Mineralocorticoid receptor antagonist

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).

[2] By regulating water excretion, mineralocorticoid receptor antagonists lower blood pressure and reduce fluid around the heart which can be very beneficial in some cardiovascular conditions.

Common side effects for antimineralocorticoid medications include nausea and vomiting, stomach cramps and diarrhoea.

[5] When aldosterone is secreted from the adrenal glands, it binds to the mineralocorticoid receptor in the renal tubule cell and forms a complex.

[6] These protein transporters increase sodium reabsorption and potassium excretion in the distal tubule and the collecting duct of the kidneys.

This leads to higher levels of potassium in serum and increased sodium excretion, resulting in decreased body fluid and lower blood pressure.

It is very important to adjust the doses for patients with renal dysfunction because if they fail to eliminate the drug through their kidneys it could accumulate in the body, causing high concentration of potassium in the blood.

[5] Spironolactone and Eplerenone competitively block the binding of aldosterone to the mineralocorticoid receptor and hindering the reabsorption of sodium and chloride ions.

[7] Despite the nonsteroidal nature of finerenone which yields a different lipophilicity and polarity profile for this compound, finerenone's affinity toward mineralocorticoid receptors is equal to that of spironolactone and 500 times that of eplerenone, hinting that the steroidal core component of most antimineralocorticoids is not essential for mineralocorticoid receptor affinity.

Their goal was to discover novel non-steroidal mineralocorticoid receptor antagonists for use as efficacious and safe drugs with the pharmacodynamics and pharmacokinetics well defined.

[8] Members of this class in clinical use include: Some drugs also have antimineralocorticoid effects secondary to their main mechanism of actions.

Antimineralocorticoid mechanism of action
Antimineralocorticoids and highlighted groups that are important for activity. The y-lactone ring shown in red and the C-7 substituent in pink.
Skeletal formulae of aldosterone antagonists.