---
title: "Spironolactone: Research & Side Effects | BodyHackGuide"
url: https://www.bodyhackguide.co/compound/spironolactone
description: "Spironolactone: mechanism, clinical studies & side effects."
lang: en
---

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# Spironolactone

Skin & Hair: https://www.bodyhackguide.co/wiki#cat-skin-&-hair

Status

Approved (prescription)

Evidence

Not graded on a research bench yet

Spironolactone is a synthetic steroid that blocks the aldosterone (mineralocorticoid) receptor and also acts as an antiandrogen; it was first approved by the FDA on 21 January 1960 as Aldactone tablets and is a prescription diuretic for heart failure, high blood pressure, edema and primary hyperaldosteronism.

Reviewed 4 November 2026

01 Overview

## What Spironolactone is

Dermatologists prescribe spironolactone off-label for acne, female pattern hair loss and hirsutism because of its antiandrogen effects (PMID: 35138351, PMID: 41714473). In the 410-woman SAFA trial in England and Wales, spironolactone improved acne quality-of-life scores over placebo at 12 and 24 weeks (PMID: 37192767), while the hair-loss trials are smaller and mostly lack a placebo arm; the only placebo-controlled trial found in a PubMed search on 27 October 2026 enrolled 48 women (PMID: 40978669). Spironolactone can raise blood potassium, enlarge breast tissue and disturb menstrual cycles, and spironolactone and its metabolite canrenone are prohibited at all times in sport as diuretics (US prescribing information for Aldactone; PMID: 10471456; WADA Prohibited List 2026).

### How it works

### Aldosterone receptor blockade

Spironolactone and its active metabolites compete with aldosterone for its receptor at the sodium-potassium exchange site in the distal tubule of the kidney, so more sodium and water are excreted while potassium is kept (US prescribing information for Aldactone). This mineralocorticoid receptor blockade underlies the labeled uses in heart failure, high blood pressure, edema and primary hyperaldosteronism, and also the risk of a high blood potassium level (hyperkalemia), the first warning on the label (US prescribing information for Aldactone).

Read the full mechanism Show less

### Antiandrogen effects

Spironolactone binds the androgen receptor: the current US label notes that it may raise PSA in men taking abiraterone for prostate cancer for this reason, and it describes progestational and antiandrogenic effects in animals (US prescribing information for Aldactone). In rat skin, spironolactone or its metabolite canrenone rapidly reduced the number of available androgen receptor binding sites, which the authors attributed to competitive inhibition by canrenone (PMID: 487244). In castrated mice, spironolactone was more than four times as potent an antiandrogen as potassium canrenoate on seminal vesicle weight, and the authors suggested that minor metabolites with high androgen receptor affinity may explain the difference (PMID: 4064345). A 21-woman acne trial found that spironolactone lowered sex hormone binding globulin without significant changes in plasma testosterone or free testosterone (PMID: 2943311).

### Why this matters for skin and hair

Acne in adult women is driven mainly by hormones, and spironolactone targets the androgen receptor of the sebaceous glands (PMID: 38380975). In female pattern hair loss, androgens promote shrinking (miniaturization) of hair follicles by progressively shortening the growth phase (anagen) (PMID: 41714473).

### Pharmacokinetics

In 12 healthy men given spironolactone 100 mg a day for 15 days, half-lives after the last dose were 1.4 hours for spironolactone, 16.5 hours for canrenone, 13.8 hours for 7-alpha-thiomethylspirolactone and 15.0 hours for 6-beta-hydroxy-7-alpha-thiomethylspirolactone, and the sulfur-containing metabolite 7-alpha-thiomethylspirolactone, rather than canrenone, was the main metabolite in serum (PMID: 2723123). Food raised spironolactone bioavailability by about 95 percent, and spironolactone and its metabolites are more than 90 percent bound to plasma proteins (US prescribing information for Aldactone).

