Spironolactone

Aka: Spironolactone, Aldactone

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II. Indications

  1. Left-sided Congestive Heart Failure
    1. First line agent for NYHA Class III or IV Heart Failure, in conjunction with ACE Inhibitor and Beta Blocker
    2. Monitor for Hyperkalemia (esp. with ACE Inhibitor) and renal dysfunction
    3. May use Eplerenone as an alternative (but more expensive)
  2. Edematous States
    1. Cirrhosis
    2. Primary Hyperaldosteronism
    3. Nephrotic Syndrome
  3. Hyperandrogenism in women
    1. Hirsutism
    2. Polycystic Ovary Disease
  4. Hyperaldosteronism
    1. First-line treatment for Hyperaldosteronism
  5. Refractory Hypertension
    1. See Hypertension Combination Therapy

III. Contraindications

  1. Anuria
  2. Renal Insufficiency with Serum Creatinine over 2.4 mg/dl (GFR <30 ml/minute/1.73m2)
  3. Hyperkalemia (Serum Potassium >5 meq/L)

IV. Mechanism

  1. Potassium-Sparing Diuretic via Aldosterone blockade
    1. Spironolactone is a Aldosterone competitive inhibitor
    2. Acts at distal convoluted renal tubule
    3. Inhibits Sodium retention
  2. Congestive Heart Failure
    1. Works synergistically with ACE Inhibitors in CHF
    2. ACE Inhibitors block Angiotensin II production
      1. Renal response is to increase Aldosterone
      2. Spironolactone blocks Aldosterone escape

V. Drug Interactions

  1. P-Glycoprotein Inhibitor
  2. Increased Serum Potassium (Hyperkalemia risk)
    1. Potassium Supplementation
    2. NSAIDs
    3. ACE Inhibitor
    4. Trimethoprim-Sulfamethoxazole
  3. Salicylates
    1. Decrease Spironolactone effect
  4. Digoxin
    1. Increased Digoxin Toxicity risk via increased Digoxin half life
  5. Norepinephrine
    1. Decreases NorepinephrineVasopressor activity

VI. Dosing

  1. Congestive Heart Failure
    1. Start 12.5 mg orally daily
    2. May increase to 25 mg orally daily after 4 weeks (up to 50 mg, but increased risk of Hyperkalemia)
    3. Monitor Serum Potassium at 3 days, 7 days and then monthly for the first 3 months
  2. Edema
    1. Dose: 50 to 100 mg orally per day divided once to twice daily
    2. Maximum: 200 mg/day
  3. Hyperandrogenism
    1. Dose: 50 mg orally twice daily
  4. Hypertension
    1. Dose: 12.5 to 50 mg orally daily
    2. Maximum: 100 mg
  5. Primary Hyperaldosteronism
    1. Dose: 100 to 400 mg/day preoperatively
    2. Use the lowest effective dose

VII. Monitoring

  1. Serum Potassium
  2. Renal Function (Serum Creatinine)

VIII. Pharmacokinetics

  1. Liver metabolism to active metabolite (canrenone)
  2. Primarily renal excretion
  3. Half-Life: 14 to 16 hours (up to 24-36 hours)
  4. Duration: 2 to 3 days

IX. Adverse Effects

  1. See Potassium-Sparing Diuretic
  2. Gynecomastia (in men)
  3. Mastodynia
  4. Erectile Dysfunction
  5. Alopecia
  6. Hyperkalemia
    1. Avoid excessive Dietary Potassium

X. Safety

  1. Pregnancy Category C
  2. Safe in Lactation

XI. Resources

  1. Spironolactone (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=fb66327e-8261-46ae-b39a-4fa79d520844

XII. References

  1. (2017) Presc Lett 24(12): 69
  2. Margo (2001) Am Fam Physician 64(8):1393-8 [PubMed]
  3. Pitt (1999) N Engl J Med 341:709-17 [PubMed]

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Related Studies

Cost: Medications

spironolactone (on 12/21/2022 at Medicaid.Gov Survey of pharmacy drug pricing)
SPIRONOLACTONE 100 MG TABLET Generic $0.18 each
SPIRONOLACTONE 25 MG TABLET Generic $0.05 each
SPIRONOLACTONE 50 MG TABLET Generic $0.10 each
SPIRONOLACTONE-HYDROCHLOROTHIAZIDE 25-25 TAB Generic $0.58 each
FPNotebook does not benefit financially from showing this medication data or their pharmacy links. This information is provided only to help medical providers and their patients see relative costs. Insurance plans negotiate lower medication prices with suppliers. Prices shown here are out of pocket, non-negotiated rates. See Needy Meds for financial assistance information. GoodRx is another tool for finding lower drug prices.

