Bilastine: new insight into antihistamine treatment

Clinical and Molecular Allergy

Giorgio Walter Canonica³  Cristoforo Incorvaia²  Laura Bonzano¹  Marcello Montagni¹  Erminia Ridolo¹ 

[1] Department of Clinical and Experimental Medicine, University of Parma, via Gramsci 14, Parma 43126, Italy;Pulmonary Rehabilitation Unit, ICP Hospital, Milan, Italy;Allergy and Respiratory Diseases Clinic, DIMI, University of Genoa, IRCCS AOU San Martino-IST, Genoa, Italy

关键词: Safety;    Efficacy;    Chronic urticaria;    Allergic rhinitis;    Bilastine;    Antihistamines;   

Others  :  1171970
DOI  :  10.1186/s12948-015-0008-x

 received in 2015-01-13, accepted in 2015-02-19,  发布年份 2015

【 摘 要 】

Bilastine is a new second generation H1-antihistamine recently approved for the symptomatic treatment of allergic rhinitis (AR) and chronic urticaria (CU). Bilastine epitomizes the evolution of research on antihistamines concerning both efficacy and safety. In AR treatment, a number of large controlled clinical trials documented its efficacy, as assessed by improvement of all nasal and ocular symptoms and quality of life. These outcomes show that bilastine meets current EAACI/ARIA criteria for medications used in the treatment of AR. Also in CU, the review of the literature indicates that once-daily treatment with bilastine 20 mg was effective in managing symptoms and improving patient’s quality of life. Concerning safety and tolerability, the profile of bilastine is very similar to placebo and in particular the adverse effects on central nervous system are insignificant. The balance of efficacy and safety of bilastine is particularly helpful when dosages higher than standard are needed to control the symptoms, as frequently occurs in patients with urticaria, in whom antihistamines doses up to four times the standard dose may be administered.

