Spironolactone
Spironolactone
Aldactone, CaroSpir
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Summary
Classes
Common uses
Heart failure with reduced ejection fraction0, Primary aldosteronism0, Ascites in cirrhosis0, Resistant hypertension0, Hirsutism / hormonal acne (off-label)0
Pharmacy
Starting dose
25 mg PO once daily for HFrEF and primary aldosteronism; up to 100 mg/d for ascites; 50-200 mg/d for hirsutism
Preparations
25 mg, 50 mg, 100 mg tablets; 25 mg/5 mL oral suspension (CaroSpir)
US FDA Max
400 mg/d (acute primary aldosteronism diagnosis); 100-200 mg/d typical chronic
Pharmacology
Routes
Oral
Onset
Natriuresis at 2-3 days; endocrine effects (gynecomastia, antiandrogen action) over weeks
Duration
Variable; biologically active metabolite carries effect beyond plasma half-life
Half-life
1.4 hours (parent); 13-24 hours for active metabolite canrenone[1]
Bioavailability
~70% (oral; bioavailability and absorption are improved with food)[1]
Pregnancy
Avoid in pregnancy; antiandrogen effects can feminize a male fetus.[citation needed]
Legal status
Rx-only in US
Purported mechanism
Spironolactone is a competitive antagonist of the mineralocorticoid receptor; blocking aldosterone-driven transcription in collecting-duct principal cells decreases epithelial sodium channel (ENaC) and Na+/K+ ATPase activity, producing natriuresis with potassium and proton retention.0 At higher concentrations it also binds the androgen receptor (antiandrogen) and the progesterone receptor (PR partial agonism), accounting for gynecomastia, breast tenderness, antiandrogen efficacy in hirsutism/acne, and menstrual irregularity. RALES (1999) established the mortality benefit in severe HFrEF that defines its modern HF role[1].
References
- ↑ 1.0 1.1 1.2 FDA Prescribing Information, Aldactone (spironolactone), Pfizer, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/012151s075lbl.pdf