The Effects of Intravenous Carvedilol, A New Multiple Action Vasodilatory β-Blocker, in Congestive Heart Failure

Dasgupta, P; Broadhurst, Paul; Lahiri, Avijit

doi:10.1097/00005344-199118041-00004

Cited by 25 publications

(8 citation statements)

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“…A subsequent trial by the same group demonstrated beneficial hemodynamic effects of intravenous carvedilol in patients with CHF secondary to ischemic heart disease (18). Therapy was continued for 8 weeks with oral carvedilol, 12.5 to 50 mg twice daily, in 15 patients (19).…”

Section: Carvedilol In Congestive Heart Failurementioning

confidence: 99%

“…It was initially observed by Lahiri et al (48) that carvedilol, 50 mg twice daily, given to patients with chronic stable angina and left ventricular dysfunction (ejection fraction of less than 40%) resulted in a significant increase in resting ejection fraction after 2 weeks of therapy. A subsequent trial by the same group demonstrated beneficial hemodynamic effects of intravenous carvedilol in patients with CHF secondary to ischemic heart disease (18). Therapy was continued for 8 weeks with oral carvedilol, 12.5 to 50 mg twice daily, in 15 patients (19).…”

Section: Carvedilol In Congestive Heart Failurementioning

confidence: 99%

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Carvedilol: A Novel Cardiovascular Drug with Multiple Actions

Ruffolo

Boyle

Brooks

et al. 1992

Cardiovascular Drug Reviews

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Carvedilol (Fig. 1) is a novel multiple action drug that has recently been introduced to the market for the treatment of mild to moderate hypertension (7,8,2426). In extensive clinical trials conducted worldwide, comparisons to all major classes of antihypertensive agents, including captopril, nifedipine, and atenolol, have demonstrated that once-daily therapy with carvedilol is both highly efficacious and possesses a favorable side effect profile. Clinical trials are currently in progress to establish the utility of carvedilol in angina and congestive heart failure.Carvedilol is both a competitive P-adrenoceptor antagonist (76,93,94) and an arterial vasodilator (73). At higher concentrations, carvedilol is also a calcium channel antagonist (73,75,93,94). The vasodilatory actions result primarily from a,-adrenoceptor blockade (73,75,76), although in certain vascular beds, calcium channel blockade may also contribute to vasodilation (96,124). In addition to these actions on the heart and vasculature, carvedilol has also been shown to possess significant antioxidant and antiproliferative actions. These multiple actions are responsible for the antihypertensive efficacy of the drug in animals (93,94,105,106) and in humans (7,8,24-26), and may also work in conjunction to provide effective therapy in angina and congestive heart failure.The antihypertensive response produced by carvedilol is associated with a decrease in peripheral vascular resistance with either no change or only a moderate reduction in heart rate. The reduction in peripheral vascular resistance produced by carvedilol is indicative of arterial vasodilation (7,8,108), and the lack of reflex tachycardia is a direct consequence of the P-adrenoceptor blocking property of the drug (7).Carvedilol has been shown in animal models to protect all the major organ systems that comprise the cardiovascular system, specifically the kidney, heart, vasculature, and brain.

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Section: Carvedilol In Congestive Heart Failurementioning

confidence: 99%

Section: Carvedilol In Congestive Heart Failurementioning

confidence: 99%

Carvedilol: A Novel Cardiovascular Drug with Multiple Actions

Ruffolo

Boyle

Brooks

et al. 1992

Cardiovascular Drug Reviews

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show abstract

“…Carvedilol is a nonselective hadrenergic receptor antagonist, with no sympatheticomimetic intrinsic activity. When added to heart failure therapy, carvedilol produces systemic arterial vasodilation without reflex tachycardia due to concomitant antagonism of peripheral vascular a 1 -adrenergic receptors and myocardial betaadrenergic receptors [2,3].…”

Section: Introductionmentioning

confidence: 99%

The effect of β-adrenergic receptor antagonism in cardiac sympathetic neuronal remodeling in patients with heart failure

Chizzola

Freitas

Marinho

et al. 2006

International Journal of Cardiology

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“…Carvedilol also reduces the release of endothelin and scavenges free radicals of oxygen (Feuerstein et al, 1997). It is used to treat systemic arterial hypertension (Cournot et al, 1992;Lund-Johansen et al, 1992) and congestive heart failure (DasGupta et al, 1991) and is purported to improve exercise capacity (Hampton, 1996;Cleland et al, 1996) and longevity in humans (Bristow et al, 1996).…”

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confidence: 99%

Effects of Silibinin on the Pharmacokinetics of Carvedilol after Oral Administration in Rats

Lee¹

2011

Journal of Pharmaceutical Investigation

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This study was designed to investigate the effects of silibinin on the pharmacokinetics of carvedilol after oral administration of carvedilol in rats. Carvedilol was administered orally (3 mg/kg) with oral silibinin (0.3, 1.5 or 6 mg/ kg) and intravenously (1 mg/kg) to rats. The effects of silibinin on P-glycoprotein (P-gp) and cytochrome P450 (CYP) 2C9 and CYP2D6 activity were also evaluated. Silibinin inhibited CYP2C9 and CYP2D6 enzyme activity with 50% inhibition concentration (IC 50) of 5.2 µM and 85.4 µM, respectively. In addition, silibinin significantly enhanced the cellular accumulation of rhodamine-123 in MCF-7/ADR cells overexpressing P-gp. Compared with the control group, the area under the plasma concentration-time curve was significantly increased by 36.3-57.1%, and the peak concentration was significantly increased by 51.1-88.5% in the presence of silibinin after oral administration of carvedilol. Consequently, the relative bioavailability of carvedilol was increased by 1.13-to 1.57-fold and the absolute bioavailability was significantly increased by 38.6-59.7%. The time to reach peak concentration and the terminal half-life were not significant. The enhanced oral bioavailability of carvedilol may result from inhibition of CYP2C9-mediated metabolism and P-gp-mediated efflux of carvedilol rather than inhibition of CYP2D6-mediated metabolism in the intestine and/or in the liver by silibinin.

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The Effects of Intravenous Carvedilol, A New Multiple Action Vasodilatory β-Blocker, in Congestive Heart Failure

Cited by 25 publications

References 0 publications

Carvedilol: A Novel Cardiovascular Drug with Multiple Actions

Carvedilol: A Novel Cardiovascular Drug with Multiple Actions

The effect of β-adrenergic receptor antagonism in cardiac sympathetic neuronal remodeling in patients with heart failure

Effects of Silibinin on the Pharmacokinetics of Carvedilol after Oral Administration in Rats

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