| Class: Potassium sparing
Treatment of hypertension (may be used alone or in combination with other antihypertensive agents); treatment of CHF following acute MI
Mechanism of Action
Eplerenone has been shown to produce sustained increases in plasma renin and serum aldosterone, consistent with inhibition of the negative regulatory feedback of aldosterone on renin secretion. The resulting increased plasma renin activity and aldosterone circulating levels do not overcome the effects of eplerenone.
Eplerenone selectively binds to recombinant human mineralocorticoid receptors relative to its binding to recombinant human glucocorticoid, progesterone and androgen receptors.
Concurrent use with moderate CYP3A4 inhibitors: Initial: 25 mg once daily
Congestive heart failure (post-MI): Initial: 25 mg once daily; dosage goal: titrate to 50 mg once daily within 4 weeks, as tolerated
Dosage adjustment per serum potassium concentrations for CHF:
5.0-5.4 mEq/L: No adjustment needed
>/= 6.0 mEq/L: Withhold medication until potassium <5.5 mEq/L, then restart at 25 mg every other day
Dosage adjustment in renal impairment:
Patients with CHF post-MI: Use with caution
| Class: Potassium sparing
Mechanisms of Action
Aldosterone antagonist activity
Spironolactone is effective in lowering the systolic and diastolic blood pressure in patients with primary hyperaldosteronism. It is also effective in most cases of essential hypertension, despite the fact that aldosterone secretion may be within normal limits in benign essential hypertension.
Through its action in antagonizing the effect of aldosterone, spironolactone inhibits the exchange of sodium for potassium in the distal renal tubule and helps to prevent potassium loss.
Spironolactone has not been demonstrated to elevate serum uric acid, to precipitate gout, or to alter carbohydrate metabolism.
Edema, hypokalemia: 25-200 mg/day in 1-2 divided doses
Hypertension (JNC 7): 25-50 mg/day in 1-2 divided doses
Diagnosis of primary aldosteronism: 100 to 400 mg/day in 1-2 divided doses
Elderly: Initial: 25 to 50 mg/day in 1-2 divided doses, increasing by 25-50 mg every 5 days as needed.
Dosing interval in renal impairment:
National Institutes of Health, U.S. National Library of Medicine, DailyMed Database.
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