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

Abstract：

:1. The kinetics and effects of ebastine 10 and 50 mg were studied after oral dosing in healthy subjects. 2. The parent drug was extensively metabolised during the first pass to its carboxylic acid derivative, carebastine. 3. The pharmacokinetics of carebastine were linear over the dose range studied and the terminal elimination half-life was 10.6 +/- 2.6 and 12.5 +/- 1.9 h respectively after 10 and 50 mg of ebastine. 4. Antihistamine (H1-receptor) activity was examined with intradermal histamine (2 micrograms). Oral ebastine reduced the histamine wheal area for up to 24 h and also reduced subjective local pain. 5. Antihistamine activity correlated well with plasma levels of carebastine in individual subjects. 6. Ebastine appears to have potential as an antihistamine for once a day dosing.

journal_name

Br J Clin Pharmacol

journal_title

British journal of clinical pharmacology

authors

Vincent J,Liminana R,Meredith PA,Reid JL

doi

10.1111/j.1365-2125.1988.tb05288.x

subject

Has Abstract

pub_date

1988-11-01 00:00:00

pages

497-502

issue

5

eissn

0306-5251

issn

1365-2125

journal_volume

26

pub_type

临床试验,杂志文章,随机对照试验

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