### Studied for

- Acne vulgaris
- Female pattern hair loss
- Hirsutism
- Heart failure
- Mineralocorticoid receptor pharmacology
- Antiandrogen pharmacology
- Pharmacoepidemiology

### Benefits listed

- Acne-specific quality of life at 12 and 24 weeks against placebo in the 410-woman SAFA trial (PMID: 37192767)
- Acne treatment success at 6 months against 3 months of doxycycline followed by placebo in a 133-woman trial (PMID: 38380975)
- Inflamed acne lesions in a 21-woman placebo-controlled crossover trial (PMID: 2943311)
- Moderate-to-marked hair improvement as an add-on to topical minoxidil in a 48-woman placebo-controlled pilot trial (PMID: 40978669)

Show 2 more Show less

- Hair density as an add-on to topical minoxidil in a 120-woman randomized trial (PMID: 35899211)
- Survival and hospital admissions in severe heart failure in the 1,663-patient RALES trial (PMID: 10471456)

02 Research

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## What the research shows

No research bench grades Spironolactone yet. Benches compare compounds people pair, with the evidence for each.

### Unlock the research summary

Enter your email to keep reading. It is free, and it opens these sections on every compound page in this browser.

- A summary of the key research
- Safety and side effects
- A link to the PubMed results

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03 Safety

## Spironolactone side effects and interactions

### Side effects

#### Common

- Menstrual irregularity (37.5 percent) as the main adverse event in a 48-woman hair-loss pilot trial, more common than with placebo (PMID: 40978669)
- Headache in 20 percent on spironolactone against 12 percent on placebo in the SAFA acne trial (PMID: 37192767)
- Breast enlargement or pain in 10 percent of men in RALES (PMID: 10471456)
- Dizziness, lightheadedness or orthostatic symptoms in 12.0 percent of women also taking low-dose oral minoxidil (PMID: 41654020)

#### Serious events

- Hyperkalemia, especially with kidney impairment or potassium-raising drugs (US prescribing information for Aldactone)
- Rise in hyperkalemia hospital admissions and deaths among older heart failure patients after RALES (PMID: 15295047)
- Feminization of male fetuses in rats exposed in late pregnancy (US prescribing information for Aldactone)
- Severe skin reactions (Stevens-Johnson syndrome, toxic epidermal necrolysis, DRESS) reported in clinical use (US prescribing information for Aldactone)
- Hepatic encephalopathy and coma in people with cirrhosis and ascites (US prescribing information for Aldactone)

### Who should not use it

Contraindications

The US label contraindicates spironolactone in people with hyperkalemia or Addison's disease and with concurrent use of eplerenone (US prescribing information for Aldactone).

Read all the contraindications and cautions Show less

Hyperkalemia risk rises with impaired kidney function and with potassium supplements, salt substitutes, ACE inhibitors, angiotensin receptor blockers, NSAIDs, heparin and trimethoprim (US prescribing information for Aldactone). Women aged 65 or older taking spironolactone for skin conditions had more hyperkalemia than women aged 45 to 64 (PMID: 41655839).

Spironolactone feminized male fetuses in rats, and the US label states that it should be avoided in pregnant women, or a pregnant woman told of the potential risk to a male fetus, because of its antiandrogenic properties (US prescribing information for Aldactone).

Sudden shifts in fluid and electrolytes may bring on hepatic encephalopathy and coma in people with liver cirrhosis and ascites (US prescribing information for Aldactone).

Gynecomastia or breast pain is a concern for men: it occurred in 10 percent of men taking spironolactone in RALES (PMID: 10471456).

Low blood pressure calls for caution: among 432 women taking spironolactone with low-dose oral minoxidil, dizziness, lightheadedness or orthostatic symptoms occurred in 12.0 percent, and taking one or more other blood pressure drugs raised the odds of these effects (odds ratio 3.29) (PMID: 41654020).

In competitive sport, spironolactone is on the World Anti-Doping Agency's list of substances prohibited at all times (WADA Prohibited List 2026).

### Interactions

8 pairings in our record: 3 to avoid, 2 with a caution and 3 to monitor.

- Eplerenone
  Avoid
  The US label contraindicates spironolactone with eplerenone (US prescribing information for Aldactone).
- Abiraterone
  Avoid
  Spironolactone binds the androgen receptor and may raise PSA in men taking abiraterone; the US label states that the combination is not recommended (US prescribing information for Aldactone).
- Mitotane
  Avoid
  Spironolactone lowered mitotane blood levels, and the US label advises against the combination (US prescribing information for Aldactone).
- ACE inhibitors and angiotensin receptor blockers
  Caution
  Combined use can lead to severe hyperkalemia (US prescribing information for Aldactone); after RALES, hospital admissions for hyperkalemia among older Ontario patients with heart failure on ACE inhibitors rose from 2.4 to 11.0 per 1,000 (PMID: 15295047).
- Potassium supplements and other potassium-raising drugs
  Caution
  Potassium supplements, potassium-containing salt substitutes, NSAIDs, heparin and trimethoprim can raise potassium and add to the hyperkalemia risk (US prescribing information for Aldactone).
- Lithium
  Monitor
  Spironolactone reduces the renal clearance of lithium, which raises the risk of lithium toxicity (US prescribing information for Aldactone).
- Oral minoxidil
  Monitor
  Among 432 women taking both drugs for hair loss, dizziness, lightheadedness or orthostatic symptoms occurred in 12.0 percent, more often with other blood pressure drugs (PMID: 41654020).
- Digoxin
  Monitor
  Spironolactone and its metabolites interfere with radioimmunoassays for digoxin and raise the apparent digoxin level (US prescribing information for Aldactone).

