Aldosterone Antagonists in the Treatment of Heart Failure

Place in Therapy

In the absence of contraindications, an aldosterone antagonist should be offered to patients with NYHA class III or IV heart failure and to patients after an MI with left ventricular dysfunction. Further studies are needed to confirm the benefit to patients with NYHA class I or II heart failure.

Careful monitoring is critical to prevent potentially life-threatening hyperkalemia. Patients with renal disease, diabetes mellitus, advanced heart failure, or advanced age and those taking certain concurrent medications have the highest risk of developing hyperkalemia. Increased vigilance in monitoring for and patient education regarding hyperkalemic symptoms is necessary in these patients. If baseline CL_cr is less than 30 mL/min or baseline serum potassium concentration is greater than 5.5 mmol/L, aldosterone antagonist therapy should be withheld. Recent updates to heart failure guidelines suggest withholding aldosterone antagonist therapy in patients with a baseline serum potassium concentration exceeding 5.0 mmol/L.^[1]

Pharmacoeconomic evaluations have found spironolactone and eplerenone to be cost-effective when compared with placebo in the populations studied in the major aldosterone antagonist trials.^[90,91] However, no published cost-effectiveness studies have compared spironolactone and eplerenone.

Spironolactone is a life-saving agent in patients with severe heart failure. Eplerenone has been found to be a life-saving agent in patients with left ventricular dysfunction 3–14 days after an MI. No studies have been conducted to establish eplerenone's effects on morbidity and mortality in severe heart failure without a recent MI. Similarly, the effects of spironolactone have not been studied in patients immediately after an MI. Eplerenone appears to have fewer adverse effects than does spironolactone. As such, it is reasonable to substitute eplerenone for spironolactone in patients who develop gynecomastia or adverse sexual effects.

Cite this: Aldosterone Antagonists in the Treatment of Heart Failure - Medscape - Jan 01, 2006.

Comparison of Spironolactone and Eplerenone
Variable^a	Spironolactone	Eplerenone
Pharmacology	Nonselective competitive aldosterone antagonist	Selective competitive aldosterone antagonist
Has active metabolites?	Yes	No
Half-life	1.4 hr^b	4–6 hr
Oral bioavailability	>90%	67%
Highly protein bound (>90%)	Yes	No
Metabolized by CYP isoenzyme system	No	Yes
Associated with gynecomastia?	Yes	No
Associated with adverse sexual effects?	Yes	No
Associated with adverse GI effects?	No	Yes
Cost for 30-day supply	Approximately $0.35/day (generic)^c	Approximately $3.75/day^c
Population showing benefit	Chronic, severe, systolic heart failure	Left ventricular systolic dysfunction immediately after MI

^aCYP = cytochrome P-450, GI = gastrointestinal, MI = myocardial infarction.
^bHalf-life of active metabolites is 14–22 hours.
^cAverage retail price based on prices obtained from two retail pharmacies.

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Aldosterone Antagonists in the Treatment of Heart Failure

Place in Therapy

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