在人体中给予消旋（±）-普萘洛尔后（+）和（-）-普萘洛尔及4-羟基普萘洛尔的血浆水平。
Plasma levels of (+) and (-)-propranolol and 4-hydroxypropranolol after administration of racemic (+/-)-propranolol in man.
作者信息
Von Bahr C, Hermansson J, Tawara K
出版信息
Br J Clin Pharmacol. 1982 Jul;14(1):79-82. doi: 10.1111/j.1365-2125.1982.tb04937.x.
Abstract
1 We have given fifteen healthy volunteers single doses of racemic (+/-)-propranolol orally (40 mg) and intravenously (5-10 mg) to find out how large the variation was of the ratio between (-)- and (+)-propranolol plasma levels in relation to that of total levels of propranolol and 4-hydroxypropranolol. 2 Total propranolol (+/-)-levels 2 h after a 40 mg oral dose of (+/-)-propranolol varied from 21 to 580 nmol/l and those of 4-hydroxypropranolol from 0 to 33 nmol/l. Their levels did not correlate. The ratio between (-)- and (+)-propranolol levels varied from 0.99 to 2.04. The plasma half-lives of the two isomers were usually similar. 3 We conclude that in most single doses studies on relationships between plasma concentrations and effects (beta-adrenoceptor blockade) it is not necessary to quantitate (+)- and (-)-propranolol levels separately since total (+/-) plasma propranolol levels varied much more than the ratio between (-)- and (+)-propranolol.
摘要
- 我们给15名健康志愿者口服（40毫克）和静脉注射（5 - 10毫克）消旋（±）-普萘洛尔单剂量，以了解（-）-和（+）-普萘洛尔血浆水平之比相对于普萘洛尔和4 - 羟基普萘洛尔总水平之比的变化有多大。2. 口服40毫克（±）-普萘洛尔2小时后，普萘洛尔（±）总水平在21至580纳摩尔/升之间变化，4 - 羟基普萘洛尔水平在0至33纳摩尔/升之间变化。它们的水平不相关。（-）-和（+）-普萘洛尔水平之比在0.99至2.04之间变化。两种异构体的血浆半衰期通常相似。3. 我们得出结论，在大多数关于血浆浓度与效应（β - 肾上腺素能受体阻滞）关系的单剂量研究中，没有必要分别定量（+）-和（-）-普萘洛尔水平，因为普萘洛尔（±）血浆总水平的变化远大于（-）-和（+）-普萘洛尔之比的变化。
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