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Prescribing Information
INSPRA® (eplerenone)
Overdosage
Return to the INSPRA Product Center

No cases of human overdosage with eplerenone have been reported. Lethality was not observed in mice, rats, or dogs after single oral doses that provided Cmax exposures at least 25 times higher than in humans receiving eplerenone 100 mg/day. Dogs showed emesis, salivation, and tremors at a Cmax 41 times the human therapeutic Cmax, progressing to sedation and convulsions at higher exposures.

The most likely manifestation of human overdosage would be anticipated to be hypotension or hyperkalemia. Eplerenone cannot be removed by hemodialysis. Eplerenone has been shown to bind extensively to charcoal. If symptomatic hypotension should occur, supportive treatment should be instituted. If hyperkalemia develops, standard treatment should be initiated.


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)

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