Inflammation Research

, Volume 60, Issue 12, pp 1107–1112 | Cite as

Comparative inhibition by bilastine and cetirizine of histamine-induced wheal and flare responses in humans

  • Martin K. ChurchEmail author
Original Research Paper


Objective and design

Comparison of bilastine and cetirizine in inhibiting skin wheal and flare responses over 24 h.


Twenty-one healthy male volunteers (aged 19–44 years).

Treatment and methods

Volunteers were randomised to receive single oral doses of 20 or 50 mg bilastine, 10 mg cetirizine or placebo before provocation of wheal and flare responses to 100 mg/ml histamine by skin prick 1.5, 4, 8, 12 and 24 h later.


There were no significant differences between overall inhibitions of wheal or flare by 20 mg bilastine and 10 mg cetirizine. Bilastine was faster in onset than cetirizine, inhibitions of wheal and flare at 1.5 h being 89 ± 3 versus 44 ± 14% (P = 0.011) and 85 ± 4 versus 45 ± 14% (P = 0.016), respectively (Student’s t test). At 1.5 h, both wheals and flares were inhibited by >70% in 11/12 volunteers taking bilastine and 3/11 taking cetirizine (P = 0.003, Fisher’s exact test). There were no significant differences between the drugs at later times. Bilastine 50 mg had a longer duration of action than bilastine 20 mg.


Both 20 mg bilastine and 10 mg cetirizine are effective and of long duration in reducing histamine-induced wheal and flare responses, the major difference between the two drugs being the more rapid onset of action of bilastine.


Bilastine Cetirizine Wheal and flare 



The author wishes to thank Drs. D. McLaverty, A.J. Stewart and B. Colgan of MDS Pharma Services (Belfast, Northern Ireland), and Román Valiente (Faes Farma SA, Department of Research and Development, Department of Clinical Research, Leioa, Spain) for their valuable comments and advice.


  1. 1.
    Bousquet J, Khaltaev N, Cruz AA, Denburg J, Fokkens WJ, Togias A, et al. Allergic rhinitis and its impact on asthma (ARIA) 2008 update (in collaboration with the World Health Organization, GA(2)LEN and AllerGen). Allergy. 2008;63(Suppl 86):8–160.PubMedCrossRefGoogle Scholar
  2. 2.
    Clough GF, Boutsiouki P, Church MK. Comparison of the effects of levocetirizine and loratadine on histamine-induced wheal, flare, and itch in human skin. Allergy. 2001;56(10):985–8.PubMedCrossRefGoogle Scholar
  3. 3.
    Denham KJ, Boutsiouki P, Clough GF, Church MK. Comparison of the effects of desloratadine and levocetirizine on histamine-induced wheal, flare and itch in human skin. Inflamm Res. 2003;52(10):424–7.PubMedCrossRefGoogle Scholar
  4. 4.
    Purohit A, Melac M, Pauli G, Frossard N. Twenty-four-hour activity and consistency of activity of levocetirizine and desloratadine in the skin. Br J Clin Pharmacol. 2003;56(4):388–94.PubMedCrossRefGoogle Scholar
  5. 5.
    Darsow U, Ring J, Scharein E, Bromm B. Correlations between histamine-induced wheal, flare and itch. Arch Dermatol Res. 1996;288(8):436–41.PubMedCrossRefGoogle Scholar
  6. 6.
    Kumar P, Shen Q, Pivetti CD, Lee ES, Wu MH, Yuan SY. Molecular mechanisms of endothelial hyperpermeability: implications in inflammation. Expert Rev Mol Med. 2009;11:e19.PubMedCrossRefGoogle Scholar
  7. 7.
    Entrican JH, Simpson JG, Stalker AL. The effects of histamine and bradykinin on the post-capillary venule. J Pathol. 1971;104(3):3.PubMedGoogle Scholar
  8. 8.
    Raud J. Intravital microscopic studies on acute mast cell-dependent inflammation. Acta Physiol Scand Suppl. 1989;578:1–58.PubMedGoogle Scholar
  9. 9.
    Glyn MC, Lawrenson JG, Ward BJ, Clark P. Rho kinase-mediated reduction in cardiac capillary endothelial cell dimensions, in situ, against flow. Microcirculation. 2008;28:1–16.CrossRefGoogle Scholar
  10. 10.
    Schmelz M, Michael K, Weidner C, Schmidt R, Torebjork HE, Handwerker HO. Which nerve fibers mediate the axon reflex flare in human skin? Neuroreport. 2000;11(3):645–8.PubMedCrossRefGoogle Scholar
  11. 11.
    Schmelz M. A neural pathway for itch. Nat Neurosci. 2001;4(1):9–10.PubMedCrossRefGoogle Scholar
  12. 12.
    Corcostegui R, Labeaga L, Innerarity 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.PubMedCrossRefGoogle Scholar
  13. 13.
    Corcostegui R, Labeaga L, Innerarity 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.PubMedCrossRefGoogle Scholar
  14. 14.
    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.PubMedCrossRefGoogle Scholar
  15. 15.
    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.PubMedCrossRefGoogle Scholar
  16. 16.
    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, parallel-group study. Clin Exp Allergy. 2009;39(9):1338–47.PubMedCrossRefGoogle Scholar
  17. 17.
    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(1):158–65.PubMedCrossRefGoogle Scholar
  18. 18.
    Jauregizar N, de la Fuente L, Lucero ML, Sologuren A, Leal N, Rodriguez M. Pharmacokinetic-pharmacodynamic modelling of the antihistaminic H1-effect of bilastine. Clin Pharmacokinet. 2009;48(8):543–54.PubMedCrossRefGoogle Scholar
  19. 19.
    Staevska M, Popov TA, Kralimarkova T, Lazarova C, Kraeva S, Popova D, et al. The effectiveness of levocetirizine and desloratadine in up to four-times conventional doses in difficult-to-treat urticaria. J Allergy Clin Immunol. 2010;125:676–82.PubMedCrossRefGoogle Scholar
  20. 20.
    Zuberbier T, Asero R, Bindslev-Jensen C, Walter CG, Church MK, Gimenez-Arnau AM, et al. EAACI/GA(2)LEN/EDF/WAO guideline: management of urticaria. Allergy. 2009;64(10):1427–43.PubMedCrossRefGoogle Scholar
  21. 21.
    Gillard M, Van Der Perren PC, Moguilevsky N, Massingham R, Chatelain P. Binding characteristics of cetirizine and levocetirizine to human H1 histamine receptors: contribution of Lys191 and Thr194. Mol Pharmacol. 2002;61(2):391–9.PubMedCrossRefGoogle Scholar
  22. 22.
    Church MK. Safety and efficacy of bilastine: a new H1-antihistamine for the treatment of allergic rhinoconjunctivitis and urticaria. Expert Opin Drug Safety. 2011;10:779–93.Google Scholar
  23. 23.
    Schinkel AH. P-Glycoprotein, a gatekeeper in the blood-brain barrier. Adv Drug Deliv Rev. 1999;36(2–3):179–94.PubMedCrossRefGoogle Scholar
  24. 24.
    Chen C, Hanson E, Watson JW, Lee JS. P-glycoprotein limits the brain penetration of nonsedating but not sedating H1-antagonists. Drug Metab Dispos. 2003;31(3):312–8.PubMedCrossRefGoogle Scholar

Copyright information

© Springer Basel AG 2011

Authors and Affiliations

  1. 1.Department of Dermatology and Allergy, Allergy Centre CharitéCharité-Universitätsmedizin BerlinBerlinGermany
  2. 2.University of SouthamptonSouthamptonUK

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