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Endothelin receptor antagonists as antihypertensives: the next frontier
Benjamin J Epstein1, Shawn Anderson
1Department of Pharmacotherapy and Translational Research, 101 S. Newell Drive, HPNP Building. 212, Room 3315, University of Florida, Gainesville, FL 32610-0486, USA. epstein@cop.ufl.edu.
Insights
Endothelin receptor antagonists (ERAs) show significant blood pressure lowering effects, particularly for resistant hypertension. These drugs also offer cardiovascular protection beyond blood pressure control.
Area of Science:
- Cardiovascular Medicine
- Pharmacology
Background:
- The endothelin system plays a critical role in cardiovascular disease.
- It contributes to blood pressure regulation and end-organ damage.
Purpose of the Study:
- To review the evolving role of endothelin receptor antagonists (ERAs) in hypertension treatment.
- To highlight the potential benefits of ERAs beyond blood pressure reduction.
Main Methods:
- Review of recent studies on ERAs in hypertension.
- Analysis of pharmacological properties and clinical trial data.
Main Results:
- ERAs demonstrate a potent antihypertensive effect, especially in resistant hypertension.
- ERAs offer protective effects on endothelial function, atherosclerosis, arterial stiffness, renal function, and proteinuria.
Conclusions:
- ERAs represent a promising therapeutic class for hypertension and cardiovascular disease.
- Further research is ongoing to fully elucidate the potential of ERAs in various cardiovascular conditions.
Abstract:
The endothelin system is a pivotal player along the continuum of cardiovascular disease. There is convincing evidence that the system not only exerts a potent pressor effect but also promotes end-organ damage independent from blood pressure changes. The role of endothelin receptor antagonists (ERAs) in the treatment of hypertension is rapidly evolving. Recent studies demonstrate a formidable antihypertensive effect. Utility of ERAs is likely to be greatest in patients with resistant hypertension. Beyond blood pressure lowering, ERAs exert several properties that may confer additional protection, including effects on endothelial function, atherosclerosis, arterial stiffening, renal function and proteinuria. The full potential of this class will only be realized when the results of ongoing and future studies in hypertension, heart failure and other forms of cardiovascular disease are completed.
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