Clinical updates on carvedilol: a first choice β-blocker in the treatment of cardiovascular diseases

  title={Clinical updates on carvedilol: a first choice $\beta$-blocker in the treatment of cardiovascular diseases},
  author={Subhash Chandra Chakraborty and Dali Shukla and Brahmeshwar Mishra and Sanjay Singh},
  journal={Expert Opinion on Drug Metabolism \& Toxicology},
  pages={237 - 250}
Importance of the field: Carvedilol, a non-selective β-blocker, has recently drawn attention because of its therapeutic benefits over other prescribed analogues for the treatment of cardiovascular diseases (CVDs). Areas covered in this review: The present review attempts to present the clinical efficacy of carvedilol in comparison to other available β-blockers. The literature search was carried out in three electronic databases (Unbound Medline, Pubmed and Sciencedirect) and internet search… 
Use of carvedilol in hypertension: an update
The present report provides an overview of the main clinical studies concerning carvedilol administered as either monotherapy or in combination with another antihypertensive or more frequently a diuretic agent, with particular focus on the additional benefits beyond blood pressure reduction.
Association of Common Polymorphisms in &bgr;1-adrenergic Receptor With Antihypertensive Response to Carvedilol
This study provides the first evidence to support that ADRB1 polymorphisms play an important role in the DBPs response to carvedilol treatment in patients with essential hypertension.
Carvedilol induces endogenous hydrogen sulfide tissue concentration changes in various mouse organs.
The study has proven that carvedilol affects H2S tissue concentration in different mouse organs and induced a change in H 2S tissue level in the heart - an increase by 75.5%.
Analysis of carvedilol enantiomers in human plasma using chiral stationary phase column and liquid chromatography with tandem mass spectrometry.
This is the first study of carvedilol enantiomers in human plasma using a chiral stationary phase column and liquid chromatography with tandem mass spectrometry to study enantioselectivity in the pharmacokinetics of carveilol administered as a single dose of 25 mg to a hypertensive patient.
Formulation and evaluation of sustained release tablets of carvedilol
The object of this research work was to formulate, develop and evaluate the Sustained Release (SR) Tablets of anti hypertensive drug (Carvedilol). The tablets were prepared relatively small dose of
Investigation of carvedilol-evoked Ca2+ movement and death in human oral cancer cells
Collectively, in OC2 cells, carvedilol induced [Ca2+]i rise by causing phospholipase C-independent Ca2+ release from mitochondria and non-endoplasmic reticulum stores, and Ca 2+ influx via protein kinase C -regulated channels, and carvingilolinduced cell death in a Ca2-independent manner that involved apoptosis.
Tempol prevents cardiac oxidative damage and left ventricular dysfunction in the PPAR-α KO mouse.
It is demonstrated that treatment with the SOD mimetic tempol can prevent cardiac dysfunction in PPAR-α KO mice by reducing the oxidation of contractile proteins and activation of the glutathione peroxidase/glutathione reductase system.
UPLC-MS/MS assay for the simultaneous quantification of carvedilol and its active metabolite 4'-hydroxyphenyl carvedilol in human plasma to support a bioequivalence study in healthy volunteers.
An ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method has been developed and successfully applied to support a bioequivalence study of 12.5 mg carvedilol tablets in 34 healthy subjects.
Labrasol-Enriched Nanoliposomal Formulation: Novel Approach to Improve Oral Absorption of Water-Insoluble Drug, Carvedilol
The results reported the successful development of biocompatible Labrasol-enriched carvedilol nanoliposomal formulation with a significant oral enhancement capability.


Profile of carvedilol controlled-release: a new once-daily formulation of carvedilol
  • G. Fonarow
  • Medicine
    Expert opinion on pharmacotherapy
  • 2006
A once-daily formulation of carvedilol (controlled release) is expected to provide not only the same life-prolonging benefits of twice-daily carveilol, but also the convenience of once- daily dosing.
Preclinical and clinical pharmacology of carvedilol.
The cardioprotection observed with carveilol is greater than that provided by beta-adrenoceptor antagonists alone, suggesting that the additional activities of carvedilol may provide benefit in the setting of myocardial ischaemia.
Safety and efficacy of carvedilol in very elderly diabetic patients with heart failure
Compared to younger ones, also in older patients, diabetes does not negatively influence the safety, tolerability and efficacy of carvedilol, but diabetes remains a strong prognostic factor limiting the reversibility of left ventricular systolic dysfunction and the effect of treatment on subsequent outcome.
Prospective, randomized comparison of effect of long-term treatment with metoprolol or carvedilol on symptoms, exercise, ejection fraction, and oxidative stress in heart failure.
Carvedilol and metoprolol showed parallel beneficial effects in the measured parameters over 6 months, with no relevant between-group differences in this heart failure population.
Are Tolerability Concerns a Class Effect of Beta-Blockers in Treating Patients with Hypertension?
By examining the differences among members of the β-blocker class, it may be possible to determine whether and which tolerability issues are indeed a class effect ofβ-blockers or whether these agents should be evaluated on a case-by-case basis.
Carvedilol therapy in pediatric patients with congestive heart failure: a study investigating clinical and pharmacokinetic parameters.
Pediatric patients with CHF not responding to standard therapy may benefit from oral carvedilol treatment, and the observed increased elimination of carveilol in children suggests that optimal dosing strategies need to be further defined among the pediatric population.
The pharmacokinetics of carvedilol and its metabolites after single and multiple dose oral administration in patients with hypertension and renal insufficiency
Compared with controls, average AUC values for carvedilol were approximately 40% and 50% higher on study Days 1 and 9 in patients with renal insufficiency, primarily due to higher R-carvedilol concentrations with only a small change (<20%) in S-carvetolol concentrations, the isomer possessing β-blocking activity.
β‐Blockers in Hypertension: A Reassessment of the Benefit of Combined α‐/β‐Blockade
A reappraisal of the role of selected agents, such as the combined α‐/β‐blocker carvedilol, in the long‐term treatment of hypertension is recommended.
Carvedilol, a novel vasodilating beta-blocker with the potential for cardiovascular organ protection.
These unique multiple actions of carvedilol provide not only for adequate control of elevated blood pressure, but may also provide for protection of the heart and vasculature from secondary damage due to hypertension itself, as well as from other causes.