Abstract
Suppression of the Renin-Angiotensin-Aldosterone system (RAAS) is an established intervention in the management of cardiovascular disease. Large, randomized controlled trials have provided a sound evidence base for the use of mineralocorticoid receptor antagonists to block the end product of the RAAS in the treatment of heart failure. However, the place for mineralocorticoid blockade in the treatment of hypertension is less well defined and lacking a strong evidence base. The main indication for the use of this strategy in hypertension is as a third line agent in the treatment of refractory hypertension. The most widely used mineralocorticoid receptor antagonist, spironolactone, is associated with dose related sexual side effects, limiting its use in clinical practice. Eplerenone, the selective mineralocorticoid receptor antagonist, is a promising cardiovascular drug licensed for the treatment of heart failure in Europe and heart failure and hypertension in the USA. It effectively blocks the mineralocorticoid receptor without the unpleasant sexual side effect profile of spironolactone. We review the use of eplerenone, a selective mineralocorticoid receptor antagonist in the treatment of hypertension; discuss its mechanism of action, safety profile as well as its current place in therapy.
Highlights
The first mineralocorticoid receptor (MR) antagonist spironolactone was patented almost 50 years ago but more recently has re-emerged as a potent tool in the armoury of cardiovascular drugs
It should be born in mind that eplerenone remains unlicensed for the treatment of hypertension in Europe
While there is a large body of preclinical data to suggest that eplerenone and spironolactone may confer end organ protection over and above blood pressure control, clinical evidence to support the use of MR blockade in routine treatment of hypertension remains lacking
Summary
The first mineralocorticoid receptor (MR) antagonist spironolactone was patented almost 50 years ago but more recently has re-emerged as a potent tool in the armoury of cardiovascular drugs. There is good evidence that the addition of spironolactone will produce better blood pressure control for the treatment of resistant hypertension In those individuals where the development of sexual side effects results in an inability to tolerate spironolactone, altering the regime to eplerenone is reasonable it should be borne in mind that the dose required is likely to be higher and twice daily dosing may be necessary. While there is a large body of preclinical data to suggest that eplerenone and spironolactone may confer end organ protection over and above blood pressure control, clinical evidence to support the use of MR blockade in routine treatment of hypertension remains lacking. There is a large amount of uncertainty regarding the differences in action of spironolactone and eplerenone and further comparisons both at preclinical and clinical trial level are required
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