title: Pharmacological characteristics of the stereoisomers of carvedilol.
abstract: The racemic compound carvedilol possesses two complementary pharmacological effects, vasodilation and beta-blockade. The R- and S-enantiomers of carvedilol and the racemate were investigated with respect to the beta-blocking, vasodilating, and hypotensive actions. In agreement with results obtained with other beta-blockers, only the S-enantiomer of carvedilol exerts beta-blocking effects. In contrast, no substantial difference between the enantiomers could be seen with respect to alpha-blockade. The greater hypotensive activity of S-carvedilol may be attributed to beta-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 beta-blockade with only a weak vasodilating effect. The R-enantiomer alone would act only as a hypotensive agent without beta-blockade.
authors.affiliation: Department of Cardiovascular Research, Boehringer Mannheim GmbH, Federal Republic of Germany.
authors.forename: W
authors.initials: W
authors.lastname: Bartsch
authors.forename: G
authors.initials: G
authors.lastname: Sponer
authors.forename: K
authors.initials: K
authors.lastname: Strein
authors.forename: B
authors.initials: B
authors.lastname: Müller-Beckmann
authors.forename: L
authors.initials: L
authors.lastname: Kling
authors.forename: E
authors.initials: E
authors.lastname: Böhm
authors.forename: U
authors.initials: U
authors.lastname: Martin
authors.forename: H O
authors.initials: HO
authors.lastname: Borbe
mesh_terms: D000317:Adrenergic alpha-Antagonists; D000319:Adrenergic beta-Antagonists / Q000494:pharmacology*; D000818:Animals; D001013:Aorta, Thoracic / Q000187:drug effects; D001794:Blood Pressure / Q000187:drug effects; D002227:Carbazoles / Q000494:pharmacology*; D000077261:Carvedilol; D003655:Decerebrate State; D006339:Heart Rate / Q000187:drug effects; D006973:Hypertension / Q000188:drug therapy; D066298:In Vitro Techniques; D007545:Isoproterenol / Q000037:antagonists & inhibitors; D008729:Methoxamine / Q000494:pharmacology; D009119:Muscle Contraction / Q000187:drug effects; D009131:Muscle, Smooth, Vascular / Q000187:drug effects; D011412:Propanolamines / Q000494:pharmacology*; D011817:Rabbits; D051381:Rats; D011918:Rats, Inbred SHR; D011942:Receptors, Adrenergic, alpha / Q000378:metabolism; D011943:Receptors, Adrenergic, beta / Q000378:metabolism; D013237:Stereoisomerism
chemical_list: D000317:Adrenergic alpha-Antagonists; D000319:Adrenergic beta-Antagonists; D002227:Carbazoles; D011412:Propanolamines; D011942:Receptors, Adrenergic, alpha; D011943:Receptors, Adrenergic, beta; D000077261:Carvedilol; D008729:Methoxamine; D007545:Isoproterenol