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β- and α-Adrenoceptor-Agonists and -Antagonists in Chronic Heart Failure

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Adrenergic Mechanisms in Myocardial Ischemia

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Summary

In patients with chronic heart failure, cardiac β-adrenoceptor function is decreased, and this decrease is related to the degree of heart failure. Under these conditions, treatment with β-adrenoceptor agonists seems to be of limited value as it might further down-regulate cardiac β-adrenoceptors, resulting, finally, in a loss of therapeutic efficacy. However, β-adrenoceptor antagonists might have beneficial effects, because they can protect the myocardium from the deleterious effects of elevated endogenous catecholamines and can, simultaneously, restore the previously down-regulated β-adrenoceptor function. Stimulation of cardiac α-adrenoceptors, however, seems not to be of any therapeutic value in patients with chronic heart failure, because a) the number of α-adrenoceptors in the human heart is very low and its function is not completely understood, and b) no α-adrenoceptor agonist is presently available that selectively stimulates cardiac α-adrenoceptors without concomitantly activating vascular α-adrenoceptors. In acute myocardial ischemia, cardiac β-adrenoceptors increase; this increase is — at least in early acute myocardial ischemia — accompanied by an increased β-adrenoceptor functional responsiveness; thus, under these conditions, β-adrenoceptor agonists again might not be of clinical value, while β-adrenoceptor antagonists may exert beneficial effects, because they can block (over)activation of the sensitized β-adrenoceptors by elevated endogenous catecholamines.

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  1. Zentrum für Innere Medizin, Medizinische Klinik und Poliklinik, Abteilung für Nieren- und Hochdruckkrankheiten, Universitätsklinikum, Hufelandstr. 55, D-4300, Essen, Germany

    Prof. Dr. Otto-Erich Brodde

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Gerd Heusch John Ross Jr.

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Brodde, OE. (1991). β- and α-Adrenoceptor-Agonists and -Antagonists in Chronic Heart Failure. In: Heusch, G., Ross, J. (eds) Adrenergic Mechanisms in Myocardial Ischemia. Steinkopff, Heidelberg. https://doi.org/10.1007/978-3-662-11038-6_5

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  • DOI: https://doi.org/10.1007/978-3-662-11038-6_5

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