Mineralocorticoid Receptor Antagonists

Drugs that bind to and block the activation of MINERALOCORTICOID RECEPTORS by MINERALOCORTICOIDS such as ALDOSTERONE.
DrugDrug NameDrug Indication
DB00421SpironolactoneSpironolactone is indicated for the treatment of New York Heart Association Class III-IV heart failure, management of edema in cirrhotic adults not responsive to fluid and sodium restrictions, primary hyperaldosteronism short-term preoperatively, primary hyperaldosteronism long-term in patients with aldosterone producing adrenal adenomas that are not candidates for surgery or patients with bilarteral micro/macronodular adrenal hyperplasia, as an add-on therapy in hypertension, and in nephrotic syndrome when treatment of the disease as well as fluid and sodium restriction with other diuretics is inadequate.[Label] Spironolactone has antiandrogenic activity which leads to many of its off label uses. Spironolactone is used off label in the treatment of hirsutism, female pattern hair loss, and adult acne vulgaris.[A178135] Spironolactone is also frequently used for its antiandrogenic effects in transgender female patients due to its low cost and reducing male-pattern hair growth.[A178138]
DB00700EplerenoneFor improvement of survival of stable patients with left ventricular systolic dysfunction (ejection fraction <40%) and clinical evidence of congestive heart failure after an acute myocardial infarction.
DB09015Canrenoic acidNot Available
DB12221CanrenoneNot Available
DB01395DrospirenoneFor the prevention of pregnancy in women who elect an oral contraceptive.
DrugDrug NameTargetType
DB00421SpironolactoneMineralocorticoid receptortarget
DB00421SpironolactoneCytochrome P450 2C8enzyme
DB00421SpironolactoneCanalicular multispecific organic anion transporter 1transporter
DB00421SpironolactoneMultidrug resistance protein 1transporter
DB00421SpironolactoneSolute carrier organic anion transporter family member 1A2transporter
DB00421SpironolactoneCytochrome P450 11B1, mitochondrialenzyme
DB00421SpironolactoneAndrogen receptortarget
DB00421SpironolactoneProgesterone receptortarget
DB00421SpironolactoneGlucocorticoid receptortarget
DB00421SpironolactoneCytochrome P450 11B2, mitochondrialtarget
DB00421Spironolactone17alpha-hydroxylasetarget
DB00421Spironolactone17,20-desmolasetarget
DB00421Spironolactone3-oxo-5-alpha-steroid 4-dehydrogenasetarget
DB00421SpironolactoneSex hormone-binding globulintarget
DB00421SpironolactoneVoltage-dependent calcium channeltarget
DB00421SpironolactoneDihydrotestosterone receptortarget
DB00421SpironolactoneNuclear receptor subfamily 1 group I member 2target
DB00421SpironolactoneBile salt export pumptransporter
DB00421SpironolactoneSerum albumincarrier
DB00421Spironolactonealpha1-acid glycoproteincarrier
DB00700EplerenoneMineralocorticoid receptortarget
DB00700EplerenoneCytochrome P450 3A4enzyme
DB00700EplerenoneCytochrome P450 3A5enzyme
DB00700EplerenoneCytochrome P450 3A7enzyme
DB00700EplerenoneCytochrome P450 11B2, mitochondrialenzyme
DB01395DrospirenoneProgesterone receptortarget
DB01395DrospirenoneMineralocorticoid receptortarget
DB01395DrospirenoneAndrogen receptortarget
DB01395DrospirenoneProstaglandin G/H synthase 2enzyme
DB01395DrospirenoneCholinesteraseenzyme
DB01395DrospirenoneCytochrome P450 3A4enzyme