Eplerenone(ep ler’ eh nown)
Inspra
PREGNANCY CATEGORY B
Drug Classes
Aldosterone receptor blocker
Antihypertensive
Therapeutic Actions
Binds to aldosterone receptors, blocking the binding of aldosterone, leading to increased loss of sodium and water and lowering of BP.
Indications
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Treatment of hypertension, alone or in combination with other antihypertensive drugs
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HF, post-MI, improvement in the survival of patients with left ventricular dysfunction after a heart attack
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Unlabeled uses: Alone or with ACE inhibitors to reduce left ventricular hypertrophy; adjunct in diabetic hypertensives with microalbuminuria
Contraindications and Cautions
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Contraindicated with allergy to eplerenone, hyperkalemia (exceeding 5.5 mEq/L), concurrent use of potassium supplements or potassium-sparing diuretics, type 2 diabetes with microalbuminuria, severe renal impairment (CrCl less than 50 mL/min or serum creatinine level higher than 2 mg/dL in males or 1.8 mg/dL in females), lactation.
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Use cautiously with hepatic impairment, pregnancy, concurrent treatment with potassium supplements, potassium-sparing diuretics, CYP450 and CYP3A4 inhibitors (eg, ketoconazole).
Available Forms
Tablets—25, 50 mg
Dosages
Adults
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Hypertension: Initially, 50 mg/day PO as a single daily dose; if necessary, may be increased to 50 mg PO bid after a minimum of a 4-wk trial period. Maximum, 100 mg/day.
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Heart failure post-MI: Start with 25 mg/day PO titrate to 50 mg/day over 4 wk.
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Heart failure: If serum K+ is lower than 5, increase dose; if 5–5.4, no adjustment necessary; if 5.5–5.9, decrease dose; if 6 or higher, withhold dose.
Pediatric patients
Safety and efficacy not established.
Pharmacokinetics
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