Modern H1- antihistamines in the treatment of allergic rhinitis: focus on bilastine

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Abstract

The second generation of H1-antihistamines is approved for the stepwise treatment of seasonal and perennial allergic rhinitis in adults and children by international and national guidelines. They reduce the severity of nasal and ocular symptoms of rhinitis and improve the quality of life of patients.

Bilastine, a piperidine derivative, is a novel H1-antihistamine. It has a potent and selective effect on H1- receptors and a rapid onset and long duration of action and substantially reduces nasal and ocular symptoms of seasonal and perennial allergic rhinitis. Bilastine has no clinically substantial hepatic metabolism and has a high safety profile: it has no sedative effect, does not affect cognitive functions, has no cardiotoxic effects, and does not interact with alcohol and benzodiazepines in normal and high doses. Tachyphylaxis does not develop despite long-term (up to 1 year) use.

Bilastine is registered for clinical use in adults and children aged >12 years. The results of clinical and experimental studies have demonstrated that bilastine has many of the features of modern H1-antihistamines recommended by international guidelines.

About the authors

Alexander V. Emelyanov

North-Western Medical University named after I.I. Mechnikov

Author for correspondence.
Email: emelav@inbox.ru
ORCID iD: 0000-0002-8574-6869
SPIN-code: 8036-2985

MD, Dr. Sci. (Med.), Professor

Russian Federation, 41 Kirochnaya street, 191015 Saint-Petersburg

Galina R. Sergeeva

North-Western Medical University named after I.I. Mechnikov

Email: sergreevagr@mail.ru
ORCID iD: 0000-0003-1544-4336
SPIN-code: 2474-2933

Cand. Sci. (Med.), Assistant

Russian Federation, 41 Kirochnaya street, 191015 Saint-Petersburg

Evgenia V. Leshenkova

North-Western Medical University named after I.I. Mechnikov

Email: leshenkova@mail.ru
ORCID iD: 0000-0003-4616-3166
SPIN-code: 1078-6570

MD, Cand. Sci. (Med.)