Ontology: Spironolactone (C0037982)

Definition (NCI) A synthetic 17-spironolactone corticosteroid with potassium-sparing diuretic, antihypertensive, and antiandrogen activities.Spironolactone competitively inhibits adrenocortical hormone aldosterone activity in the distal renal tubules, myocardium, and vasculature. This agent may inhibit the pathophysiologic effects of aldosterone produced in excess by various types of malignant and benign tumors.
Definition (MSH) A potassium sparing diuretic that acts by antagonism of aldosterone in the distal renal tubules. It is used mainly in the treatment of refractory edema in patients with congestive heart failure, nephrotic syndrome, or hepatic cirrhosis. Its effects on the endocrine system are utilized in the treatments of hirsutism and acne but they can lead to adverse effects. (From Martindale, The Extra Pharmacopoeia, 30th ed, p827)
Definition (CSP) potassium sparing diuretic that acts by antagonism of aldosterone in the distal renal tubules; used mainly in the treatment of refractory edema in patients with congestive heart failure, nephrotic syndrome, or hepatic cirrhosis; its effects on the endocrine system are utilized in the treatments of hirsutism and acne but they can lead to adverse effects.
Definition (PDQ) A synthetic 17-spironolactone corticosteroid with potassium-sparing diuretic, antihypertensive, and antiandrogen activities. Spironolactone competitively inhibits adrenocortical hormone aldosterone activity in the distal renal tubules, myocardium, and vasculature. This agent may inhibit the pathophysiologic effects of aldosterone produced in excess by various types of malignant and benign tumors. Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=39444&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=39444&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C840" NCI Thesaurus)
Concepts Pharmacologic Substance (T121) , Steroid (T110)
MSH D013148
SnomedCT 13929005, 387078006
LNC LP16280-7, MTHU003227
English Spirolactone, Veroshpiron, Verospirone, Pregn-4-ene-21-carboxylic acid, 7-(acetylthio)-17-hydroxy-3-oxo-, gamma-lactone, (7alpha,17alpha)-, 17-Hydroxy-7alpha-mercapto-3-oxo-17alpha-pregn-4-ene-21-carboxylic Acid, gamma Lactone, Acetate, spironolactone, Spironolactone, SPL, spironolactone (medication), SPIRONOLACTONE, Spironolactone [Chemical/Ingredient], spirolactones, spirolactone, Spironolactone (product), Spironolactone (substance)
Swedish Spironolakton
Czech spironolakton
Finnish Spironolaktoni
Russian SPIROLAKTON, VEROSHPIRON, SPIRONOLAKTON, ВЕРОШПИРОН, СПИРОЛАКТОН, СПИРОНОЛАКТОН
Japanese アポラスノン, ダイロパール, アルパメド, アルダクトンA, ラッカルミン, メラルコン, アルダクトン, アルマトール, アレキサン, ホクラトン, ピロラクトン, スピロラクトン, オジロール, スピロノール, スピロノラクトン, アポタクッス
Italian Spirolattone, Spironolattone
Croatian SPIRONOLAKTON
Polish Spironolakton, Aldakton
Spanish espironolactona (producto), espironolactona (sustancia), espironolactona, Espirolactona, Espironolactona
French Spironolactone
German Spirolacton, Spironolacton
Portuguese Espirolactona, Espironolactona
Derived from the NIH UMLS (Unified Medical Language System)

Ontology: Aldactone (C0591054)

Concepts Pharmacologic Substance (T121) , Steroid (T110)
MSH D013148
English Pfizer Brand of Spironolactone, aldactone, Aldactone, Roche Brand of Spironolactone, Searle Brand of Spironolactone
Derived from the NIH UMLS (Unified Medical Language System)

Related Topics in Pharmacology

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