This interaction data is compiled from published research and community reports. It may not be exhaustive. Always consult a healthcare professional before combining compounds.

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04 Dosing

Free with email

## Dosing

No dose on record

Our record lists no dose for Spironolactone. This section holds what it does list.

### Unlock the Dosing section

- Route

05 Prices

## Spironolactone prices

No listings

We do not track a vendor for Spironolactone yet, so this page states no price.

06 Chemistry

## Chemistry and structure

Molecular formula

C24H32O4S

Molecular mass

416.6 g/mol

CAS number

52-01-7

Half-life

About 1.4 hours for spironolactone itself, with longer-lasting active metabolites: 16.5 hours for canrenone and 13.8 hours for 7-alpha-thiomethylspirolactone after 15 days of dosing in 12 healthy men (PMID: 2723123). The US prescribing information for Aldactone gives the same values.

View on PubChem (https://pubchem.ncbi.nlm.nih.gov/compound/5833)

07 Related

## Related to Spironolactone

### In the same category

- Acetyl Hexapeptide-8Marketed topical cosmetic ingredient Acetyl Hexapeptide-8 (INCI: Acetyl Hexapeptide-3 in older nomenclature, commercially known as Argireline) is a synthetic hexapeptide designed as a competitive inhibitor of the SNARE complex at the neuromuscular junction.: https://www.bodyhackguide.co/compound/acetyl-hexapeptide-8
- AHK-CuPreclinical AHK-Cu is a copper chelating tripeptide related to but distinct from GHK-Cu.: https://www.bodyhackguide.co/compound/ahk-cu
- DutasteridePhase 3 Dutasteride is a synthetic 4-azasteroid drug that blocks both type 1 and type 2 steroid 5-alpha-reductase, the enzymes that turn testosterone into dihydrotestosterone (DHT); it was developed at Glaxo Wellcome under the code GG745 and approved by the FDA in 2001 as Avodart for benign prostatic hyperplasia.: https://www.bodyhackguide.co/compound/dutasteride
- KetoconazoleApproved drug Ketoconazole is a synthetic imidazole antifungal that blocks the fungal cytochrome P450 enzyme lanosterol 14-alpha-demethylase and so stops the yeast or mold from making ergosterol for its cell membrane; it was the first broad-spectrum oral antifungal approved by the FDA, as Nizoral tablets from Janssen in 1981, and is also sold as 2 percent and 1 percent shampoos, creams and foams.: https://www.bodyhackguide.co/compound/ketoconazole
- Melanotan 2Discontinued A synthetic melanocortin receptor agonist studied for skin tanning, sexual function, and appetite suppression.: https://www.bodyhackguide.co/compound/melanotan-2
- MinoxidilFDA-Approved Minoxidil is an FDA-approved treatment for pattern hair loss. Originally an oral blood-pressure drug, its hair-growth side effect led to the topical products (Rogaine) at 2% and 5%.: https://www.bodyhackguide.co/compound/minoxidil

All compounds (https://www.bodyhackguide.co/wiki)

### Compare Spironolactone

- Alternatives to Spironolactone: https://www.bodyhackguide.co/alternatives-to/spironolactone

### Research tools

- Peptide Calculator Reconstitution and syringe units: https://www.bodyhackguide.co/tools/reconstitution
- Reconstitution Guide How to mix, step by step: https://www.bodyhackguide.co/guides/how-to-reconstitute-peptides
- Nasal Spray Calc mL per actuation: https://www.bodyhackguide.co/tools/intranasal
- Half-Life Visualizer Decay curves: https://www.bodyhackguide.co/tools/halflife

All articles (https://www.bodyhackguide.co/blog)

08 Questions

## Frequently asked questions

What is spironolactone?

