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血浆蛋白结合、注射速率与硫喷妥钠麻醉效果之间的相互关系。

Interrelation between plasma protein binding, rate of injection and the anaesthetic effect of thiopental.

作者信息

Kurz H, Fichtl B

出版信息

Biopharm Drug Dispos. 1981 Apr-Jun;2(2):191-6. doi: 10.1002/bdd.2510020212.

DOI:10.1002/bdd.2510020212
PMID:7248482
Abstract
  1. Following thiopental injection to rabbits in doses of 5 mg kg-1 intravenously (i.v.) the sleeping time lasted longer after injection by bolus than after administration made more slowly over 30 or 60s, respectively. 2. Peak concentration in the blood of the animals after bolus injection was about four time higher than after slow injection. 3. The determination of protein binding showed that the unbound fraction of thiopental at the high concentration following bolus injection is almost doubled compared with the unbound concentration following the slow injections. Therefore it is concluded that this contributes to an increased concentration of thiopental in the brain during the initial phase of distribution thus extending the sleeping time. 4. The results from experiments using a distribution model give additional evidence supporting this conception.
摘要
  1. 给兔子静脉注射剂量为5毫克/千克的硫喷妥钠后,推注给药后的睡眠时间比分别在30秒或60秒内缓慢给药后的睡眠时间更长。2. 推注注射后动物血液中的峰值浓度比缓慢注射后高约四倍。3. 蛋白质结合测定表明,推注注射后高浓度下硫喷妥钠的未结合部分与缓慢注射后的未结合浓度相比几乎增加了一倍。因此得出结论,这有助于在分布的初始阶段大脑中硫喷妥钠浓度的增加,从而延长睡眠时间。4. 使用分布模型的实验结果提供了支持这一概念的额外证据。

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Interrelation between plasma protein binding, rate of injection and the anaesthetic effect of thiopental.血浆蛋白结合、注射速率与硫喷妥钠麻醉效果之间的相互关系。
Biopharm Drug Dispos. 1981 Apr-Jun;2(2):191-6. doi: 10.1002/bdd.2510020212.
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引用本文的文献

1
Pharmacodynamics and pharmacokinetics of thiopental.硫喷妥钠的药效学与药代动力学。
Clin Pharmacokinet. 1998 Aug;35(2):95-134. doi: 10.2165/00003088-199835020-00002.