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Binds to mineralocorticoid receptors, thereby blocking the binding of aldosterone, a component of the renin-angiotensin-aldosterone system (RAAS). Aldosterone synthesis occurs primarily in the adrenal gland and is regulated by multiple factors, including angiotensin II and non-RAAS mediators such as adrenocorticotropic hormone (ACTH) and potassium. Aldosterone binds to mineralocorticoid receptors in epithelial tissues (such as the kidneys) and non-epithelial tissues (such as the heart, blood vessels, and brain) and increases blood pressure by inducing sodium reabsorption and possibly other mechanisms.

Eplerenone is a new, highly selective aldosterone receptor blocker that can be used for the treatment of heart failure, hypertension, and coronary heart disease. Eplerenone can be used alone or in combination with other antihypertensive drugs to treat hypertension. The recommended dose for adults is the initial dose: 50 mg orally once daily. Maintenance dose: 50 mg orally, 1-2 times daily. Maximum dose: 100 mg/day. Obvious antihypertensive effects appear within four weeks of taking the drug. Patients whose blood pressure responds inadequately to the initial dose may be increased to 50 mg twice daily. Initial adult dose for the treatment of congestive heart failure: 25 mg orally once daily; gradually increase to target dose over 4 weeks as tolerated by the patient. Target dose: 50 mg orally, once daily.

In patients with low-renin hypertension, the antihypertensive effect is better than that of losartan. For patients with hypertension who are poorly controlled by ARB alone, adding eplerenone (50~100 mg·d) for 8 weeks can further enhance the effect of reducing systolic blood pressure (SBP) and diastolic blood pressure (DBP). For elderly patients with hypertension who are poorly controlled by ACEI or ARB, the addition of low-dose (25-50 mg/d, average 37.5 mg) eplerenone can effectively reduce the average 24-hour systolic blood pressure (SBP) and diastolic blood pressure (DBP).