Multidisciplinary Real-World Experience With Bilastine, a Second Generation Antihistamine

February 2020 | Volume 19 | Issue 2 | Original Article | 145 | Copyright © February 2020

Published online February 11, 2020

Charles W. Lynde , Gordon Sussman , Pierre-Luc Dion , Lyn Guenther , Jacques Hébert , Jaggi Rao , Tim Vander Leek , Susan Waserman

aDepartment of Medicine, University of Toronto, Toronto, ON, Canada bDivision of Allergy/Clinical Immunology, University of Toronto, Toronto, ON, Canada cDivision of Dermatology, Université Laval, Québec, Québec, Canada; CISSS de Chaudière-Appalaches – Hôtel-Dieu de Lévis, Lévis, Québec, Canada dWestern University, London, ON. Royal College of Physicians and Surgeons of Canada, eDepartment of Medicine, Université Laval, Québec, Canada fDivision of Dermatology, University of Alberta, Edmonton, Alberta, Canada gDepartment of Pediatrics, Stollery Children’s Hospital, University of Alberta, Edmonton, Alberta, Canada hDivision of Clinical Immunology & Allergy, Department of Medicine, McMaster University, Hamilton, ON, Canada

This current real-world case project serves as a mechanism to help optimize patient care by recognizing the role bilastine can play in the treatment of a broad range of conditions such as SAR, PAR, urticarial vasculitis as well as both chronic and inducible urticarias. Additionally, the project explores where bilastine can manage pruritus due to skin conditions, such as in atopic dermatitis (AD), which may require adjunctive AH use to skincare and AD treatment.


A real-world case-based approach was used to explore the role bilastine can play in the treatment of conditions that require AH use. These real-life patient cases are coupled with evidence from the literature. Recommendations given by the panel reflect the use of bilastine for these conditions and demonstrate how patients can benefit from its use. Any discussion concerning off-label use should be considered an expert opinion only.

The target audience for this publication are physicians, such as allergists and dermatologists, who treat patients with conditions requiring AHs.


A literature review was conducted to explore the role of second- generation AHs, and to assess their value for patients with conditions requiring AHs. Databases searched were: EMBASE, MEDLINE, CINAHL, PubMed, The Cochrane Library, RCP Guidelines Database, and DARE. The searches were conducted February 24–25, 2019, and included guidelines and other publications in the English language, which were dated from 2000 to 2019. References selected further included evidence on bilastine and its use in the presented cases. Medical subject heading terms were used in various combinations in the literature searches and included: 1st and 2nd generation AHs use, specifically bilastine; efficacy for conditions requiring AHs; allergic rhinoconjunctivitis, chronic urticaria, safety of AHs; elimination; tolerance; anticholinergic effects; cardiotoxicity; metabolism; AHs interaction with other drugs; drowsiness using AHs and use of AHs during various activities (such as driving and flying a plane); adverse events; effects of its use in populations of various age groups and impact on quality of life.


An expert panel (authors) of allergists and dermatologists who commonly treat patients with bilastine was established to present real-life case studies covering conditions including SAR, PAR, urticarial vasculitis, urticaria and pruritus due to various causes, such as AD. The panel members used a template for their case studies, which asked the following questions: What are the case and the impact of the condition? What are the treatment options, and what treatment(s) were previously used? Why might bilastine work in this case, where does it fit and what were the results of bilastine use? Did any adverse events occur? If yes, describe. What (if any) are the special circumstances related to this particular case and what lessons are learned? During a one-day authorship meeting, the panel presented their cases, followed by a group discussion, after which the authors decided which of the real-world cases using bilastine were included in the manuscript. The publication was developed, reviewed by the panel members, and prepared for publication.

Antihistamines for Treatment of Allergic Conditions
First-generation AHs
AHs have been in use since 1940 for various allergic conditions.1 The first generation AHs were discovered by Bovet and Staub in 1937 and have anticholinergic and sedative activity.1,10,11 AHs act as inverse agonists rather than antagonists of histamine H1-receptors, which are members of the superfamily of G-protein- coupled receptors (GPCRs).10 The older first-generation AHs penetrate readily into the brain to cause sedation, drowsiness, fatigue, impaired concentration, and memory, possibly by negatively impacting rapid-eye-movement (REM) sleep.10,12,13 These first-generation AHs may cause detrimental effects on learning and examination performance in children, may impair the ability of adults to work and drive, and their use should be discouraged. 10,12 Both the Allergic Rhinitis and its Impact on Asthma (ARIA) guidelines14 and the European Academy of Allergy and Clinical Immunology (EAACI) / Global Allergy and Asthma European Network (GA2 LEN)/ European Dermatology Forum (EDF)/ World Allergy Organization (WAO) guidelines for the management of urticaria13 recommend (strong recommendation, high quality evidence) the use of second-generation, non-sedating AHs and discourage the use of first-generation AHs.

Many physicians still combine a second-generation AH in the morning with a sedating first-generation AH at night to enhance sleep. Staevska et al. compared levocetirizine with or without nightly hydroxyzine, and noted the two treatments were equally effective in decreasing symptoms, quality of life improvement, and lack of nighttime disturbance; however, hydroxyzine increased daytime somnolence.4

A media audit of US coverage of transport accidents from 1996 to 2008 in which first-generation AHs were implicated, revealed 54 fatalities.12 The authors suggested this was likely a gross underestimation of the true figure because these were only media reported events.12 A similar audit performed on second-generation AHs found no articles that associated these AHs as a cause of transport accidents.12

Second-generation AHs
Second generation AHs cause less sedation because of their limited penetration of the blood-brain barrier.10 They are highly selective for the histamine H1-receptor and have minimal anticholinergic effects.10 The second-generation AHs commonly