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Aldosterone Antagonists
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eplerenone (Inspra ®)
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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 Aldosterone increases blood pressure primarily by inducing sodium reabsorption. Eplerenone reduces blood pressure by blocking aldosterone binding at mineralocorticoid receptors found in the kidney, heart, blood vessels and brain. Dosing (adults) Oral: Hypertension: Initial: 50 mg once daily; may increase to 50 mg twice daily if response is not adequate; may take up to 4 weeks for full therapeutic response. Doses >100 mg/day are associated with increased risk of hyperkalemia and no greater therapeutic effect. 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 mEq/L: Increase dose from 25 mg every other day to 25 mg daily or Increase dose from 25 mg daily to 50 mg daily 5.0-5.4 mEq/L: No adjustment needed 5.5-5.9 mEq/L: Decrease dose from 50 mg daily to 25 mg daily or Decrease dose from 25 mg daily to 25 mg every other day or Decrease does from 25 mg every other day to withhold medication >/= 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 hypertension with Clcr<50 mL/minute or serum creatinine >2.0 mg/dL in males or >1.8 mg/dL in females: Use is contraindicated; risk of hyperkalemia increases with declining renal function Patients with CHF post-MI: Use with caution Supplied Tablet [film coated]: 25 mg, 50 mg |
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spironolactone (Aldactone ®):
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Class: Potassium sparing Management of edema associated with excessive aldosterone excretion; hypertension; primary hyperaldosteronism; hypokalemia; treatment of hirsutism; cirrhosis of liver accompanied by edema or ascites Mechanism of Action Competes with aldosterone for receptor sites in the distal renal tubules, increasing sodium chloride and water excretion while conserving potassium and hydrogen ions; may block the effect of aldosterone on arteriolar smooth muscle as well Adults: Oral: To reduce delay in onset of effect, a loading dose of 2 or 3 times the daily dose may be administered on the first day of therapy. 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 Acne in women (unlabeled use): 25 to 200 mg once daily Hirsutism in women (unlabeled use): 50 to 200 mg/day in 1-2 divided doses CHF, severe (with ACE inhibitor and a loop diuretic ± digoxin): 25 mg/day, increased or reduced depending on individual response and evidence of hyperkalemia 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: Clcr 10-50 mL/minute: Administer every 12-24 hours. Clcr<10 mL/minute: Avoid use. Supplied Tablet: 25 mg, 50 mg, 100 mg |
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