The pharmacokinetics, antihistamine and concentration-effect relationship of ebastine in healthy subjects.
The pharmacokinetics, antihistamine and concentration-effect relationship of ebastine in healthy subjects.
复制标题
依巴斯汀在健康受试者中的药代动力学、抗组胺药和浓度-效应关系。
DOI：
10.1111/j.1365-2125.1988.tb05288.x
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发表时间：
1988
影响因子：
3.4
通讯作者：
J. Reid
中科院分区：
文献类型：
--
作者：
J. Vincent;R. Limiñana;P. Meredith;J. Reid
1.在健康受试者中研究了依巴斯汀10 mg和50 mg口服给药后的动力学和效应。2.母体药物在第一次通过时被广泛代谢为其羧酸衍生物卡巴斯汀。3.在研究的剂量范围内，卡巴斯汀的药代动力学呈线性，依巴斯汀10和50 mg给药后，终末消除半衰期分别为10.6 +/- 2.6和12.5 +/- 1.9 h。4.用皮内组胺（2 μ g）检查抗组胺（H1受体）活性。口服依巴斯汀可减少组胺风团面积长达24小时，也可减轻主观局部疼痛。5.在个体受试者中，抗组胺活性与卡巴斯汀的血浆水平相关性良好。6.依巴斯汀似乎具有作为抗组胺药每日一次给药的潜力。
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.