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| J Korean Med Assoc > Volume 50(3); 2007 > Article |
Abstract
Anti-adrenergic medication is very important to the treatment of chronic heart failure because a failing human heart is adrenergically activated. The increase in cardiac adrenergic drive and circulating norepinephrine are damaging to a failing heart. Certain beta-blockers have been shown to improve the cardiac function and symptoms and to reduce the risk of death and hospitalization in patients with heart failure. Recently, the third-generation beta-blockers have emerged for the treatment of heart failure. This article reviews the neurohormonal pathophysiology of heart failure and the different beta-blockers and their effects.
References
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Figure 1
Impact on mortality of carvedilol use at discharge compared with no β blocker at discharge in eligible patients without contraindications
Log-rank test: P<.004
Table 1
Summary of selected clinical trials evaluating beta-blockade therapy in CHF
Differences are statistically significant unless otherwise indicated
Abbreviations: Ex HR, exercise heart rate; LVEF, left ventricular ejection fraction; NA, not applicable; NS, not statistically significant; SD, sudden death
*Approximate equivalence of metoprolol titrate
†Decrease in mean heart rate (not exercise heart rate)
‡Difference compared with metoprolol
MDC=Metoprolol in dilated cardiomyopathy
CIBIS=Cardiac insufficiency bisoprolol study
COPERNICUS=The carvedilol prospective randomized cumulative survival trial
MERIT-HF=The metoprolol CR / XL randomised intervention trial in congestive heart failure
COMET=Commentary on the carvedilol or metoprolol European trial
BEST=Beta-blocker evaluation of survival trial
Table 3
Adrenergic receptor blocking affinities of beta-blocking agent in human receptors*
*Beta receptors are the average of data from radiological binding data in myocardial membranes and recombinant receptors, and inhibition in functional assays; alpha1 receptors are from myocardial membranes. Metoprolol and bisoprolol data are from radiological binding data in myocardial membranes. Nebivolol data are from another laboratory, in guinea pig receptor preparations
†K(Beta1) = average of high-affinity dissociation constant determined from 125I-CYP competition curves in human ventricular myocardial membranes, dissociation constant determined from competition curves in transfected cells expressing recombinant human beta1 receptors, and dissociation constant determined from inhibition of isoproterenol-mediated stimulation of muscle contraction in preparations of nonfailing human heart.
K(Beta2) = average of low-affinity dissociation constant determined from 125I-CYP competition curves, dissociation constant determined from simple curve fitting in transfected cells expressing recombinant human beta2 receptors, and dissociation constant determined from inhibition of isoproterenol-mediated stimulation of adenyl cyclase in membrane preparations of human heart.
K(Alpha1) = dissociation constant determined from 125I-BE2254 competition curves in human ventricular myocardial membranes
‡Based on an alpha1 K1 of 69 nM in human saphenous vein ring segments
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