Class: Selective aldosterone receptor antagonists
- Tablets 25 mg
- Tablets 50 mg
Binds to mineralocorticoid receptor, blocking the binding of aldosterone.
T max is 1.5 h.
Approximately 50% is protein bound (primarily to alpha 1-acid glycoprotein). The Vd is 43 to 90 L (at steady state).
Metabolized by CYP3A4; no active metabolites formed.
The elimination t ½ is approximately 4 to 6 h. Approximately 32% is excreted in feces and approximately 67% is excreted in urine. Less than 5% is excreted as unchanged drug. The plasma Cl is approximately 10 L/h.
Special PopulationsRenal Function Impairment
AUC and C max increased 38% and 24%, respectively, in those with severe renal function impairment.Hepatic Function Impairment
C max and AUC increased 3.6% and 42%, respectively, in those with moderate hepatic function impairment.Elderly
C max increased 22% and AUC increased 45%.Race
C max decreased 19% and AUC decreased 26% in black patients.
Indications and Usage
Treatment of hypertension; improve survival of stable patients with left ventricular systolic dysfunction and clinical evidence of CHF after an acute MI.
Patients with serum potassium greater than 5.5 mEq/L, type 2 diabetes with microalbuminuria, serum creatinine greater than 2 mg/dL in men or greater than 1.8 mg/dL in women, Ccr 30 mL/min or less, patients treated concurrently with potassium supplements, potassium-sparing diuretics (eg, spironolactone), or strong inhibitors of CYP3A4 (eg, ketoconazole).
Dosage and AdministrationCHF Post-MI
PO Start with 25 mg every day and titrate to target dose of 50 mg every day within 4 wk as tolerated by the patient.Dosage Adjustment in CHF
PO If serum potassium is less than 5 mEq/L, increase dose from 25 mg every day to 50 mg every day; if potassium levels are between 5 and 5.4 mEq/L, maintain dose; if potassium levels are between 5.5 and 5.9 mEq/L, decrease dose from 50 mg every day to 25 mg every day, or 25 mg every day to 25 mg every other day, or 25 mg every other day to withhold; if potassium levels are 6 mEq/L or greater, withhold the dose. When potassium levels have fallen below 5.5 mEq/L, restart dose at 25 mg every other day.Hypertension
PO Initial dose 50 mg every day. The full therapeutic effect is seen within 4 wk. Patients with an inadequate BP response to 50 mg every day may be increased to 50 mg bid (max, 100 mg/day). Patients receiving weak CYP3A4 inhibitors (eg, saquinavir) start with 25 mg every day.
Administer with or without food. Administer with food if GI upset occurs.
Store tablets at controlled room temperature (59° to 86°F).
Drug InteractionsACE inhibitors and angiotensin II receptor antagonists
May increase the risk of hyperkalemia.CYP3A4 inhibitors (eg, clarithromycin, nefazodone, ritonavir)
Elevated plasma levels of eplerenone, increasing the risk of side effects.St. John's wort
Reduced plasma levels of eplerenone, decreasing the therapeutic effect.
Angina pectoris; MI.
Headache; dizziness; fatigue.
Diarrhea; abdominal pain.
Albuminuria; abnormal vaginal bleeding; mastodynia, gynecomastia (men).
Hyponatremia; hypercholesterolemia; hypertriglyceridemia; increased BUN; increased uric acid; increase serum creatinine; increased ALT; hyperkalemia.
Category B .
Safety and efficacy not established.
Hyperkalemia may occur. Risk can be minimized by patient selection, avoidance of certain drugs, and monitoring. Ensure that serum potassium is determined before starting therapy, within the first week, and at 1 mo after the start of therapy or dose adjustment. Periodically assess serum potassium thereafter.
- Advise patient to take every day as prescribed, without regard to meals. Advise patient to take with food if GI upset occurs.
- Advise patient to try to take each dose at about the same time each day.
- Inform patient that drug controls but does not cure hypertension and to continue taking it as prescribed even when BP is not elevated.
- Caution patient not to change the dose or stop taking unless advised by health care provider.
- Instruct patient to continue taking other BP medications as prescribed by health care provider.
- Instruct patient in BP and pulse measurement skills.
- Advise patient to monitor and record BP and pulse at home and to inform health care provider should abnormal measurements be noted. Also advise patient to take record of BP and pulse to each follow-up visit.
- Instruct patient to lie or sit down if experiencing dizziness or lightheadedness when standing.
- Emphasize to hypertensive patient importance of the following other modalities on BP: weight control, regular exercise, smoking cessation, moderate intake of alcohol and salt.
- Caution patient not to take any prescription or OTC medications, salt substitutes, potassium supplements, or dietary supplements unless advised by health care provider.
Copyright © 2009 Wolters Kluwer Health.
More about eplerenone
- Other brands: Inspra