions: Four principal histamine receptor subtypes exist: H1, H2, H3, and H4. These are G-protein-coupled receptors that transfer extracellular signals via G proteins, which act as intermediaries between cell surface receptors and intracellular second messengers (Figure 1).5,30 H1 and H2 receptors are widely distributed throughout the body, but the H3 subtype is mainly located in the central nervous system (CNS) and the H4 subtype in hematopoietic tissues.30 The allergic response is primarily mediated by the H1 receptor subtype.

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