Spironolactone uses and side effects
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Spironolactone: Uses and Side Effects
Mechanism of Action
Spironolactone is a potassium-sparing diuretic and aldosterone antagonist (mineralocorticoid receptor blocker). It also competitively inhibits androgen receptors and has progesterone receptor agonist activity, which accounts for many of its off-target effects.
Clinical Uses
| Indication | Notes |
|---|---|
| Heart failure (HFrEF) | Reduces mortality in systolic heart failure; blocks aldosterone-mediated cardiac remodeling |
| Primary hyperaldosteronism | First-line medical therapy for bilateral adrenal hyperplasia; blocks excess aldosterone |
| Hypertension | Particularly resistant hypertension; fourth-line add-on agent |
| Edema / ascites | Useful in cirrhotic ascites (often combined with furosemide) |
| Hirsutism | Dose-dependent antiandrogen effect; competitive androgen receptor inhibition + 5α-reductase inhibition |
| Acne (female patients) | Reduces androgenic stimulation of sebaceous glands |
| Polycystic ovary syndrome (PCOS) | Addresses hyperandrogenism (hirsutism, acne) |
| Female pattern hair loss | Off-label antiandrogen use |
| Gender-affirming therapy (MTF) | Used as antiandrogen component |
Side Effects
Endocrine / Hormonal (dose-dependent)
- Gynecomastia in men (androgen receptor antagonism)
- Sexual dysfunction in men (decreased libido, erectile dysfunction)
- Menstrual irregularities in women (may be mitigated by concurrent oral contraceptive use)
- Risk of feminization of a male fetus if used during early pregnancy — contraindicated in pregnancy
Electrolyte / Renal
- Hyperkalemia — most serious; risk increases with renal impairment, ACE inhibitors/ARBs, NSAIDs, or high potassium diet
- Hyponatremia — from diuretic effect
- Contraindicated in significant renal impairment (risk of dangerous hyperkalemia)
Cardiovascular
- Postural hypotension / dizziness — especially early in treatment
- Increased diuresis — can cause volume depletion
Gastrointestinal
- Nausea, vomiting, gastric upset
- Diarrhea
Other
- Breast tenderness
- Headache
- Fatigue
Key Drug Interactions
- ACE inhibitors / ARBs / potassium supplements → additive hyperkalemia risk
- NSAIDs → reduced diuretic efficacy + increased hyperkalemia risk
- Oral contraceptives containing drospirenone (DSP) → DSP has mild mineralocorticoid activity; combination not recommended (additive potassium retention)
Monitoring
- Serum potassium and renal function should be checked at baseline, within 1 week of initiation or dose change, and periodically thereafter
- Blood pressure monitoring, especially in the elderly
Sources: "Evaluation and Treatment of Hirsutism in Premenopausal Women" (p. 12); "Management of Primary Aldosteronism" (p. 24)
Note: Eplerenone is a more selective mineralocorticoid receptor antagonist with fewer hormonal side effects than spironolactone, though it is somewhat less potent at equivalent doses.
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