What is the use of Spironolactone (aldosterone antagonist)?

From the Guidelines

Spironolactone is conditionally recommended for the treatment of acne in women, particularly those with hormonal acne, at a dose of 50-100 mg daily, due to its anti-androgenic properties and moderate certainty evidence from recent studies 1.

Key Points to Consider

• Spironolactone works by blocking aldosterone receptors, reducing sodium and water retention, and preserving potassium levels in the body, while also inhibiting 5a-reductase and increasing steroid-hormone binding globulin 1.
• The medication is not FDA-approved for acne treatment but has been used off-label for over 30 years due to its impact on sebum production through inhibition of the androgen receptor on sebocytes 1.
• Common side effects include menstrual irregularities, diuresis, breast tenderness or enlargement, gynecomastia, fatigue, headache, and dizziness, with menstrual irregularities being dose-dependent and less common among those using combined oral contraceptives (COC) 1.
• Potassium monitoring should be considered in older patients, those with medical co-morbidities, and patients taking medications affecting renal, adrenal, and hepatic function, and a diet high in potassium should be avoided 1.
• Spironolactone should not be used in pregnancy due to the risk of feminization of a male fetus and carries a warning on tumorigenicity based on chronic toxicity studies in rats 1.

Clinical Considerations

• The starting dose is typically 50-100 mg daily, with doses up to 200 mg/day possible but associated with increased side effects 1.
• Several months of treatment are typically required to reach the full effectiveness of spironolactone for acne 1.
• Regular monitoring of kidney function and potassium levels is necessary while taking this medication, especially when starting treatment or adjusting dosage 1.
• Spironolactone may be effective for acne in women of all ages and its use should not be limited only to adult women or women with prominent acne on the lower face or acne that flares with their menstrual cycle 1.

From the FDA Drug Label

The FDA drug label does not answer the question.

From the Research

Uses of Spironolactone

• Spironolactone is used in the treatment of patients with heart failure with reduced ejection fraction, by halting the disease progression, with significant beneficial effects on both morbidity and mortality 2.
• It is also used to treat resistant hypertension, edema in patients with cirrhosis, and other on- and off-label uses 2.
• In dermatology, spironolactone is used to treat acne, hidradenitis suppurativa, female pattern baldness, and hirsutism due to its anti-androgenic effect 3, 4.

Benefits and Safety

• Spironolactone has been shown to be a very effective adjunctive agent in the treatment of patients with heart failure with reduced ejection fraction 2.
• The use of spironolactone in patients with heart failure with preserved ejection fraction may offer some symptomatic relief 2.
• Spironolactone has a good safety profile, but may cause side effects such as hyperkalemia, hyponatremia, hypotension, gynecomastia, and abdominal pain 5.
• Close follow-up by a dedicated heart failure team can minimize the risk for adverse events and complications associated with spironolactone use 5.

Formulations and Administration

• A liquid suspension formulation of spironolactone, CaroSpir®, was approved by the FDA in 2017, which enables more heart failure and other patients to avail themselves of the protective and beneficial effects of spironolactone 2.
• The new drug formulation comes as a banana-flavored oral suspension that contains 25 mg/5 mL of spironolactone, supplied in 4-ounce (118 mL) and 16-ounce (473 mL) bottles 2.