The pharmacology of carvedilol

@article{Ruffolo2005ThePO,
  title={The pharmacology of carvedilol},
  author={Robert R. Ruffolo and Miklos Gellai and Jacob Paul Hieble and Robert Nicholas Willette and Andrew J. Nichols},
  journal={European Journal of Clinical Pharmacology},
  year={2005},
  volume={38},
  pages={S82-S88}
}
SummaryCarvedilol is a potent antihypertensive agent with a dual mechanism of action. At relatively low concentrations it is a competitive β-adrenoceptor antagonist and a vasodilator, whereas at higher concentrations it is also a calcium channel antagonist. The antihypertensive activity of carvedilol is characterized by a decrease in peripheral vascular resistance, resulting from the vasodilator activity of the compound, with no reflex tachycardia, as a result of β-adrenoceptor blockade. The… 
Clinical pharmacology of carvedilol
SummaryAnimal work has shown that carvedilol is a nonselective β-blocking drug. It has a vasodilator action from α-receptor blockade, but there is evidence that it has further action to relax smooth
Carvedilol and the kidney
  • A. Dupont
  • Medicine, Biology
    The clinical investigator
  • 2004
TLDR
It is concluded from these studies that renal perfusion and renal function are well maintained during acute and chronic treatment with carvedilol.
Pharmacological profile of β-adrenoceptor blockers with vasodilating properties, especially carvedilol — rationale for clinical use
TLDR
Carvedilol is a dual-acting drug designed to produce β-blockade and vasodilatation in the same dose range, designed to reduce the total peripheral resistance, and blood flow to the kidneys is preserved.
Pharmacology of Carvedilol: Rationale for Use in Hypertension, Coronary Artery Disease, and Congestive Heart Failure
TLDR
The multiple actions of carvedilol may provide the underlying pharmacologic rationale for the use of this drug in the treatment of patients with coronary artery disease or congestive heart failure, and these actions may account, at least in part, for the reduction in mortality produced by carveilol in clinical trials involving patients with congestiveheart failure.
Electrophysiologic Effects of Carvedilol: Is Carvedilol an Antiarrhythmic Agent?
TLDR
Experimental data available on the electrophysiologic properties of carvedilol are reviewed, with a focus on their clinical relevance.
The dose dependency of the (x- and ,-adrenoceptor antagonist activity of carvedilol in man
TLDR
In conclusion, carvedilol 6.25, 12.5 and 25 mg demonstrated ,-adrenoceptor antagonist activity with some evidence for a-adRenoceptor antagonists activity with the 25 mg dose, and labetalol 400 mg showed both ,B- and a-Adreno receptor antagonist activity, with a IP- to a- adrenOceptor antagonist ratio of approximately 4 to 1.
Comparison of the antihypertensive effects of carvedilol and metoprolol on resting and exercise blood pressure
TLDR
Carvedilol was even effective in the treatment of patients whose blood pressure was unsatisfactorily controlled by metoprolol, showing the importance of the vasodilation component of carvedilol.
β-Adrenoceptor Blocker Carvedilol Provides Cardioprotection via an Adenosine-Dependent Mechanism in Ischemic Canine Hearts
TLDR
Carvedilol shows a cardioprotective effect against ischemia and/or reperfusion injury via adenosine-dependent mechanisms in dogs and in human umbilical vein endothelial cells cultured with or without xanthine andxanthine oxidase, carvedilol caused an increase of ecto-5′-nucleotidase activity.
...
...

References

SHOWING 1-10 OF 15 REFERENCES
Pharmacological Profile of Carvedilol, a Compound with &bgr;‐Blocking and Vasodilating Properties*
TLDR
The balanced ratio of the vasodilatation and &bgr;‐blocking actions makes this substance an interesting choice for the treatment of various cardiovascular diseases.
Studies on the Mode of Vasodilating Action of Carvedilol*
TLDR
Investigations were performed on isolated rat aortic strips and in pithed rats in order to elucidate the mechanism of vasorelaxation or the acute blood pressure lowering effect induced by carvedilol, and it is suggested that a not yet defined postreceptor mechanism is involved.
Pharmacology of carvedilol.
Alpha and beta adrenoceptor blocking action of carvedilol in the canine mesenteric artery and vein.
TLDR
Results indicate that carvedilol blocks alpha 1 and beta adrenoceptors but not alpha 2 adrenoCEPTors in vascular tissues, and also the compound action potentials of sympathetic nerve bundles running along the mesenteric vessels.
The pharmacology of dobutamine.
  • R. Ruffolo
  • Medicine, Biology
    The American journal of the medical sciences
  • 1987
TLDR
The hemodynamic profile of dobutamine in patients with congestive heart failure is derived from a unique and complex series of interactions with alpha- and beta-adrenoceptors in the cardiovascular system.
Vasodilatory Effects of Carvedilol and Pindolol
TLDR
It is concluded that carvedilol and pindolol possess distinct vasodilatory properties and had a stronger hypotensive effect than pINDolol and was well tolerated.
Acute and Long‐Term Hemodynamic Effects of Carvedilol, a Combined &bgr;‐Adrenoceptor Blocking and Precapillary Vasodilating Agent, in Hypertensive Patients
TLDR
It is shown that carvedilol given orally has a useful antihypertensive effect both acutely and during prolonged treatment, and it has an attractive hemodynamic profile, in agreement with the hemodynamic findings in essential hypertension.
SOME QUANTITATIVE USES OF DRUG ANTAGONISTS
TLDR
Various applications of pAx measurements are discussed based on the hypothesis that drugs and drug antagonists compete for receptors according to the mass law, and a new measure, pAh, is introduced to express the activity of unsurmountable antagonists.
...
...