Aldosterone Receptor Antagonist
Aldosterone receptor antagonists are a type of diuretic used in patients with CHF. They have a high affinity for the aldosterone receptor in the kidneys[1]. Blocking the aldosterone receptor prevents an increase in aldosterone, ultimately preventing changes to the cardiovascular system and allowing for increased water excretion. Aldosterone receptor antagonists also prevent secretion of potassium into distal tubule of the nephron[2]. Two common aldosterone receptor antagonists are spironolactone and eplerenone[3]. Spironolactone is taken orally with doses of 12.5-25 mg per day and has a long half-life of 13-17 hours[4]. Eplerenone is also taken orally with doses of 50 mg twice daily with a half-life of 4 hours[5] and both are excreted by via the liver and kidneys[6].
Due to the prevention of potassium secretion into the distal tubule both these drugs are associated with an adverse effect of hyperkalemia due to them being potassium sparing diuretics. In addition, spironolactone is associated with breast pain in men and gynecomastia because it tends to bind to progesterone and androgen receptors[3]. Most aldosterone receptor antagonists are used in conjunction with other medications, specifically Beta Blockers and Ace Inhibitors. This drug, while acting to relieve the body of excessive fluids, can inadvertently disrupt the electrolyte and pH balance in the system. Because the main side effect is hyperkalemia, is it important to check for any irregular heartbeats if the patient begins complaining of chest pains or shortness of breath[7]. In addition to monitoring the patient’s vitals before, during and after treatment, patients should be educated on lifestyle changes to help decrease their mortality.
- ↑ Seawell MR, Al Darazi F, Farah V, Ramanathan KB, Newman KP, Bhattacharya SK, Weber KT. Mineralocorticoid receptor antagonism confers cardioprotection in heart failure. [Review]. Current Heart Failure Reports. 2013;10(1):36-45.
- ↑ Nagarajan V, Chamsi-Pasha M, Tang WH. The role of aldosterone receptor antagonists in the management of heart failure: an update. [Review]. Cleveland Clinic Journal of Medicine. 2012;79(9):631-9.
- ↑ 3.0 3.1 Lainscak M, Pelliccia F, Rosano G, Vitale C, Schiariti M, Greco C, Speziale G, Gaudio C (2015). Safety profile of mineralocorticoid receptor antagonists: Spironolactone and eplerenone. Int J Cardiol. 200, 25-9
- ↑ U.S. Food and Drug Administration (FDA). Aldactone spironolactone tablets, USP. Available online at: https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/012151s062lbl.pdf. Last accessed 11/29/18.
- ↑ U.S. Food and Drug Administration (FDA). INSPRA eplerenone tablets. Available online at: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/21437lbl.pdf. Last accessed 11/29/18.
- ↑ Nappi JM, Sieg A (2011). Aldosterone and aldosterone receptor antagonists in patients with chronic heart failure. Vasc Health Risk Manag. 7, 353-63.
- ↑ Sica DA. Diuretic-related side effects: development and treatment. J Clin Hypertens. 2004;6:532–540.
