Pharmacological Profile of Carvedilol as a β-Blocking Agent with Vasodilating and Hypotensive Properties

Sponer, G.; Bartsch, W.; Strein, K.; Müller-Beckmann, B.; Böhm, E

doi:10.1097/00005344-198703000-00009

Cited by 109 publications

(50 citation statements)

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“…These drugs were also administered to control groups of 8 healthy animals each without immunization with myosin for 3 weeks. Doses were selected on the basis of previous findings 17 to ensure a near-equipotent ␤1-AR blocking effect.…”

Section: Protocol Imentioning

confidence: 99%

β2-Adrenergic Agonists Suppress Rat Autoimmune Myocarditis

et al. 2006

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Background-The therapeutic potential of ␤2-adrenergic receptor (AR) agonists in the treatment of autoimmune diseases has been reported. However, the role of these drugs in the myocardial structure-induced autoimmune process, which is thought to play a crucial role in the progression of myocarditis to subsequent complications, has not been elucidated. Methods and Results-Experimental autoimmune myocarditis (EAM) was induced in rats by immunization with cardiac myosin. On daily administration from day 0 after immunization, the ␤2-selective AR agonists formoterol or salbutamol ameliorated EAM on day 21 and increased myocardial interleukin-10/interferon-␥ mRNA levels. Propranolol, a nonselective ␤-AR antagonist, aggravated EAM on day 21 and decreased mRNA levels, whereas metoprolol, a ␤1-selective AR antagonist, showed no effect. These results were reflected in vivo by the proliferation of cardiac myosin-primed lymph node cells from drug-treated rats. In vitro addition of ␤2-selective AR agonists inhibited the activation of cardiac myosin fragment-specific myocarditogenic T lymphocytes, and this effect was reversed by ICI118,551, a ␤2-selective AR antagonist. Furthermore, treatment with 2 different ␤2-selective AR agonists starting on day 14 also ameliorated EAM on day 21. Conclusions-␤2-AR

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Section: Protocol Imentioning

confidence: 99%

β2-Adrenergic Agonists Suppress Rat Autoimmune Myocarditis

et al. 2006

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“…Carvedilol (SK & F 105517, BM 14190) is a vasodilator with 3-adrenoceptor blocking properties, under development for the treatment of hypertension and angina pectoris (Cubeddu et al, 1987;Sponer et al, 1987). The concomitant administration of carvedilol with digoxin is therefore possible.…”

Section: Introductionmentioning

confidence: 99%

Carvedilol increases the systemic bioavailability of oral digoxin.

Mey¹,

Brendel²,

Enterling³

1990

Brit J Clinical Pharma

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The effects of a single oral dose of 25 mg carvedilol on the plasma and urinary kinetics of digoxin after an oral and intravenous 0.5 mg dose, were investigated in two separate double-blind, placebo-controlled, period-balanced cross-over studies in healthy male subjects. Carvedilol increased the mean maximum plasma concentration and the area under the plasma concentration time-curve of digoxin when administered orally. The effects were virtually confined to the first 4 h after dosing, and the apparent terminal disposition rate constant was not changed. Carvedilol did not alter the plasma and urinary kinetics of intravenously administered digoxin.

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“…This agent produces a decrease in blood pressure with a reduction in total peripheral resistance attributable to its vasodilating activity (1,2). In our previous report (3), the contribution of the potent ablocking activity of carvedilol to the reduction in blood pressure was strongly suggested.…”

mentioning

confidence: 95%

“…Carvedilol is a noncardioselective a-adrenoceptor blocking agent without partial agonist activity (1). This agent produces a decrease in blood pressure with a reduction in total peripheral resistance attributable to its vasodilating activity (1,2).…”

mentioning

confidence: 99%

Effect of carvedilol on venous return: A mechanism of reduction in blood pressure.

et al. 1991

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ABSTRACT-We studied the effect of carvedilol, a ~Q-blocker with a potent a-blocking activity, on venous return in anesthetized dogs. Though 3,ug/kg of carvedilol caused a slight increase in blood pressure and total peripheral resistance, these changes disappeared by further doses of the agent. On the other hand, each dose of carvedilol (3 -100 ,a g/kg) decreased venous return significantly and dose-dependently. These results indicate that the hypotensive effect of carvedilol mainly depends on the decrease in venous return rather than arterial vasodilation.

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Pharmacological Profile of Carvedilol as a β-Blocking Agent with Vasodilating and Hypotensive Properties

Cited by 109 publications

References 0 publications

β2-Adrenergic Agonists Suppress Rat Autoimmune Myocarditis

β2-Adrenergic Agonists Suppress Rat Autoimmune Myocarditis

Carvedilol increases the systemic bioavailability of oral digoxin.

Effect of carvedilol on venous return: A mechanism of reduction in blood pressure.

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