Plasma levels of (+) and (-)-propranolol and 4-hydroxypropranolol after administration of racemic (+/-)-propranolol in man.
Plasma levels of (+) and (-)-propranolol and 4-hydroxypropranolol after administration of racemic (+/-)-propranolol in man.
复制标题
给予人外消旋(i-)-普萘洛尔后，()和(-)-普萘洛尔以及4-羟基普萘洛尔的血浆水平。
DOI：
10.1111/j.1365-2125.1982.tb04937.x
复制
发表时间：
1982
影响因子：
3.4
通讯作者：
K. Tawara
中科院分区：
文献类型：
--
作者：
C. von Bahr;J. Hermansson;K. Tawara
1我们给15名健康志愿者口服（40 mg）和静脉注射（5-10 mg）单剂量外消旋（+/-）-普萘洛尔，以了解（-）-和（+）-普萘洛尔血浆浓度与普萘洛尔和4-羟基普萘洛尔总浓度之比的变化有多大。2口服（+/-）普萘洛尔40 mg后2小时的总普萘洛尔（+/-）水平为21 - 580 nmol/l，4-羟基普萘洛尔为0 - 33 nmol/l。它们的水平没有相关性。（-）-和（+）-普萘洛尔水平之间的比值为0.99 - 2.04。两种异构体的血浆半衰期通常相似。3我们的结论是，在大多数关于血浆浓度和效应（β-肾上腺素受体阻滞）之间关系的单次给药研究中，没有必要分别定量（+）-和（-）-普萘洛尔水平，因为总（+/-）血浆普萘洛尔水平的变化远远大于（-）-和（+）-普萘洛尔之间的比值。
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.