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异戊巴比妥、戊巴比妥和苯妥英在健康志愿者和尿毒症患者体内与血细胞及血浆蛋白的结合情况。

Binding of amobarbital, pentobarbital and diphenylhydantoin to blood cells and plasma proteins in healthy volunteers and uraemic patients.

作者信息

Ehrnebo M, Odar-Cederlöf I

出版信息

Eur J Clin Pharmacol. 1975 Aug 14;8(6):445-53. doi: 10.1007/BF00562320.

Abstract

By equilibrium dialysis of human plasma it has been shown that the binding of pentobarbital and diphenylhydantoin to plasma proteins is decreased in uraemic patients (46 and 74 per cent bound, respectively) compared to healthy volunteers (61 and 88 per cent bound). The degree of binding of pentobarbital was significantly correlated with that of diphenylhydantoin and amobarbital, which suggests similarity of their binding sites. Appreciable proportions of the drugs were found in blood cells both in healthy and uraemic subjects. As expected, the distribution of drugs in whole blood was different in the uraemics from healthy subjects, because of the decreased plasma protein binding and the lowered red cell count in uraemia. Analysis of the data showed that the ratio between the concentrations in blood cells and plasma water in uraemic patients was not significantly different from that in healthy subjects.

摘要

通过对人血浆进行平衡透析表明,与健康志愿者相比(苯巴比妥和苯妥英分别有61%和88%与血浆蛋白结合),尿毒症患者中苯巴比妥和苯妥英与血浆蛋白的结合减少(分别为46%和74%与血浆蛋白结合)。苯巴比妥的结合程度与苯妥英和异戊巴比妥的结合程度显著相关,这表明它们的结合位点具有相似性。在健康受试者和尿毒症受试者的血细胞中均发现有相当比例的药物。正如预期的那样,由于血浆蛋白结合减少以及尿毒症患者红细胞计数降低,尿毒症患者全血中药物的分布与健康受试者不同。对数据的分析表明,尿毒症患者血细胞与血浆水中的浓度比与健康受试者相比无显著差异。

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