Russian Federation, 41 Kirochnaya street, 191015 Saint-Petersburg

References

  1. Bousquet J, van Cavuwenberge P, Khaltaev N, et al. Allergic rhinitis and its impact on asthma (ARIA). J Allergy Clin Immunol. 2001;108(5 Suppl.):S.147–S.334. doi: 10.1067/mai.2001.118891
  2. Bousquet J, Schünemann HJ, Togias A, et al.; Allergic Rhinitis and Its Impact on Asthma Working Group. Next-generation Allergic Rhinitis and Its Impact on Asthma (ARIA) guidelines for allergic rhinitis based on Grading of Recommendations Assessment, Development and Evaluation (GRADE) and real-world evidence. J Allergy Clin Immunol. 2020;145(1):70–80.e3. doi: 10.1016/j.jaci.2019.06.049
  3. Papadopoulos NG, Bernstein JA, Demoly P. Phenotypes and endotypes of rhinitis and their impact on management: a PRACTALL report. Allergy. 2015;70(5):474–494. doi: 10.1111/all.12573
  4. Bousquet PJ, Combescure C, Klossek JM, et al. Change in visual analog scale score in a pragmatic randomized cluster trial of allergic rhinitis. J Allergy Clin Immunol. 2009;123(6):1349–1354. doi: 10.1016/j.jaci.2009.02.033
  5. Eguiluz-Gracia I, Testera-Montes A, Rondon C. Medical algorithm: Diagnosis and treatment of local allergic rhinitis. Allergy. 2021. doi: 10.1111/all.14848
  6. Nenasheva NM, Shilenkova VV. Control of symptoms of allergic rhinitis in adults in the Russian Federation: results of an online survey. RMJ “Medical review”. 2021;51(1):25–31. (In Russ). doi: 10.32364/2587-6821-2021-5-1-25-31
  7. Polner SA. Federal clinical recommendations: Allergic rhinitis. Russian Allergological Journal. 2017;14(2):47–54. (In Russ). doi: 10.36691/RJA323
  8. Farre M, Perez-Manna C, Papaseit E, et al. Bilastine vs. hydroxyzine: occupation of brain histamine H1-receptors evaluated by positron emission tomography in healthy volunteers. Br J Clin Pharm. 2014;78(5):970–980. doi: 10.1111/bcp.12421
  9. Church MK, Maurer M, Simons FE, et al. Risk of first generation H1-antihistamines: a GA(2)LEN position paper. Allergy. 2010;65(4):459–466. doi: 10.1111/j.1398-9995.2009.02325.x
  10. Simons FE, Simons KJ. Histamine and H1-antihistamines: Celebrating a century of progress. J Allergy Clin Immunol. 2011;128(6):1139–1150. doi: 10.1016/j.jaci.2011.09.005
  11. Mizuguchi H, Wakugawa T, Sadakata H, et al. Elucidation of inverse agonist activity of bilastine. Pharmaceutics. 2020;12(6):525. doi: 10.3390/pharmaceutics12060525
  12. Church MK, Tiongco-Recto M, Ridolo E, Novák Z. Bilastine: a lifetime companion for the treatment of allergies. Current Medical Research and Opinion. 2020;36(3):445–454. doi: 10.1080/03007995.2019.1681134
  13. Corcóstegui R, Labeaga L, Innerárity A, et al. Preclinical pharmacology of bilastine, a new selective histamine H1 receptor antagonist: receptor selectivity and in vitro antihistaminic activity. Drugs R D. 2005;6(6):371–384. doi: 10.2165/00126839-200506060-00005
  14. 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):391–398. doi: 10.1007/s00011-009-0117-4
  15. Garcıa-Gea C, Martınez J, Ballester MR, et al. 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):120–132. doi: 10.1002/hup.2378
  16. García-Gea С, Martínez-Colomer J, Antonijoan R, et al. 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):675–685. doi: 10.1097/JCP.0b013e31818b2091
  17. Valk PJ, Simons R, Jetten AM, et al. Cognitive performance effects of bilastine 20 mg during 6 hours at 8000 ft cabin altitude. Aerosp Med Hum Perform. 2016;87(7):622–627. doi: 10.3357/AMHP.4522.2016
  18. Reményi A, Grósz A, Szabó SA, et al. Comparative study of the effect of bilastine and cetirizine on cognitive functions at ground level and at an altitude of 4,000 m simulated in hypobaric chamber: a randomized, double-blind, placebo-controlled, cross-over study. Expert Opinion Drug Saf. 2018;17(9):859–868. doi: 10.1080/14740338.2018.1502268
  19. Tyl B, Kabbaj M, Azzam S, 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 QTConcentration analysis. J Clin Pharm. 2013;52(6):893–903. doi: 10.1177/0091270011407191
  20. Graff C, Struijk J, Kanters JK, et al. 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):339–351. doi: 10.2165/11599270-000000000-00000
  21. Kuna P, Bachert C, Nowacki Z, et al.; Bilastine International Working Group. 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, parallel-group study. Clin Exp Allergy. 2009;39(9):1338–1347. doi: 10.1111/j.1365-2222.2009.03257.x
  22. Bachert C, Kuna P, Sanquer F, et al.; Bilastine International Working Group. Comparison of the efficacy and safety of bilastine 20 mg vs desloratadine 5 mg in seasonal allergic rhinitis patients. Allergy. 2009;64(1):158–165. doi: 10.1111/j.1398-9995.2008.01813.x
  23. Sastre J, Mullol J, Valero A, et al.; Bilastine Study Group Collaborators. 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):121–130. doi: 10.1185/03007995.2011.640667
  24. Okubo K, Gotoh M, Asako M, et al. Efficacy and safety of bilastine in Japanese patients with perennial allergic rhinitis: A multicenter, randomized, double-blind, placebo-controlled, parallel-group phase III study. Allergol Int. 2017;66(1):97–105. doi: 10.1016/j.alit.2016.05.014
  25. Okubo K, Gotoh M, Togawa M, et al. Long-term safety and efficacy of bilastine following up to 12 weeks or 52 weeks of treatment in Japanese patients with allergic rhinitis: Results of an open-label trial. Auris Nasus Larynx. 2017;44(3):294–301. doi: 10.1016/j.anl.2016.07.021
  26. Novák Z, Yáñez A, Kiss I, et al.; Bilastine Paediatric Safety Study Group. Safety and tolerability of bilastine 10 mg administered for 12 weeks in children with allergic diseases. Pediatr Allergy Immunol. 2016;27(5):493–498. doi: 10.1111/pai.12555
  27. Camelo-Nunes IC, Sole D. Allergic rhinitis: indicators of quality of life. J Bras Pneumol. 2010;36(1):124–133. doi: 10.1590/s1806-37132010000100017
  28. Kirmaz C, Aydemir O, Bayrak P, et al. Sexual dysfunction in patients with allergic rhinoconjunctivitis. Ann Allergy Asthma Immunol. 2005;95(6):525–529. doi: 10.1016/S1081-1206(10)61013-7
  29. Locks RB, Dos Santos K, da Silva J. Quality of life in patients with allergic rhinitis: a clinical trial comparing the use of bilastine versus loratadine. Clin Otolaryngol. 2017;42(2):218–224. doi: 10.1111/coa.12695
  30. Jauregui I, Bartra J, del Cuvillo A, et al. Bilastine and quality of life. J Investig Allergol Clin Immunol. 2011;21(Suppl 3):16–23.
  31. Montoro J, Mullol J, Davila I, et al. Bilastine and the central nervous system. J Investig Allergol Clin Immunol. 2011;21(3):9–15.
  32. Vozmediano V, Sologuren A, Lukas JC, et al. Model informed pediatric development applied to bilastine: ontogenic pk model development, dose selection for first time in children and PK study design. Pharm Res. 2017;34(12):2720–2734. doi: 10.1007/s11095-017-2248-6
  33. Vozmediano V, Lukas JC, Encinas E, et al. Model-informed pediatric development applied to bilastine: analysis of the clinical PK data and confirmation of the dose selected for the target population. Eur J Pharm Sci. 2019;128:180–192. doi: 10.1016/j.ejps.2018.11.016
  34. Bilastine 10 mg orodispersible tablets: summary of product characteristics; 2018 [cited 2021 May 24]. Available from: http://www.gov.uk/pil-spc
  35. Bilastine 2.5 mg/ml oral solution: summary of product characteristics; 2018 [cited 2021 May 24]. Available from: http:// www.gov.uk/pil-spc
  36. Demoly P, Chiriac AM, Berge B, Rostin M. Reasons for prescribing second generation antihistamines to treat allergic rhinitis in real-life conditions and patient response. Allergy Asthma Clin Immun. 2014;10(1):29. doi: 10.1186/1710-1492-10-29
  37. Demoly P, Aubier M, de Blay F, et al. Evaluation of patients’ expectations and benefits in the treatment of allergic rhinitis with a new tool: the patient benefit index – the benefica study. Allergy Asthma Clin Immunol. 2015;11(1):8. doi: 10.1186/s13223-015-0073-1
  38. Lynde CW, Sussman GB, Dion PL, et al. Multidisciplinary real-world experience with bilastine, a second generation antihistamine. J Drugs Dermatol. 2020;19(2):145–154. doi: 10.36849/JDD.2020.4835.

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