Eplerenone: The first selective aldosterone receptor antagonist for the treatment of hypertension (PDF)


Eplerenone is a selective aldosterone receptor antagonist under FDA review for treatment of hypertension. With a high trough-to-peak ratio, it is suitable for once-daily dosing. It significantly reduces blood pressure in patients with mild to severe hypertension and can be used alone or in combination with other antihypertensives. Although chemically related to spironolactone, eplerenone has a lower binding affinity for androgenic and progestogenic receptors than spironolactone, which may translate into a lower incidence of endocrine-related adverse effects. In addition, eplerenone lowers blood pressure particularly well in patients with low-renin, salt-sensitive hypertension, such as African Americans.

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