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  • 1
    ISSN: 1432-1041
    Keywords: stereoisomers ; α-blockade ; β-blockade ; carvedilol
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The racemic compound carvedilol possesses two complementary pharmacological effects, vasodilation and β-blockade. TheR- andS-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 theS-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 ofS-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 theS-enantiomer would lead to relatively strong β-blockade with only a weak vasodilating effect. TheR-enantiomer alone would act only as a hypotensive agent without β-blockade.
    Type of Medium: Electronic Resource
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  • 2
    ISSN: 1432-1041
    Keywords: carvedilol ; nitrendipine ; antihypertensive treatment ; elderly patients ; essential hypertension
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Carvedilol and nitrendipine were given for 12 weeks in a double-blind study to 81 elderly patients (≥ 60 years) with essential hypertension. The effects on blood pressure were measured (Riva Rocci) before medication and after 2 h with the patient in a lying and standing position after 4 weeks of placebo therapy as well as after 4, 8 and 12 weeks of treatment. Carvedilol (25 mg/o. d.) reduced blood pressure measured in the supine and erect position very successfully, similar to the reduction achieved with nitrendipine (20 mg/o. d.), without influencing the pulse rate. Both substances were well tolerated. Carvedilol is an alternative substance for lowering high blood pressure in elderly hypertensive patients.
    Type of Medium: Electronic Resource
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  • 3
    ISSN: 1432-1440
    Keywords: Carvedilol ; β1 and β2 Receptors ; α1-Blockade ; Myocardial adrenergic receptors ; Lymphocyte β-adrenergic receptors
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary Carvedilol, a new β-blocker with vasodilating properties due to α1-blockade, was investigated in preparations of human ventricular myocardium. Carvedilol demonstrated a high affinity and is a slightly β1-selective competitive β-blocking agent, with a K D for β1-receptors of approximately 4–5 nM and a mild selectivity for β1 vs. β2 receptors of 6- to 39-fold, depending on the method employed to assess subtype potency. In addition, carvedilol was also a potent α1-blocking agent, with a β1:α1 blocking relative potency of 1.7-fold. In human lymphocytes containing β2-receptors and in human myocardial membranes containing both β1- and β2-receptors carvedilol exhibited the unique property of guanine nucleotide modulatable binding. Despite this, no intrinsic sympathomimetic activity of carvedilol was detected in preparations of isolated human heart or in myocardial membranes. Vasodilation related to α1-blockade and the lack of intrinsic activity should translate into improved tolerability and good efficacy in the treatment of heart failure.
    Type of Medium: Electronic Resource
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