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Comparative inhibition by oral bilastine, parenteral dexchlorpheniramine, and a new bilastine parenteral (i.v. and i.m.) formulation of histamine-induced wheal and flare response : A randomised phase I trial
Coimbra, Jimena (Institut de Recerca Sant Pau)
Puntes, Montserrat (Institut de Recerca Sant Pau)
Molina, Pol (Institut de Recerca Sant Pau)
Gich, Ignasi (Hospital de la Santa Creu i Sant Pau (Barcelona, Catalunya))
Antonijoan, Rosa (Institut de Recerca Sant Pau)
Gilaberte, Inmaculada (FAES FARMA S.A)
Arranz, Paula (FAES FARMA S.A)
Sánchez, Carlos (Medical Department. FAES FARMA S. A.)
Universitat Autònoma de Barcelona. Departament de Farmacologia, de Terapèutica i de Toxicologia

Data: 2024
Resum: Background: Bilastine is a well-known non-sedating second-generation antihistamine authorised worldwide for the symptomatic treatment of allergic rhinoconjunctivitis (seasonal and perennial) and urticaria with proven efficacy and good safety and tolerability profile. When the oral route is not suitable or a rapid onset of action is preferred, parenteral formulations represent an effective treatment option. However, the parenteral formulations currently available are sedating antihistamines. The objective of this research was to compare the peripheral anti-H activity of different bilastine formulations (i. v. , i. m. and oral) and dexchlorpheniramine among them also versus placebo. Methods: This was a single-dose, randomized, crossover, double-blind, placebo-controlled, phase I clinical study performed on 25 adult healthy volunteers that compared the peripheral antihistaminic activity of a single dose of bilastine 12 mg i. v. , bilastine 12 mg i. m. , bilastine 20 mg oral tablets and dexchlorpheniramine 5 mg i. m. among them and versus placebo by inhibiting the histamine-induced wheal and flare (W&F) response. Pharmacokinetics, safety, and tolerability were also evaluated. Results: All bilastine formulations showed a rapid onset of action (15 min for parenteral and 30 min for the oral formulation), and the maximum effect in both wheal (i. v. 74. 44 %; i. m. :74. 29 %; oral 70,27 %) and flare area reduction (i. v. and i. m. 80. 63 %; oral 77. 67 %), was significantly larger compared to dexchlorpheniramine i. m. (25. 85 % for wheal and 28. 65 % for flare) and placebo (1. 35 % for wheal and 4. 02 % for flare). A more pronounced reduction in itching score was reached for bilastine oral, followed by i. m. and i. v. formulations. No serious adverse events (SAEs) were reported during the study, and 8 treatment-emergent adverse events (TEAEs) were reported by 5 subjects, all resolved without sequelae. For psychomotor assessments, dexchlorpheniramine i. m. showed a fast onset of drowsiness, as well as decreased attention and coordination when compared to all bilastine formulations and placebo. Conclusions: All bilastine formulations showed a peripheral H-blocking effect inducing a significantly greater inhibition of the wheal and flare response as compared to dexchlorpheniramine i. m. or placebo and provided a greater reduction of the itching sensation score. This study reconfirmed that bilastine has no sedative effect, even in a parenteral formulation. These results suggest that new bilastine parenteral formulation (i. v. or i. m. ) may represent a suitable alternative for patients requiring immediate treatment of histamine-mediated type I hypersensitivity reactions, such as acute urticaria, or in those cases where oral administration is not possible.
Nota: Altres ajuts: FAES FARMA and Basque Country Government (grant number ZE-2018/00036, 2018)
Drets: Aquest document està subjecte a una llicència d'ús Creative Commons. Es permet la reproducció total o parcial, la distribució, la comunicació pública de l'obra i la creació d'obres derivades, fins i tot amb finalitats comercials, sempre i quan es reconegui l'autoria de l'obra original. Creative Commons
Llengua: Anglès
Document: Article ; recerca ; Versió publicada
Matèria: Bilastine ; Intravenous ; Intramuscular ; Rhinoconjunctivitis ; Urticaria ; Pharmacodynamics
Publicat a: European Journal of Pharmaceutical Sciences, Vol. 203 (December 2024) , ISSN 1879-0720

DOI: 10.1016/j.ejps.2024.106900


9 p, 1.1 MB

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Documents de recerca > Documents dels grups de recerca de la UAB > Centres i grups de recerca (producció científica) > Ciències de la salut i biociències > Institut de Recerca Sant Pau
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 Registre creat el 2025-01-22, darrera modificació el 2025-01-31



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