solid dispersions in water-soluble carriers have attracted considerable interest as a means of improving the dissolution rate, and hence possibly bioavailability, of a range of hydrophobic drugs. the poor solubility of carvedilol leads to poor dissolution and hence variation in bioavailability. the purpose of the present investigation was to increase the solubility and dissolution rate of carve...

As a third-generation β-adrenergic blocker (β-blocker), carvedilol is able to reverse cardiac structural remodeling, however, its mechanism of action remains unclear. In order to investigate this mechanism, hypertension was induced in rats by unilateral renal artery narrowing. Additionally, carvedilol alone or carvedilol combined with L-NAME, a specific inhibitor of nitric oxide (NO) synthase, ...

BACKGROUND Postoperative atrial fibrillation (POAF) remains the most common complication after cardiac surgery. Current guidelines recommend β-blockers to prevent POAF. Carvedilol is a non-selective β-adrenergic blocker with anti-inflammatory, antioxidant, and multiple cationic channel blocking properties. These unique properties of carvedilol have generated interest in its use as a prophylaxis...

The stress-related catecholamine hormones and the α- and β-adrenergic receptors (α- and β-AR) may affect carcinogenesis. The β-AR GRK/β-arrestin biased agonist carvedilol can induce β-AR-mediated transactivation of the EGFR. The initial purpose of this study was to determine whether carvedilol, through activation of EGFR, can promote cancer. Carvedilol failed to promote anchorage-independent gr...

Spherically agglomerated solid dispersions of carvedilol (CAR) were prepared with polyvinyl-pyrrolidone (PVP) using acetone, water and dichloromethane as solvent, non-solvent and bridging liquid, respectively. The prepared agglomerates were evaluated for its percentage yield, drug content, morphology, thermal behavior, micromeritic properties, aqueous solubility and in vitro drug release. Diffe...

UNLABELLED We evaluated whether myocardial beta-adrenergic receptor (beta-AR) density, as determined by 11C-CGP12177 PET, could predict improvement of cardiac function by beta-blocker carvedilol treatment in patients with idiopathic dilated cardiomyopathy (IDC). METHODS Ten patients with IDC (left ventricular ejection fraction [LVEF]<45%) were studied. Myocardial beta-AR density was estimated...

BACKGROUND Data suggest that carvedilol possesses antioxidant properties that might provide vascular protection. We sought to compare the effects of carvedilol and metoprolol tartrate on endothelial function and oxidative stress in a head-to-head trial. METHODS Thirty-four patients with type 2 diabetes mellitus (T2DM) and hypertension were randomized to receive either carvedilol (n = 16) or m...

BACKGROUND Carvedilol appears to be more effective than propranolol in the treatment of portal hypertension in cirrhotic patients. Aim. To compare the effects of carvedilol vs. propranolol on systemic and splanchnic haemodynamics and to evaluate the adverse events associated with these treatments. MATERIAL AND METHODS We performed a systematic review following the Cochrane and PRISMA recommen...

Carvedilol functions as a nonselective β-adrenergic receptor (AR)/α1-AR antagonist that is used for treatment of hypertension and heart failure. Carvedilol has been shown to function as an inverse agonist, inhibiting G protein activation while stimulating β-arrestin-dependent signaling and inducing receptor desensitization. In the present study, short-circuit current (Isc) measurements using hu...

Carvedilol is a beta-adrenoceptor antagonist used for treating chronic heart failure (CHF). Two clinical studies were conducted to evaluate the population pharmacokinetics and pharmacodynamics of R- and S-carvedilol, and associated covariates, in patients with CHF. Fifty-eight patients (male=45, female=13) with New York Heart Association class I-IV CHF were enrolled in two clinical studies. R- ...