【 授权许可】

   
2015 Ridolo et al.; licensee BioMed Central.

【 参考文献 】

• [1]Bousquet J, Van Cauwenberge P, Khaltaev N: ARIA Workshop Group: World health organization. Allergic rhinitis and its impact on asthma. J Allergy Clin Immunol 2001, 108(5 Suppl):S147-334.
• [2]Dykewicz MS, Fineman S: Executive summary of joint task force practice parameters on diagnosis and management of rhinitis. Ann Allergy Asthma Immunol 1998, 81:463-8.
• [3]Zuberbier T, Aberer W, Asero R, Bindslev-Jensen C, Brzoza Z, Canonica GW, et al.: The EAACI/GA (2) LEN/EDF/WAO Guideline for the definition, classification, diagnosis, and management of urticaria: the 2013 revision and update. Allergy 2014, 69(7):868-87.
• [4]Kakumanu S, Glass C, Craig T: Poor sleep and daytime somnolence in allergic rhinitis: significance of nasal congestion. Am J Respir Med 2002, 1(3):195-200.
• [5]Thompson AK, Juniper E, Meltzer EO: Quality of life in patients with allergic rhinitis. Ann Allergy Asthma Immunol 2000, 85:338-47.
• [6]Weldon D: Quality of life in patients with urticaria and angioedema: assessing burden of disease. Allergy Asthma Proc 2014, 35(1):4-9.
• [7]Bousquet J, Khaltaev N, Cruz AA, Denburg J, Fokkens WJ, Togias A, et al.: Allergic rhinitis and its impact on asthma (ARIA) 2008 update. Allergy 2008, 63(Suppl. 86):8-160.
• [8]Meltzer EO, Bukstein DA: The economic impact of allergic rhinitis and current guidelines for treatment. Ann Allergy Asthma Immunol 2011, 106(2Suppl):S12-6.
• [9]Simons FE, Simons KJ: Histamine and H1-antihistamines: celebrating a century of progress. J Allergy Clin Immunol 2011, 128(6):1139-1150.e4.
• [10]Corcóstegui R, Labeaga L, Innerárity A, Berisa A, Orjales A: Preclinical pharmacology of bilastine, a new selective histamine H1 receptor antagonist: receptor selectivity and in vitro antihistaminic activity. Drugs R D 2005, 6(6):371-84.
• [11]Corcóstegui R, Labeaga L, Innerárity A, Berisa A, Orjales A: In vivo pharmacological characterisation of bilastine, a potent and selective histamine H1 receptor antagonist. Drugs R D 2006, 7(4):219-31.
• [12]Alvarez-Mon M, San Antonio E, Lucero M, Sanz E, Ledo F, De la Hera A: Bilastine, a novel antihistamine that preferentially inhibits histamine and interleukin-4 release from human mast cells and granulocytes. Allergy 2009, 64(Suppl 90):555.
• [13]Jauregizar N, de la Fuente L, Lucero ML, Sologuren A, Leal N, Rodríguez M: Pharmacokinetic-pharmacodynamic modelling of the antihistaminic (H1) effect of bilastine. Clin Pharmacokinet 2009, 48(8):543-54.
• [14]Sádaba B, Gómez-Guiu A, Azanza JR, Ortega I, Valiente R: Oral availability of bilastine. Clin Drug Investig 2013, 33(5):375-81.
• [15]Lucero ML, Gonzalo A, Ganza A, Leal N, Soengas I, Ioja E, et al.: Interactions of bilastine, a new oral H (1) antihistamine, with human transporter systems. Drug Chem Toxicol 2012, 35(Suppl 1):8-17.
• [16]Lucero ML, Gonzalo A, Mumford R, Betanzos M, Alejandro A: An overview of bilastine metabolism during preclinical investigations. Drug Chem Toxicol 2012, 35(Suppl 1):18-24.
• [17]Sologuren A, Lucero ML, Valiente R, Valiente R, Charles H, Mair SJ: Human mass balance with [14C]-bilastine following oral administration to healthy volunteers. Basic Clin Pharmacol Toxicol 2009, 105(Suppl. 1):106-7.
• [18]Lucero ML, Orjales A, Morag N: In vitro hepatic metabolism of [14C]-bilastine. suppl I 2007, 39:114.
• [19]Church MK: Comparative inhibition by bilastine and cetirizine of histamine-induced wheal and flare responses in humans. Inflamm Res 2011, 60(12):1107-12.
• [20]Horak F, Jager S: Wiener Provokations-Kammer (Vienna challenge chamber): eine neue Methode des Allergenexpositionstests. Wiener klin Wochenschr 1987, 99:509-10.
• [21]Stübner P, Zieglmayer R, Horak F: A direct comparison of the efficacy of antihistamines in SAR and PAR: randomised, placebo-controlled studies with levocetirizine and loratadine using an environmental exposure unit - the Vienna challenge chamber (VCC). Curr Med Res Opin 2004, 20(6):891-902.
• [22]Horak F, Zieglmayer P, Zieglmayer R, Lemell P: The effects of bilastine compared with cetirizine, fexofenadine, and placebo on allergen-induced nasal and ocular symptoms in patients exposed to aeroallergen in the Vienna challenge chamber. Inflamm Res 2010, 59(5):391-8.
• [23]Bachert C, Kuna P, Sanquer F, Ivan P, Dimitrov V, Gorina MM, et al.: Comparison of the efficacy and safety of bilastine 20 mg vs desloratadine 5 mg in seasonal allergic rhinitis patients. Allergy 2009, 64:158-65.
• [24]Kuna P, Bachert C, Nowacki Z, van Cauwenberge P, Agache I, Fouquert L, et al.: Efficacy and safety of bilastine 20 mg compared with cetirizine 10 mg and placebo for the symptomatic treatment of seasonal allergic rhinitis: A randomized, double-blind, parallelgroup study. Clin Exp Allergy 2009, 39:1338-47.
