PHARMACOLOGICAL CHARACTERISTICS OF THE STEREOISOMERS OF CARVEDILOL

被引：77

作者：

BARTSCH, W ^{[1
]}

SPONER, G ^{[1
]}

STREIN, K ^{[1
]}

MULLERBECKMANN, B ^{[1
]}

KLING, L ^{[1
]}

BOHM, E ^{[1
]}

MARTIN, U ^{[1
]}

BORBE, HO ^{[1
]}

机构：

[1] ASTA PHARMA AG,DEPT BIOCHEM,FRANKFURT,GERMANY

来源：

EUROPEAN JOURNAL OF CLINICAL PHARMACOLOGY | 1990年 / 38卷

关键词：

α-blockade; β-blockade; carvedilol; stereoisomers;

D O I：

10.1007/BF01409475

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The racemic compound carvedilol possesses two complementary pharmacological effects, vasodilation and β-blockade. The R- and S-enantiomers of carvedilol and the racemate were investigated with respect to the β-blocking, vasodilating, and hypotensive actions. In agreement with results obtained with other β-blockers, only the S-enantiomer of carvedilol exerts β-blocking effects. In contrast, no substantial difference between the enantiomers could be seen with respect to α-blockade. The greater hypotensive activity of S-carvedilol may be attributed to β-blockade, which inhibits counter-regulatory mechanisms provoked by vasodilation. From these results it is concluded that there is a rationale for using carvedilol as the racemate. Using the S-enantiomer would lead to relatively strong β-blockade with only a weak vasodilating effect. The R-enantiomer alone would act only as a hypotensive agent without β-blockade. © 1990 Springer-Verlag.

引用

页码：S104 / S107

页数：4

共 13 条

[1]

ALMIRANTE L, 1966, J MED CHEM, V9, P620

[2] STEREOCHEMISTRY, A BASIS FOR SOPHISTICATED NONSENSE IN PHARMACOKINETICS AND CLINICAL-PHARMACOLOGY [J].