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
Treatment of hypertension, alone or in combination with other antihypertensive drugs
HF, post-MI, improvement in the survival of patients with left ventricular dysfunction after a heart attack
Unlabeled uses: Alone or with ACE inhibitors to reduce left ventricular hypertrophy; adjunct in diabetic hypertensives with microalbuminuria
Contraindications and Cautions
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.
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
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.
Heart failure post-MI: Start with 25 mg/day PO titrate to 50 mg/day over 4 wk.
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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