Aldosterone Receptor Blockers

Aldosterone Receptor Blockers work by inhibiting a hormone called aldosterone and produce a diuretic (increase in the amount of urine passed) effect. Aldosterone is a hormone that results in more sodium staying in the body and causes fluid retention. Spironolactone and eplerenone work in heart failure by blocking the effects of aldosterone by helping to remove excess sodium from the body and helping remodel the ventricle's size, shape, and function. (The heart contains two ventricles, which are also known as chambers in the heart that pump blood out into the body.)

Drugs in this Class
Spironolactone Tablets (Aldactone Tablets)

Summarizing the Evidence

  • Spironolactone has been shown in clinical studies to not only reduce death, but reduce death from further progression of heart failure and from sudden death related to other heart related problems in patients with moderate to severe heart failure. In these studies, spironolactone also improved heart failure symptoms. Spironolactone was also well tolerated by patients in these studies.

  • Spironolactone has been shown in clinical studies to reduce the amount of magnesium that is present in the heart muscle, which can lead to a reduction in magnesium-induced arrhythmias (irregular beating of the heart). These arrhythmias can result in death in some patients.

  • Eplerenone has been shown in clinical studies to reduce the risk and number of hospitalizations for those patients with severe heart failure. These studies have also shown a reduction in sudden death from heart-related events, heart attacks, and heart failure.

  • In some patients, spironolactone has been shown to have some sexual side effects (such as men developing larger than normal mammary glands) and eplerenone has been found to be free of causing these types of side effects.

  • To date, studies that directly compare spironolactone to eplerenone for the treatment of heart failure are lacking. Spironolactone is generally used more often than eplerenone due to the fact that spironolactone has been available for a longer period of time, it has substantial evidence to prove its effectiveness and safety, and it is available generically.

  • Because of its effectiveness and safety in addition to its low cost, spironolactone should be considered for all patients who have symptomatic heart failure and is strongly recommended for patients with moderate to severe heart failure.

Dosing and Administration

  • For heart failure, spironolactone is typically dosed as 25mg once daily. Eplerenone is typically dosed as 50 mg once daily for the treatment of heart failure.ul>

    Generic Availability

    • Spironolactone is available generically and thus is relatively inexpensive. Currently eplerenone is not available generically.

    Drug Interactions

    Some interactions between medications can be more severe than others. The best way for you to avoid harmful interactions is to tell your doctor and/or pharmacist what medications you are currently taking, including any over-the-counter products, vitamins, and herbals. For specific information on how the drugs interact and the severity of the interaction, please use our Drug Interactions Checker.

    Side Effects

    To view specific side effect information, please use our Side Effect Checker.

    Additional Information

    References

    1. Johnson JA, Parker RB, Patterson JH. Heart Failure. In: DiPiro JT, Talbert RL, Yee GC, et al., (Eds). Pharmacotherapy: a pathophysiologic approach. 6th ed. New York: McGraw-Hill, 2005:219-260.
    2. Pitt B, Zannad F, Remme WJ, et al. The effect of spironolactone on morbidity and mortality in patients with severe heart failure. Randomized aldactone evaluation study investigators. N Engl J Med 1999; 341:709-17.
    3. Hunt SA, Baker DW, Chin MH, et al. ACC/AHA Guideline Update for the Diagnosis and Management of Chronic Heart Failure in the Adult- Summary Article. Circulation. 2005: 112(12); 1677-1916.
    4. Adams KF Jr., Lindenfeld J, et al. Executive Summary: HFSA 2006 Comprehensive Heart Failure Practice Guidelines. Journal of Cardiac Failure. 2006:12(1); 10-38.
    5. Gao X, Peng L, et al. Spironolactone reduced arrhythmia and maintained magnesium homeostasis in patients with congestive heart failure. Journal of Cardiac Failure. 2007 April;13(3): 170-177.
    6. Weber KT. Aldosterone and Spironolactone in Heart Failure. New England Journal of Medicine. 1999; 341:752-755
    7. Pitt B, Remme W, Zannad F, et al. Eplerenone, a Selective Aldosterone Blocker, in Patients with Left Ventricular Dysfunction after Myocardial Infarction. The New England Journal of Medicine. 2003 April; 348(14):1309-1321.
    8. Pitt B, Williams G, Remme W, et al. The EPHESUS trial: eplerenone in patients wth heart failure due to systolic dysfunction complicating acute myocardial infarction: Eplerenone Post-AMI Heart Failure Efficacy and Survival Study. Cardiovascular Drugs Therapy. 2001;159:79-87.
    9. Spironolactone. Drug Facts and Comparisons. St. Louis, MO. Last updated: August 2007.
    10. Eplerenone. Drug Facts and Comparisons. St. Louis, MO. Last updated: August 2007.

    Last Updated: June 2008

    Note: The above information is intended to supplement, not substitute for, the expertise and judgment of your physician, pharmacist, or other healthcare professional. It should not be construed to indicate that the use of the product is safe, appropriate, or effective for you. Consult your healthcare professional before taking any medication.

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