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吲哚洛尔与普萘洛尔浓度-反应关系的对比。

Contrasts between pindolol and propranolol concentration-response relationships.

作者信息

Carruthers S G, Pacha W L, Aellig W H

出版信息

Br J Clin Pharmacol. 1985 Oct;20(4):417-20. doi: 10.1111/j.1365-2125.1985.tb05088.x.

Abstract

The plasma concentration-response relationships of oral and intravenous pindolol and propranolol have been studied in a group of eight healthy male subjects who received each dosage form in a randomized single-blind cross-over manner. Despite similar elimination half-lives, the duration of action of pindolol was longer than that of propranolol. This longer duration of action was associated with a flatter concentration-response curve for pindolol and may be related to the partial agonist activity of pindolol. Propranolol concentration-response curves were dependent on the route of drug administration whereas pindolol curves were similar following oral and intravenous routes of administration.

摘要

在一组8名健康男性受试者中,以随机单盲交叉方式给予口服和静脉注射的吲哚洛尔及普萘洛尔,研究了它们的血浆浓度-反应关系。尽管吲哚洛尔和普萘洛尔的消除半衰期相似,但吲哚洛尔的作用持续时间比普萘洛尔长。这种较长的作用持续时间与吲哚洛尔较平缓的浓度-反应曲线有关,可能与吲哚洛尔的部分激动剂活性有关。普萘洛尔的浓度-反应曲线取决于给药途径,而吲哚洛尔的曲线在口服和静脉给药后相似。

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本文引用的文献

1
Measurement of partial agonist activity of pindolol.吲哚洛尔部分激动剂活性的测定。
Clin Pharmacol Ther. 1981 Nov;30(5):581-6. doi: 10.1038/clpt.1981.207.
3
Cardiac dose-response relationships of oral and intravenous pindolol.口服和静脉注射吲哚洛尔的心脏剂量-反应关系。
Br J Clin Pharmacol. 1982;13(Suppl 2):193S-198S. doi: 10.1111/j.1365-2125.1982.tb01910.x.
4
Operational models of pharmacological agonism.药理学激动作用的操作模型。
Proc R Soc Lond B Biol Sci. 1983 Dec 22;220(1219):141-62. doi: 10.1098/rspb.1983.0093.

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