Eplerenone ( Inspra ) is a steroid nucleus-based mineralcorticoid receptor antagonist with a higher degree of selectivity than Spironolactone. Eplerenone is thought to be a more selective blocker at the mineralcorticoid receptor since there is evidence that some of the effects result from a blockade of cortisol stimulation of the mineralcorticoid receptor.

In the United States, Inspra is indicated to improve survival of stable patients with left ventricular systolic dysfunction ( ejection fraction less than or equal to 40% ) and clinical evidence of congestive heart failure ( CHF ) after an acute myocardial infarction.
Eplerenone is also indicated for the treatment of hypertension. Eplerenone may be used alone or in combination with other antihypertensive agents.

Eplerenone is contraindicated in all patients with serum potassium greater than 5.5 mEq/L at initiation, creatinine clearance less than or equal to 30 mL/min, or concomitant administration of strong CYP3A4 inhibitors.
Eplerenone is also contraindicated for the treatment of hypertension in patients with type 2 diabetes with microalbuminuria, serum creatinine greater than 2.0 mg/dL in males or greater than 1.8 mg/dL in females, creatinine clearance less than 50 mL/min, or concomitant administration of potassium supplements or potassium sparing diuretics.

Serum potassium should be measured before initiating eplerenone therapy, within the first week, and at one month after the start of treatment or dose adjustment. Serum potassium should be assessed periodically thereafter, especially in patients at risk for the development of hyperkalemia such as elderly patients with renal insufficiency and patients with type 2 diabetes and microalbuminuria.

Most common adverse reactions ( greater than 2% and more frequent than with placebo ) in patients with CHF post-myocardial infarction: hyperkalemia and increased creatinine. Most common adverse reactions ( greater than or equal to 2% and more frequent than with placebo ) in hypertensive patients: dizziness, diarrhea, coughing, fatigue and flu-like symptoms.

In the European Union ( EU ), Eplerenone is indicated to reduce the risk of cardiovascular mortality and morbidity in stable patients with left ventricular dysfunction ( LVEF less than or equal to 40% ) and clinical evidence of heart failure after recent myocardial infarction.

Source: Pfizer, 2011

XagenaMedicine2011