Kalpana Kalpana

Antimineralocorticoid

Updated on
Share on FacebookTweet on TwitterShare on LinkedIn
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.

Contents

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).

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:

  • Widespread use
  • 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
  • Uncommon use (to date)
  • 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.

    References

    Antimineralocorticoid Wikipedia


    Similar Topics
    The Hollywood Revue of 1929
    Eleanor Campbell (scientist)
    Sámuel Mészáros
    Topics