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Clinical ResearchResearch compound

Spironolactone

An aldosterone antagonist (potassium-sparing diuretic) that is also an antiandrogen. Oral spironolactone is one of the most widely used, but OFF-LABEL, agents for female-pattern hair loss (FPHL); the compounded, roughly 5% topical form is intended for local, scalp-level antiandrogen action with a smaller systemic burden. It is not approved for hair anywhere.

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Spironolactone vial

WHAT IS SPIRONOLACTONE?

Detailed overview

Spironolactone is originally an aldosterone antagonist, a potassium-sparing diuretic, which the FDA approved for high blood pressure, heart failure, hyperaldosteronism and edema; for hair loss, however, it is not approved anywhere. In addition, it has an antiandrogen effect: it blocks the androgen receptor and reduces androgen (testosterone) production, so less DHT acts on the hair follicle. Through this mechanism, oral spironolactone has become one of the most widely used, but exclusively OFF-LABEL, agents for female-pattern hair loss (FPHL), as well as for hirsutism and acne in women. The aim of the compounded, roughly 5% topical form is to achieve a local, scalp-level antiandrogen effect with far smaller systemic absorption compared to the oral form; this form is not approved. According to the evidence, oral spironolactone has moderate evidence in women (FPHL), while the topical evidence is still only emerging and limited: systematic reviews and treatment guidelines for FPHL and androgenetic alopecia mention oral spironolactone mainly as an off-label option for women. Importantly, this is primarily a FEMALE FPHL option: in men the oral form is generally avoided because of feminizing effects (e.g. gynecomastia), and topical use in men is at an experimental stage, precisely in order to avoid systemic feminization.

Class

Aldosterone antagonist (potassium-sparing diuretic) + antiandrogen

Status

Approved for other indications; off-label for hair, mainly in women

Mechanism of action

Androgen receptor antagonist + reduces androgen production

Form / dose

Topical ~5% / oral 50–200 mg/day (in women)

Evidence

Moderate for oral in women; still emerging and limited for topical

Data console

Lab data

/lab/molecular-data.jsonLIVE
> Classification-
> StructureN/A
> Molecular weightN/A
> Target area-
> Storage2–8°C
> Stability~30 days reconstituted

Safety

Side effects, stop signs, contraindications

Side effects · 4

  • Hyperkalemia (raised blood potassium): the main systemic risk of the oral form; potassium levels must be monitored, with extra caution alongside ACE inhibitors, ARBs or potassium supplements.
  • Menstrual irregularity in women: the antiandrogen and hormonal effect can make the cycle irregular.
  • Breast tenderness and enlargement: a common, dose-related effect; in men this feminizing effect (gynaecomastia) is precisely why the oral form is generally avoided.
  • Increased urination (diuresis) with the oral form; the topical ~5% form has less systemic effect but local scalp irritation can occur.

Contraindications · 3

  • Pregnancy: spironolactone is teratogenic (risk of feminizing a male fetus) and is therefore contraindicated in pregnancy; pregnancy must be excluded/prevented before and during treatment.
  • Men: oral spironolactone is generally avoided for hair loss because of feminizing effects (e.g. gynaecomastia); topical use in men is investigational, precisely to avoid systemic feminization.
  • Pre-existing hyperkalemia or a condition/medication that raises potassium (ACE inhibitors, ARBs, potassium supplements): to be avoided or used only under close medical supervision with potassium monitoring, because of increased hyperkalemia risk.

Related Hair & Skin

Same therapeutic category

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Educational hair and skin info from official sources (PubMed, FDA, EMA). Does NOT replace medical consultation. Talk to a dermatologist!

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MolekulaX Editorial Team·Source-verified · PubMed · FDA · EMA

The information here is strictly for educational and scientific purposes. It does not replace medical advice or clinical consultation, and it does not encourage illegal substance or pharmaceutical use. Data is sourced. When in doubt, consult your doctor.