INSPRA® (eplerenone) tablets Description

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Prescribing Information

INSPRA^® (eplerenone) tablets
Description


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INSPRA contains eplerenone, a blocker of aldosterone binding at the mineralocorticoid receptor.

Eplerenone is chemically described as Pregn-4-ene-7,21-dicarboxylic acid, 9,11-epoxy-17-hydroxy-3-oxo-,γ-lactone, methyl ester, (7α,11α,17α)-. Its empirical formula is C₂₄H₃₀O₆ and it has a molecular weight of 414.50. The structural formula of eplerenone is represented below:

Eplerenone is an odorless, white to off-white crystalline powder. It is very slightly soluble in water, with its solubility essentially pH independent. The octanol/water partition coefficient of eplerenone is approximately 7.1 at pH 7.0.

INSPRA for oral administration contains 25 mg or 50 mg of eplerenone and the following inactive ingredients: lactose, microcrystalline cellulose, croscarmellose sodium, hypromellose, sodium lauryl sulfate, talc, magnesium stearate, titanium dioxide, polyethylene glycol, polysorbate 80, and iron oxide yellow and iron oxide red.

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INSPRA Safety Information

Important Safety Information

INSPRA is indicated to improve survival of stable patients with left ventricular systolic dysfunction (ejection fraction ≤40%) and clinical evidence of congestive heart failure after an acute myocardial infarction.

INSPRA is contraindicated in all patients with the following: serum potassium >5.5 mEq/L at initiation; creatinine clearance ≤30 mL/min; concomitant use with the following potent CYP3A4 inhibitors: ketoconazole, itraconazole, nefazodone, troleandomycin, clarithromycin, ritonavir, nelfinavir, or other drugs described in their labeling as strong inhibitors of CYP3A4.

The principal risk of INSPRA is hyperkalemia. Hyperkalemia can cause serious, sometimes fatal, arrhythmias. Hyperkalemia can be minimized by patient selection, avoidance of certain concomitant treatments, and periodic monitoring until the effect of INSPRA has been established. Patients who develop hyperkalemia (>5.5 mEq/L) may still benefit from INSPRA with proper dose adjustment.

Patients with congestive heart failure post-acute MI receiving INSPRA who have renal insufficiency (serum creatinine levels >2 mg/dL [males] or >1.8 mg/dL [females]; creatinine clearance ≤50 mL/min) or patients with diabetes, including those with proteinuria, should be treated with caution, due to the increased risk of hyperkalemia.

Adverse events reported more frequently in patients treated with INSPRA than placebo were hyperkalemia (3.4% vs 2.0%) and increased creatinine (2.4% vs 1.5%). Laboratory measurements of serum potassium >5.5 mEq/L occurred in 15.6% of patients receiving INSPRA vs 11.2% of patients receiving placebo. Laboratory measurements of serum potassium ≥ 6.0 mEq/L occurred in 5.5% of patients receiving INSPRA vs 3.9% of patients receiving placebo. Discontinuations due to hyperkalemia or abnormal renal function were less than 1.0% in both groups. Hypokalemia occurred less frequently in patients treated with INSPRA (0.6% vs 1.6%).

Please see full prescribing information.

INSPRA^® (eplerenone tablets)

inspra_safety_information.htm

Full Prescribing Information