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The Adrenergic Pharmacology of Carvedilol

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Abstract

Evidence is growing that increased sympathetic drive has major impact on hemodynamic disorders underlying cardiovascular diseases. In particular, mechanisms mediated by adrenoceptors contribute substantially to increased resistance of peripheral vessels, mediated mainly by α-adrenoceptors, leading to hypertension and imbalance of oxygen demand and supply in coronary artery disease (CAD). In addition, sympathetically driven arrhythmogenicity and cardiac remodeling contribute substantially to progression of congestive heart failure (CHF). Consequently, it has been shown in a considerable number of well conducted clinical trials that adrenoceptor antagonists provide benefits for patients suffering from hypertension and CHF. For example, β-adrenoceptor antagonists do not only reduce the blood pressure of hypertensive subjects, but also prevent ischemic heart attacks in patients with CAD, and reduce the risk for suffering from late complications such as stroke or secondary myocardial infarction. In particular, β-adrenoceptor antagonists that are devoid of intrinsic sympathomimetic activities [1] have demonstrated strong cardioprotection. Furthermore, it has been recently shown that the neurohormonal antagonist carvedilol and the β1-adrenoceptor antagonists bisoprolol and metoprolol, are capable of slowing the progression of CHF as indicated by reduction in the rates of hospitalization and mortality [2–4, and metoprolol unpublished data]. The present paper reviews the adrenergic pharmacology of carvedilol established in various in vitro and in vivo experimental paradigms.

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Authors and Affiliations

  1. Roche Diagnostics GmbH, Mannheim

    Gisbert Sponer

  2. DuPont Pharmaceuticals Company, Wilmington, DE

    Giora Z. Feuerstein

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  2. Giora Z. Feuerstein
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Sponer, G., Feuerstein, G.Z. The Adrenergic Pharmacology of Carvedilol. Heart Fail Rev 4, 21–28 (1999). https://doi.org/10.1023/A:1009899516798

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