Temazepam.

Louis A. Pagliaro, Ann Marie Pagliaro
{"title":"Temazepam.","authors":"Louis A. Pagliaro, Ann Marie Pagliaro","doi":"10.4324/9781315825731-103","DOIUrl":null,"url":null,"abstract":"In a single and multiple dose absorption, distribution, metabolism, and excretion (ADME) study, using 3H labeled drug, temazepam was well absorbed and found to have minimal (8%) first pass metabolism. There were no active metabolites formed and the only significant metabolite present in blood was the O-conjugate. The unchanged drug was 96% bound to plasma proteins. The blood level decline of the parent drug was biphasic with the short half-life ranging from 0.4 0.6 hours and the terminal half-life from 3.5 18.4 hours (mean 8.8 hours), depending on the study population and method of determination. Metabolites were formed with a half-life of 10 hours and excreted with a half-life of approximately 2 hours. Thus, formation of the major metabolite is the rate limiting step in the biodisposition of temazepam. There is no accumulation of metabolites. A dose-proportional relationship has been established for the area under the plasma concentration/time curve over the 15 30 mg dose range.","PeriodicalId":74327,"journal":{"name":"Nursing times","volume":"102 14 1","pages":"31"},"PeriodicalIF":0.0000,"publicationDate":"2020-03-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"5","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Nursing times","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.4324/9781315825731-103","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 5

Abstract

In a single and multiple dose absorption, distribution, metabolism, and excretion (ADME) study, using 3H labeled drug, temazepam was well absorbed and found to have minimal (8%) first pass metabolism. There were no active metabolites formed and the only significant metabolite present in blood was the O-conjugate. The unchanged drug was 96% bound to plasma proteins. The blood level decline of the parent drug was biphasic with the short half-life ranging from 0.4 0.6 hours and the terminal half-life from 3.5 18.4 hours (mean 8.8 hours), depending on the study population and method of determination. Metabolites were formed with a half-life of 10 hours and excreted with a half-life of approximately 2 hours. Thus, formation of the major metabolite is the rate limiting step in the biodisposition of temazepam. There is no accumulation of metabolites. A dose-proportional relationship has been established for the area under the plasma concentration/time curve over the 15 30 mg dose range.
羟基安定。
在一项单剂量和多剂量吸收、分布、代谢和排泄(ADME)研究中,使用3H标记的药物,替马西泮被很好地吸收,并发现具有最小(8%)的首过代谢。没有形成活性代谢产物,血液中存在的唯一重要代谢产物是O-缀合物。不变的药物96%与血浆蛋白结合。母体药物的血液水平下降是双相的,短半衰期为0.4至0.6小时,终半衰期为3.5至18.4小时(平均8.8小时),具体取决于研究人群和测定方法。代谢物的形成半衰期为10小时,排泄半衰期约为2小时。因此,主要代谢产物的形成是替马西泮生物分散的限速步骤。没有代谢物的积累。已经建立了在15-30mg剂量范围内血浆浓度/时间曲线下的面积的剂量比例关系。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
求助全文
约1分钟内获得全文 求助全文
来源期刊
自引率
0.00%
发文量
0
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
确定
请完成安全验证×
copy
已复制链接
快去分享给好友吧!
我知道了
右上角分享
点击右上角分享
0
联系我们:info@booksci.cn Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。 Copyright © 2023 布克学术 All rights reserved.
京ICP备2023020795号-1
ghs 京公网安备 11010802042870号
Book学术文献互助
Book学术文献互助群
群 号:481959085
Book学术官方微信