Spironolactone is a synthetic steroid that blocks the aldosterone receptor and also acts as an antiandrogen (PMID: 19370553; US prescribing information for Aldactone). Spironolactone was first approved by the FDA in 1960 as Aldactone tablets (Drugs@FDA NDA 012151). It is labeled for heart failure, high blood pressure, edema and primary hyperaldosteronism (US prescribing information for Aldactone).

Is spironolactone approved for acne or hair loss?

Spironolactone is not FDA approved for acne or hair loss, and dermatologists use spironolactone off-label for those conditions (PMID: 35138351, PMID: 38380975). The American Academy of Dermatology's 2024 acne guideline makes a conditional recommendation for spironolactone (PMID: 38300170). Topical minoxidil is the only FDA-approved treatment for female pattern hair loss, and spironolactone is used for it off-label (PMID: 41714473).

Does spironolactone work for acne in women?

In the 410-woman SAFA trial, spironolactone improved the Acne-QoL symptom score over placebo by 1.27 points at 12 weeks and 3.45 points at 24 weeks (PMID: 37192767). In a 133-woman French trial, 6 months of spironolactone with benzoyl peroxide had higher treatment success at month 6 than 3 months of doxycycline with benzoyl peroxide followed by 3 months of placebo with benzoyl peroxide (PMID: 38380975). A 2025 meta-analysis of five placebo-controlled trials found higher odds of objective acne improvement with spironolactone (PMID: 40823723).

What is the evidence for spironolactone in female pattern hair loss?

In a 48-woman placebo-controlled pilot trial, spironolactone added to topical minoxidil raised terminal hair counts more than placebo, a difference that fell just short of significance (p=0.063), while more women on spironolactone were rated as moderately or markedly improved (PMID: 40978669). In a 204-woman trial, bicalutamide produced larger dermoscopic hair gains than spironolactone (PMID: 41742379). An open study of 80 women on spironolactone or cyproterone acetate found regrowth in 44 percent, without a control group (PMID: 15787815).

What do studies show about potassium levels with spironolactone?

Among 974 healthy young women taking spironolactone for acne, high potassium readings occurred in 0.72 percent of measurements, about the same as the 0.76 percent background rate in that population (PMID: 25796182). Among women aged 45 or older taking spironolactone for skin conditions, 10.1 percent had high potassium, and 22.4 percent of those aged 65 or older did (PMID: 41655839). The US label warns that spironolactone can cause hyperkalemia, especially with kidney impairment or potassium-raising drugs (US prescribing information for Aldactone).

Did spironolactone ever carry a cancer warning?

Aldactone labels on Drugs@FDA from 2008 to 2014 opened with a boxed warning that spironolactone was a tumorigen in chronic rat studies (Drugs@FDA NDA 012151). The Aldactone (spironolactone) label approved on 6 March 2018 has no boxed warning and keeps the rat findings in its toxicology section (Drugs@FDA NDA 012151). A 2022 meta-analysis of about 4.5 million people, most of them older adults, found no statistically significant association between spironolactone and breast cancer, with very low certainty of evidence, and the authors called for studies in younger people and in people with acne (PMID: 35138351).

Is spironolactone banned in sport?

Spironolactone is named in class S5, diuretics and masking agents, on the World Anti-Doping Agency's 2026 Prohibited List (WADA Prohibited List 2026). Spironolactone and its metabolite canrenone are prohibited both in and out of competition (WADA Prohibited List 2026).

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          "text": "Aldactone labels on Drugs@FDA from 2008 to 2014 opened with a boxed warning that spironolactone was a tumorigen in chronic rat studies (Drugs@FDA NDA 012151). The Aldactone (spironolactone) label approved on 6 March 2018 has no boxed warning and keeps the rat findings in its toxicology section (Drugs@FDA NDA 012151). A 2022 meta-analysis of about 4.5 million people, most of them older adults, found no statistically significant association between spironolactone and breast cancer, with very low certainty of evidence, and the authors called for studies in younger people and in people with acne (PMID: 35138351)."
        }
      },
      {
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          "@type": "Answer",
          "text": "Spironolactone is named in class S5, diuretics and masking agents, on the World Anti-Doping Agency's 2026 Prohibited List (WADA Prohibited List 2026). Spironolactone and its metabolite canrenone are prohibited both in and out of competition (WADA Prohibited List 2026)."
        }
      }
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