Effect of food on the bioavailability of fexofenadine hydrochloride (MDL 16 455A)

Stoltz, M.; Arumugham, Thangam; Lippert, Christina; Yu, Dale K.; Bhargava, Vijay O.; Eller, Mark G.; Weir, Scott J.

doi:10.1002/(sici)1099-081x(199710)18:7<645::aid-bdd50>3.0.co;2-3

Cited by 22 publications

(5 citation statements)

References 2 publications

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“…15,16 Although a high-fat breakfast decreases both peak plasma concentrations and area under the plasma concentrationtime curve values of fexofenadine, the changes were smaller than those reported for astemizole and loratadine. 17 Plasma concentrations of ebastine and carebastine measured at steady state in this study exhibited high variability-approximately 100% in the case of ebastine and 45% for carebastine. Food had no significant influence on steady-state concentrations of ebastine measured at 8 hours postdose, while concentrations of carebastine at the same 8-hour time point were increased by 15% (p < 0.05 vs. without food).…”

Section: Discussionmentioning

confidence: 76%

A Double-Blind, Placebo-Controlled Study of the Efficacy and Safety of Ebastine 20 mg Once Daily Given with and without Food in the Treatment of Seasonal Allergic Rhinitis

Hampel

Gillen²,

Rohatagi³

et al. 2002

Journal of Clinical Pharmacology

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The efficacy and safety of ebastine 20 mg once daily given with and without food were compared in patients ages 12 to 70 years with seasonal allergic rhinitis (SAR) caused by mountain cedar allergen. This double-blind, placebo-controlled study was conducted at six centers in Texas. Efficacy and safety analyses were performed on the intent-to-treat population, which comprised 652 patients; 540 patients completed the study. Following 2 weeks' treatment, no significant differences (p > or = 0.91) were found between the ebastine with and without food groups in the percentage change from baseline of daily "reflective" total rhinitis symptom scores (i.e., patients' assessment of severity over the previous 12 h), but both ebastine groups exhibited significantly greater reductions versus patients receiving placebo (p < 0.0001). There were also no significant differences in the percentages of patients experiencing adverse events between the ebastine with and without food groups. Mean steady-state plasma concentrations of ebastine and its active metabolite carebastine were, respectively, 5.5% (ns) and 15.1% (p < 0.05) higher when ebastine was given with food versus its administration without food. Overall, these results indicate that in clinical practice, ebastine does not need to be administered with reference to food.

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Section: Discussionmentioning

confidence: 76%

A Double-Blind, Placebo-Controlled Study of the Efficacy and Safety of Ebastine 20 mg Once Daily Given with and without Food in the Treatment of Seasonal Allergic Rhinitis

Hampel

Gillen²,

Rohatagi³

et al. 2002

Journal of Clinical Pharmacology

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“…Studies of fexofenadine pharmacokinetics dose ranged from 120 to 240 mg have been performed in healthy American [21,23] , Chinese [24,25] , German [26] , Indian [27] , Japanese [28][29][30] , and Korean [31] volunteers. To minimize variation in AUC 0-t , AUCs were adjusted and recalculated based on equivalent duration.…”

Section: Resultsmentioning

confidence: 99%

Does ethnic variability exist in the systemic exposures of oatp1a2 substrates–fexofenadine in taiwanese?

Chen¹,

Juan²,

2015

Indian J Pharm Sci

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Chen, et al.: An Ethnic Differernce in OATP1A2 in TaiwaneseThe aim of this study was to investigate differences in organic anion transporting polypeptide 1A2 activity among the Taiwanese population via an analysis of 3 pharmacokinetic studies completed in a total of 103 healthy male Taiwanese subjects. The pharmacokinetics of fexofenadine was measured as an indicator of organic anion transporting polypeptide 1A2 activity. Using the Kolmogorov-Smirnov test and quantile plots, the frequency distributions of area under the concentration-time curve and concentration were shown to be tri-modal and to represent 3 pharmacokinetic phenotypes. In a comparison with published data, the mean area under the concentration-time curve of fexofenadine in the Taiwanese subjects was similar to that in American, German, and Indian subjects, but significantly different from that in some Asian populations, including Korean and Japanese ethnic groups. These results suggested that Taiwanese subjects showed genetic variation in fexofenadine pharmacokinetics that was associated with differences in organic anion transporting polypeptide 1A2 activity.

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“…Fexofenadine and bilastine are quite similar in some pharmacological aspects, including alterations in their pharmacokinetic profile when administered with food. Similar to bilastine, fexofenadine plasma AUC and C max are reduced by 17% and 11%, respectively, for a capsule formulation, and by 24% and 25%, respectively, for a tablet formulation, when the drug is administered 30 min after a high-fat breakfast versus a 10-h fast [ 24 ]. In addition, fexofenadine and bilastine are non-brain-penetrating antihistamines and zwitterions, display similar binding to H 1 -receptors, have similar acid-base dissociation constants, have larger molecular weights than other non-sedating antihistamines, and exhibit the hysteresis phenomenon [ 1 , 25 , 26 ].…”

Section: Discussionmentioning

confidence: 99%

Lack of Clinical Relevance of Bilastine-Food Interaction in Healthy Volunteers: A Wheal and Flare Study

Coimbra

Puntes

Gich

et al. 2022

Int Arch Allergy Immunol

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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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Effect of food on the bioavailability of fexofenadine hydrochloride (MDL 16 455A)

Cited by 22 publications

References 2 publications

A Double-Blind, Placebo-Controlled Study of the Efficacy and Safety of Ebastine 20 mg Once Daily Given with and without Food in the Treatment of Seasonal Allergic Rhinitis

A Double-Blind, Placebo-Controlled Study of the Efficacy and Safety of Ebastine 20 mg Once Daily Given with and without Food in the Treatment of Seasonal Allergic Rhinitis

Does ethnic variability exist in the systemic exposures of oatp1a2 substrates–fexofenadine in taiwanese?

Lack of Clinical Relevance of Bilastine-Food Interaction in Healthy Volunteers: A Wheal and Flare Study

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