c428744ee3174a2444c2523920b19f81 270743.pdf b308e06762660e718a0e3dac0fd75fcea096ca16 270743.pdf d1e893fbdcbdbc663ad89a75bcd51f5289f34f532fbdc98e4804707b7b7a4fec 270743.pdf Title: Lack of Clinical Relevance of Bilastine-Food Interaction in Healthy Volunteers: A Wheal and Flare Study Subject: Introduction: The aim of this study was to compare the pharmacodynamic activity of bilastine administered under fasting and fed conditions in healthy volunteers. Methods: In this randomized, open-label, two-period, crossover study involving 24 healthy subjects, once-daily oral bilastine 20 mg was administered for 4 days under fasting and fed conditions, with a 7-day washout period. Bilastine plasma concentrations were measured for 24 h after the first and fourth doses in each period. Pharmacodynamic activity was assessed by wheal and flare surface inhibition and subjective assessment of itching, after intradermal injection of histamine 5 μg. Results: When administered under fed versus fasting conditions, exposure to bilastine 20 mg decreased (mean maximum plasma concentration and area under the curve from time 0 to 24 h decreased by 34.27% and 32.72% [day 1], respectively, and 33.08% and 28.87% [day 4]). Despite this, the antihistaminic effect of bilastine 20 mg was not altered by food. On day 1, as assessed by wheal and flare surface inhibition, the maximum effect and duration of action of bilastine did not differ to a significant extent between fasting and fed conditions, with only a short 30-min delay in the onset of wheal inhibition. At steady state (day 4), bilastine’s pharmacodynamic effects were not significantly affected under fasting or fed conditions. Conclusion: The pharmacokinetic interaction of bilastine with food does not imply a significant reduction of its peripheral antihistaminic efficacy. Despite a slight delay in onset of action on the first treatment day, the global clinical efficacy of bilastine is not affected by coadministration with food. Author: Coimbra J.; Puntes M.; Gich I.; Martínez J.; Molina P.; Antonijoan R.; Campo C.; Labeaga L. 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Subject: Introduction: The aim of this study was to compare the pharmacodynamic activity of bilastine administered under fasting and fe搀 挀漀渀搀椀琀椀漀渀猀 椀渀 栀攀愀氀琀栀礀 瘀漀氀甀渀琀攀攀爀猀⸀ 䴀攀琀栀漀搀猀㨀 䤀渀 琀栀椀猀 爀愀渀搀漀洀椀稀攀搀Ⰰ 漀瀀攀渀ⴀ氀愀戀攀氀Ⰰ 琀眀漀ⴀ瀀攀爀椀漀搀Ⰰ 挀爀漀猀猀漀瘀攀爀 猀琀甀搀礀 椀渀瘀漀氀瘀椀渀最 ㈀㐀 栀攀愀氀琀栀礀 猀畜ഀ戀樀攀挀琀猀Ⰰ 漀渀挀攀ⴀ搀愀椀氀礀 漀爀愀氀 戀椀氀愀猀琀椀渀攀 ㈀  洀最 眀愀猀 愀搀洀椀渀椀猀琀攀爀攀搀 昀漀爀 㐀 搀愀礀猀 甀渀搀攀爀 昀愀猀琀椀渀最 愀渀搀 昀攀搀 挀漀渀搀椀琀椀漀渀猀Ⰰ 眀椀琀栀 愀 㜀ⴀ搀愀礀 眀愀猀栀漀甀琀 瀀攀爀椀d. Bilastine plasma concentrations were measured for 24 h after the first and fourth doses in each period. Pharmacodynamic acti瘀椀琀礀 眀愀猀 愀猀猀攀猀猀攀搀 戀礀 眀栀攀愀氀 愀渀搀 昀氀愀爀攀 猀甀爀昀愀挀攀 椀渀栀椀戀椀琀椀漀渀 愀渀搀 猀甀戀樀攀挀琀椀瘀攀 愀猀猀攀猀猀洀攀渀琀 漀昀 椀琀挀栀椀渀最Ⰰ 愀昀琀攀爀 椀渀琀爀愀搀攀爀洀愀氀 椀渀樀攀挀琀椀漀渀 漀昀 栀椀tamine 5 μg. Results: When administered under fed versus fasting conditions, exposure to bilastine 20 mg decreased (mean maxim甀洀 瀀氀愀猀洀愀 挀漀渀挀攀渀琀爀愀琀椀漀渀 愀渀搀 愀爀攀愀 甀渀搀攀爀 琀栀攀 挀甀爀瘀攀 昀爀漀洀 琀椀洀攀   琀漀 ㈀㐀 栀 搀攀挀爀攀愀猀攀搀 戀礀 ㌀㐀⸀㈀㜀─ 愀渀搀 ㌀㈀⸀㜀㈀─ 嬀搀愀礀 ㄀崀Ⰰ 爀攀猀瀀攀挀琀椀瘀攀氀礀Ⰰ 愀渀搀 ㍜ഀ㌀⸀ 㠀─ 愀渀搀 ㈀㠀⸀㠀㜀─ 嬀搀愀礀 㐀崀⸀ 䐀攀猀瀀椀琀攀 琀栀椀猀Ⰰ 琀栀攀 愀渀琀椀栀椀猀琀愀洀椀渀椀挀 攀昀昀攀挀琀 漀昀 戀椀氀愀猀琀椀渀攀 ㈀  洀最 眀愀猀 渀漀琀 愀氀琀攀爀攀搀 戀礀 昀漀漀搀⸀ 伀渀 搀愀礀 ㄀Ⰰ 愀猀 愀猀獜ഀ攀猀猀攀搀 戀礀 眀栀攀愀氀 愀渀搀 昀氀愀爀攀 猀甀爀昀愀挀攀 椀渀栀椀戀椀琀椀漀渀Ⰰ 琀栀攀 洀愀砀椀洀甀洀 攀昀昀攀挀琀 愀渀搀 搀甀爀愀琀椀漀渀 漀昀 愀挀琀椀漀渀 漀昀 戀椀氀愀猀琀椀渀攀 搀椀搀 渀漀琀 搀椀昀昀攀爀 琀漀 愀 猀椀最渀椀昀椀ant extent between fasting and fed conditions, with only a short 30-min delay in the onset of wheal inhibition. At steady state 搀愀礀 㐀Ⰰ 戀椀氀愀猀琀椀渀攠ᤀ猀 瀀栀愀爀洀愀挀漀搀礀渀愀洀椀挀 攀昀昀攀挀琀猀 眀攀爀攀 渀漀琀 猀椀最渀椀昀椀挀愀渀琀氀礀 愀昀昀攀挀琀攀搀 甀渀搀攀爀 昀愀猀琀椀渀最 漀爀 昀攀搀 挀漀渀搀椀琀椀漀渀猀⸀ 䌀漀渀挀氀甀猀椀漀渀㨀 吀栀攀pharmacokinetic interaction of bilastine with food does not imply a significant reduction of its peripheral antihistaminic effi挀愀挀礀⸀ 䐀攀猀瀀椀琀攀 愀 猀氀椀最栀琀 搀攀氀愀礀 椀渀 漀渀猀攀琀 漀昀 愀挀琀椀漀渀 漀渀 琀栀攀 昀椀爀猀琀 琀爀攀愀琀洀攀渀琀 搀愀礀Ⰰ 琀栀攀 最氀漀戀愀氀 挀氀椀渀椀挀愀氀 攀昀昀椀挀愀挀礀 漀昀 戀椀氀愀猀琀椀渀攀 椀猀 渀漀琀 愀昀ected by coadministration with food. 