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Ebastine in the light of CONGA recommendations for the development of third-generation antihistamines

In 2003 a consensus group on new-generation antihistamines (CONGA) defined the characteristics required for a third-generation H(1) antihistamine as there had been much controversy about this issue since the early 1990s. One of the antihistamines that had been claimed to belong to such a group is th...

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Autores principales: Rico, S, Antonijoan, RM, Barbanoj, MJ
Formato: Texto
Lenguaje:English
Publicado: Dove Medical Press 2009
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3048600/
https://www.ncbi.nlm.nih.gov/pubmed/21437146
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author Rico, S
Antonijoan, RM
Barbanoj, MJ
author_facet Rico, S
Antonijoan, RM
Barbanoj, MJ
author_sort Rico, S
collection PubMed
description In 2003 a consensus group on new-generation antihistamines (CONGA) defined the characteristics required for a third-generation H(1) antihistamine as there had been much controversy about this issue since the early 1990s. One of the antihistamines that had been claimed to belong to such a group is the second-generation antihistamine, ebastine. The objective of this review is to analyze the pharmacology of ebastine, in light of the CONGA recommendations for the development of new-generation antihistamines: (1) anti-inflammatory properties, (2) potency, efficacy and effectiveness, (3) lack of cardiotoxicity, (4) lack of drug interactions, (5) lack of CNS effects, and (6) pharmacological approach. Ebastine seems to have anti-inflammatory properties that help to ameliorate nasal congestion, though this has not yet been conclusively demonstrated. Its pharmacological–therapeutic profile does not differ greatly from that of other second-generation antihistamines. Its cardiac safety has been widely assessed and no cardiac toxicity has been found at therapeutic doses despite initial concerns. The risk of potentially relevant drug interactions has been investigated and ruled out. Ebastine does not produce sedation at therapeutic doses and drug interaction studies with classical CNS depressants have not demonstrated a synergistic effect. Pharmacologically, ebastine is an H(1) inverse agonist. Perhaps the answer to the quest for new-generation antihistamines lies not only in H(1) but in a combined approach with other histamine receptors.
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spelling pubmed-30486002011-03-23 Ebastine in the light of CONGA recommendations for the development of third-generation antihistamines Rico, S Antonijoan, RM Barbanoj, MJ J Asthma Allergy Review In 2003 a consensus group on new-generation antihistamines (CONGA) defined the characteristics required for a third-generation H(1) antihistamine as there had been much controversy about this issue since the early 1990s. One of the antihistamines that had been claimed to belong to such a group is the second-generation antihistamine, ebastine. The objective of this review is to analyze the pharmacology of ebastine, in light of the CONGA recommendations for the development of new-generation antihistamines: (1) anti-inflammatory properties, (2) potency, efficacy and effectiveness, (3) lack of cardiotoxicity, (4) lack of drug interactions, (5) lack of CNS effects, and (6) pharmacological approach. Ebastine seems to have anti-inflammatory properties that help to ameliorate nasal congestion, though this has not yet been conclusively demonstrated. Its pharmacological–therapeutic profile does not differ greatly from that of other second-generation antihistamines. Its cardiac safety has been widely assessed and no cardiac toxicity has been found at therapeutic doses despite initial concerns. The risk of potentially relevant drug interactions has been investigated and ruled out. Ebastine does not produce sedation at therapeutic doses and drug interaction studies with classical CNS depressants have not demonstrated a synergistic effect. Pharmacologically, ebastine is an H(1) inverse agonist. Perhaps the answer to the quest for new-generation antihistamines lies not only in H(1) but in a combined approach with other histamine receptors. Dove Medical Press 2009-08-31 /pmc/articles/PMC3048600/ /pubmed/21437146 Text en © 2009 Rico et al, publisher and licensee Dove Medical Press Ltd. This is an Open Access article which permits unrestricted noncommercial use, provided the original work is properly cited.
spellingShingle Review
Rico, S
Antonijoan, RM
Barbanoj, MJ
Ebastine in the light of CONGA recommendations for the development of third-generation antihistamines
title Ebastine in the light of CONGA recommendations for the development of third-generation antihistamines
title_full Ebastine in the light of CONGA recommendations for the development of third-generation antihistamines
title_fullStr Ebastine in the light of CONGA recommendations for the development of third-generation antihistamines
title_full_unstemmed Ebastine in the light of CONGA recommendations for the development of third-generation antihistamines
title_short Ebastine in the light of CONGA recommendations for the development of third-generation antihistamines
title_sort ebastine in the light of conga recommendations for the development of third-generation antihistamines
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3048600/
https://www.ncbi.nlm.nih.gov/pubmed/21437146
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