Antimineralocorticoid

Skeletal formulae of the aldosterone antagonists

An antimineralocorticoid, 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). ^[1]

In congestive heart failure, they are used in addition to other drugs for additive diuretic effect, which reduces edema and the cardiac workload.

Examples

Members of this class in clinical use include:

• Spironolactone – the first and most widely used member of this class
• Eplerenone – much more selective than spironolactone on target, but somewhat less potent and efficacious
• Canrenone and potassium canrenoate – very limited use
• Finerenone – non-steroidal and more potent and selective than either eplerenone or spironolactone

Some drugs also have antimineralocorticoid effects secondary to their main mechanism of actions. Examples include progesterone, drospirenone, gestodene, and benidipine.^[2]

See also

• Potassium-sparing diuretic
• Mineralocorticoid
• Corticosteroid
• Antiglucocorticoid

References

1. Rossi S, editor. Australian Medicines Handbook 2006. Adelaide: Australian Medicines Handbook; 2006.
2. 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.

External links

• Aldosterone Antagonists at the US National Library of Medicine Medical Subject Headings (MeSH)
• MeSH list of agents 82000451