心得安在健康志愿者中的浓度-效应关系：一项回顾性分析。
Concentration-effect relationship of oxprenolol in healthy volunteers: a retrospective analysis.
作者信息
Racine-Poon A, Moppert J
出版信息
Br J Clin Pharmacol. 1985;19 Suppl 2(Suppl 2):143S-149S. doi: 10.1111/j.1365-2125.1985.tb02755.x.
Abstract
A mathematical model describing the relationship between plasma concentrations of oxprenolol and submaximal-exercise heart rates has been developed on the basis of data available from 34 healthy volunteers. This relationship, which is exponential in type, is consistent with the 'law of diminishing returns', and is independent of the pharmaceutical formulations used; it appears to be established instantaneously, and is not modified by repeated drug administration over 8 days. At oxprenolol concentrations of 190-250 ng/ml, between half and three-quarters of the subjects investigated reached 90% of their estimated maximum levels of beta-adrenoceptor blockade.
摘要
基于34名健康志愿者提供的数据，建立了一个描述氧烯洛尔血浆浓度与次最大运动心率之间关系的数学模型。这种呈指数型的关系符合“收益递减规律”，且与所用药物制剂无关；它似乎能瞬间建立，并且在8天内反复给药也不会改变。在氧烯洛尔浓度为190 - 250纳克/毫升时，半数至四分之三的受试对象达到了其估计最大β-肾上腺素能受体阻滞水平的90%。
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本文引用的文献
1
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Clin Pharmacokinet. 1981 Nov-Dec;6(6):429-53. doi: 10.2165/00003088-198106060-00002.
2
Initiation and maintenance of beta-blockade with intravenous oxprenolol.
Eur J Clin Pharmacol. 1983;24(1):7-14. doi: 10.1007/BF00613920.
3
Kinetics of pharmacologic response.药理反应动力学
Pharmacol Ther. 1982;16(2):143-66. doi: 10.1016/0163-7258(82)90051-1.
4
Ineffectiveness of beta-adrenergic blockers on ventilatory response to carbon dioxide.
Clin Pharmacol Ther. 1982 Sep;32(3):289-94. doi: 10.1038/clpt.1982.162.
5
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6
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7
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10
Simplified method for the determination of oxprenolol and other beta-receptor-blocking agents in biological fluids by gas-liquid chromatography.
J Chromatogr. 1976 Jun 9;121(1):72-5. doi: 10.1016/s0021-9673(00)82299-2.
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