NDLI: Itraconazole and rifampin alter significantly the disposition and antihistamine effect of ebastine and its metabolites in healthy participants.

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Itraconazole and rifampin alter significantly the disposition and antihistamine effect of ebastine and its metabolites in healthy participants.

Content Provider	World Health Organization (WHO)-Global Index Medicus
Author	Shon, Ji-Hong Yeo, Chang-Woo Liu, Kwang-Hyeon Lee, Sang-Seop Cha, In-Jun Shin, Jae-Gook
Description	Country affiliation: South Korea Author Affiliation: Shon JH ( Department of Pharmacology and PharmacoGenomics Research Center, Inje University College of Medicine, Busan, South Korea.)
Abstract	The present study was performed to elucidate the effects of itraconazole and rifampin on the pharmacokinetics and pharmacodynamics of ebastine, a nonsedative H1 receptor antagonist. In a 3-way crossover sequential design with 2-week washouts, 10 healthy participants were pretreated with itraconazole for 6 days, rifampin for 10 days, or neither. After oral administration of 20 mg ebastine, blood and urine samples were collected for 72 and 24 hours, respectively, and histamine-induced wheal and flare reactions were measured to assess the antihistamine response for 12 hours. Itraconazole pretreatment decreased the oral clearance of ebastine to 10% (P < .001) and increased the AUC(infinity) of the active metabolite, carebastine, by 3-fold (P < .001). On the other hand, rifampin pretreatment decreased the AUC(infinity) of carebastine to 15% (P < .001), with an enormous reduction in the oral bioavailability of ebastine and significantly reduced histamine-induced skin reactions. From these results, the disposition of ebastine and carebastine seems to be significantly altered by coadministration of itraconazole or rifampin. The antihistamine response after ebastine dosing would be decreased following rifampin pretreatments.
File Format	HTM / HTML
ISSN	00912700
Issue Number	2
Volume Number	50
e-ISSN	15524604
Journal	The Journal of Clinical Pharmacology
Language	English
Publisher	Wiley
Publisher Date	2010-02-01
Publisher Place	Great Britain (UK)
Access Restriction	One Nation One Subscription (ONOS)
Subject Keyword	Discipline Pharmacology Butyrophenones Metabolism Pharmacokinetics Itraconazole Pharmacology Piperidines Rifampin Adult Antifungal Agents Therapeutic Use Cross-over Studies Drug Interactions Enzyme Inhibitors Histamine Adverse Effects Histamine H1 Antagonists Humans Hypersensitivity, Immediate Chemically Induced Drug Therapy Male Skin Immunology Young Adult Clinical Trial Journal Article Research Support, Non-u.s. Gov't
Content Type	Text
Resource Type	Article
Subject	Pharmacology Pharmacology (medical)

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The pharmacokinetics, antihistamine and concentration-effect relationship of ebastine in healthy subjects.

Itraconazole and rifampin alter significantly the disposition and antihistamine effect of ebastine and its metabolites in healthy participants.

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