Spironolactone is a potassium-sparing diuretic. It binds to mineralocorticoid receptors and functions as aldosterone antagonists.[A178192] It promotes sodium and water excretion and potassium retention.[A11837] Spironolactone was originally developed purely for this ability before other pharmacodynamic properties of the drug were discovered.[A11837, A178246] It is indicated to treat several conditions, including heart failure, edema, hyperaldosteronism, and hypertension.[L44602] Off-label uses of spironolactone include hirsutism, female pattern hair loss, and adult acne vulgaris.[A178135, A261025] Spironolactone was developed in 1957, marketed in 1959, and approved by the FDA on January 21, 1960.[A178243, L6187]
Spironolactone is indicated for the treatment of the following conditions: - NYHA Class III-IV heart failure and reduced ejection fraction to increase survival, manage edema, and reduce the need for hospitalization for heart failure. Spironolactone is usually administered in conjunction with other heart failure therapies.[L44602] - Hypertension, as add-on therapy, in patients not adequately controlled by other agents.[L44602, L47810] - Edema associated with hepatic cirrhosis when edema is not responsive to fluid and sodium restriction.[L44602, L47810] - Edema associated with nephrotic syndrome when treatment of the underlying disease, restriction of fluid and sodium intake, and the use of other diuretics produce an inadequate response.[L44602] - Refractory edema associated with congestive cardiac failure, malignant ascites, hepatic cirrhosis with ascites, and essential hypertension.[L47810] - Short-term preoperative treatment of patients with primary hyperaldosteronism.[L44602, L47810] - Diagnosis of primary aldosteronism.[L47810] - Long-term maintenance therapy for patients with discrete aldosterone-producing adrenal adenomas who are not candidates for surgery.[L44602] - Long-term maintenance therapy for patients with bilateral micro or macronodular adrenal hyperplasia (idiopathic hyperaldosteronism).[L44602] As spironolactone has antiandrogenic activity, its off-label uses include the treatment of hirsutism, female pattern hair loss, and adult acne vulgaris.[A178135, A261025]
Categories
Agents causing hyperkalemia
Antihypertensive Agents
Antihypertensive Agents Indicated for Hypertension
BSEP/ABCB11 Substrates
Cardiovascular Agents
Cytochrome P-450 CYP2C8 Inhibitors
Cytochrome P-450 CYP2C8 Inhibitors (moderate)
Cytochrome P-450 Enzyme Inhibitors
Diuretics
Fused-Ring Compounds
Hormone Antagonists
Hormones, Hormone Substitutes, and Hormone Antagonists
Drug Info/Drug Targets: DrugBank 3.0: a comprehensive resource for 'omics' research on drugs. Knox C, Law V, Jewison
T, Liu P, Ly S, Frolkis A, Pon A, Banco K, Mak C, Neveu V, Djoumbou Y, Eisner R, Guo AC, Wishart DS.
Nucleic Acids Res. 2011 Jan; 39 (Database issue):D1035-41. | PMID:21059682
