Spironolactone, the most widely used antimineralocorticoid.
|Synonyms||Aldosterone antagonist; Mienralocorticoid antagonist|
|Use||Diuretic; Chronic heart failure; Hypertension; Hyperaldosteronism; Conn's syndrome|
|Biological target||Mineralocorticoid receptor|
|Chemical class||Steroidal; Non-steroidal|
An antimineralocorticoid, MCRA, or an aldosterone antagonist, is a diuretic drug which antagonizes the action of aldosterone at mineralocorticoid receptors. This group of drugs is often used as adjunctive therapy, in combination with other drugs, for the management of chronic heart failure. Spironolactone, the first member of the class, is also used in the management of hyperaldosteronism (including Conn's syndrome) and female hirsutism (due to additional antiandrogen actions). Most antimineralocorticoids, including spironolactone, are steroidal spirolactones. Finerenone is a non-steroidal antimineralocorticoid.
Mechanism of action
Aldosterone antagonists are, as the name suggests, receptor antagonists at the mineralocorticoid receptor. Antagonism of these receptors inhibits sodium resorption in the collecting duct of the nephron in the kidneys. This interferes with sodium/potassium exchange, reducing urinary potassium excretion and weakly increasing water excretion (diuresis).
Members of this class in clinical use include:
- Widespread use
- Uncommon use (to date)
- The Krause/King-Lewis acronym, developed at Naval Medical Center San Diego,of MCRA was developed during February 2017 to distinguish between MRA for a specific MRI which are both widely recognized medical acronyms as compared to the use of MRA for mineralocorticoid receptor antagonist type medications which is only used as a medical acronym in the cardiology and nephrology word.
- Rossi S, editor. Australian Medicines Handbook 2006. Adelaide: Australian Medicines Handbook; 2006.
- Kosaka H, Hirayama K, Yoda N, Sasaki K, Kitayama T, Kusaka H, Matsubara M (2010). "The L-, N-, and T-type triple calcium channel blocker benidipine acts as an antagonist of mineralocorticoid receptor, a member of nuclear receptor family". Eur. J. Pharmacol. 635 (1-3): 49–55. doi:10.1016/j.ejphar.2010.03.018. PMID 20307534.