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Labeaga L. Lack of Clinical Relevance of Bilastine-Food Interaction in Healthy Volunteers: A Wheal and Flare Study Copyright: All rights reserved. No part of this publication may be translated into other languages, reproduced or utilized in any form or by any means, electronic or mechanical, including photocopying, recording, microcopying, or by any information storage and retrieval system, without permission in writing from the publisher.<br /> Drug Dosage: The authors and the publisher have exerted every effort to ensure that drug selection and dosage set forth in this text are in accord with current recommendations and practice at the time of publication. However, in view of ongoing research, changes in government regulations, and the constant flow of information relating to drug therapy and drug reactions, the reader is urged to check the package insert for each drug for any changes in indications and dosage and for added warnings and precautions. This is particularly important when the recommended agent is a new and/or infrequently employed drug.<br /> Disclaimer: The statements, opinions and data contained in this publication are solely those of the individual authors and contributors and not of the publishers and the editor(s). The appearance of advertisements or/and product references in the publication is not a warranty, endorsement, or approval of the products or services advertised or of their effectiveness, quality or safety. The publisher and the editor(s) disclaim responsibility for any injury to persons or property resulting from any ideas, methods, instructions or products referred to in the content or advertisements. Introduction: The aim of this study was to compare the pharmacodynamic activity of bilastine administered under fasting and fed conditions in healthy volunteers. Methods: In this randomized, open-label, two-period, crossover study involving 24 healthy subjects, once-daily oral bilastine 20 mg was administered for 4 days under fasting and fed conditions, with a 7-day washout period. Bilastine plasma concentrations were measured for 24 h after the first and fourth doses in each period. Pharmacodynamic activity was assessed by wheal and flare surface inhibition and subjective assessment of itching, after intradermal injection of histamine 5 μg. Results: When administered under fed versus fasting conditions, exposure to bilastine 20 mg decreased (mean maximum plasma concentration and area under the curve from time 0 to 24 h decreased by 34.27% and 32.72% [day 1], respectively, and 33.08% and 28.87% [day 4]). Despite this, the antihistaminic effect of bilastine 20 mg was not altered by food. On day 1, as assessed by wheal and flare surface inhibition, the maximum effect and duration of action of bilastine did not differ to a significant extent between fasting and fed conditions, with only a short 30-min delay in the onset of wheal inhibition. At steady state (day 4), bilastine’s pharmacodynamic effects were not significantly affected under fasting or fed conditions. Conclusion: The pharmacokinetic interaction of bilastine with food does not imply a significant reduction of its peripheral antihistaminic efficacy. Despite a slight delay in onset of action on the first treatment day, the global clinical efficacy of bilastine is not affected by coadministration with food. 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