• [25]Sastre J, Mullol J, Valero A, Valiente R: Bilastine Study Group: Efficacy and safety of bilastine 20 mg compared with cetirizine 10 mg and placebo in the treatment of perennial allergic rhinitis. Curr Med Res Opin 2012, 28(1):121-30.
• [26]Kowal K, DuBuske L: Bilastine as a potential treatment in allergic rhinitis. Am J Rhinol Allergy 2014, 28(4):312-6.
• [27]Dávila I, Sastre J, Mullol J, Montoro J, Jáuregui I, Ferrer M, et al.: Effect of bilastine upon nasal obstruction. J Investig Allergol Clin Immunol 2011, 21(Suppl 3):2-8.
• [28]Bartra J, Mullol J, Montoro J, Jáuregui I, del Cuvillos A, Dávila I, et al.: Effect of bilastine upon the ocular symptoms of allergic rhinoconjunctivitis. J Investig Allergol Clin Immunol 2011, 21(Suppl 3):24-33.
• [29]Zuberbier T, Oanta A, Bogacka E, Medina I, Wesel F, Uhl P, et al.: Comparison of the efficacy and safety of bilastine 20 mg vs levocetirizine 5 mg for the treatment of chronic idiopathic urticaria: a multi-centre, double-blind, randomized, placebo-controlled study. Allergy 2010, 65(4):516-28.
• [30]Siebenhaar F, Weller K, Mlynek A, Magerl M, Altrichter S, Vieira Dos Santos R, et al.: Acquired cold urticaria: clinical picture and update on diagnosis and treatment. Clin Exp Dermatol 2007, 32(3):241-5.
• [31]Magerl M, Pisarevskaja D, Staubach P, Martus P, Church MK, Maurer M: Critical temperature threshold measurement for cold urticaria: a randomized controlled trial of H (1) -antihistamine dose escalation. Br J Dermatol 2012, 166(5):1095.
• [32]Siebenhaar F, Degener F, Zuberbier T, Martus P, Maurer M: High-dose desloratadine decreases wheal volume and improves cold provocation thresholds compared with standard-dose treatment in patients with acquired cold urticaria: a randomized, placebo-controlled, crossover study. J Allergy Clin Immunol 2009, 123(3):672.
• [33]Krause K, Spohr A, Zuberbier T, Church MK, Maurer M: Up-dosing with bilastine results in improved effectiveness in cold contact urticaria. Allergy 2013, 68(7):921-8.
• [34]Farré M, Pérez-Mañá C, Papaseit E, Menoyo E, Pérez M, Martin S, et al.: Bilastine vs. hydroxyzine: occupation of brain histamine H1 -receptors evaluated by positron emission tomography in healthy volunteers. Br J Clin Pharmacol 2014, 78(5):970-80.
• [35]García-Gea C, Martínez-Colomer J, Antonijoan RM, Valiente R, Barbanoj MJ: Comparison of peripheral and central effects of single and repeated oral dose administrations of bilastine, a new H1 antihistamine: a dose-range study in healthy volunteers with hydroxyzine and placebo as control treatments. J Clin Psychopharmacol 2008, 28(6):675-85.
• [36]Conen S, Theunissen EL, Van Oers AC, Valiente R, Ramaekers JG: Acute and subchronic effects of bilastine (20 and 40 mg) and hydroxyzine (50 mg) on actual driving performance in healthy volunteers. J Psychopharmacol 2011, 25(11):1517-23.
• [37]García-Gea C, Martínez J, Ballester MR, Gich I, Valiente R, Antonijoan RM: Psychomotor and subjective effects of bilastine, hydroxyzine, and cetirizine, in combination with alcohol: a randomized, double-blind, crossover, and positive-controlled and placebo-controlled Phase I clinical trials. Hum Psychopharmacol 2014, 29(2):120-32.
• [38]Tyl B, Kabbaj M, Azzam S, Sologuren A, Valiente R, Reinbolt E, et al.: Lack of significant effect of bilastine administered at therapeutic and supratherapeutic doses and concomitantly with ketoconazole on ventricular repolarization: results of a thorough QT study (TQTS) with QT-concentration analysis. J Clin Pharmacol 2012, 52(6):893-903.
• [39]Graff C, Struijk JJ, Kanters JK, Andersen MP, Toft E, Tyl B: Effects of bilastine on T-wave morphology and the QTc interval: a randomized, double-blind, placebo-controlled, thorough QTc study. Clin Drug Investig 2012, 32(5):339-51.
• [40]Sadaba B, Azanza JR, Gomez-Guiu A, Rodil R: Critical appraisal of bilastine for the treatment of allergic rhinoconjunctivitis and urticaria. Ther Clin Risk Manag 2013, 9:197-205.
• [41]Bousquet J, Ansótegui I, Canonica GW, Zuberbier T, Baena-Cagnani CE, Bachert C, et al.: Establishing the place in therapy of bilastine in the treatment of allergic rhinitis according to ARIA: evidence review. Curr Med Res Opin 2012, 28(1):131-9.
• [42]Jauregui I, Ferrer M, Bartra J, del Cuvillo A, Davila I, Montoro J, et al.: Bilastine for the treatment of urticaria. Expert Opin Pharmacother 2013, 14(11):1537-44.
• [43]Scaglione F: Safety profile of bilastine: 2nd generation H1-antihistamines. Eur Rev Med Pharmacol Sci 2012, 16:1999-2005.
• [44]Zuberbier T: Pharmacological rationale for the treatment of chronic urticaria with second-generation non-sedating antihistamines at higher than standard doses. J Eur Acad Dermatol Venereol 2012, 26(1):9-18.