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Spironolactone – Uses, Dosage and Side Effects

Spironolactone is a potassium-sparing diuretic and aldosterone antagonist used to treat heart failure, high blood pressure, and fluid retention.

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Things worth knowing about "Spironolactone"

Spironolactone is a potassium-sparing diuretic and aldosterone antagonist used to treat heart failure, high blood pressure, and fluid retention.

What is Spironolactone?

Spironolactone is a prescription medication belonging to the class of potassium-sparing diuretics. It acts as an aldosterone antagonist, meaning it blocks the effects of aldosterone, a hormone that regulates the balance of water and salt in the body. Spironolactone has been used in clinical medicine for decades and is included on the World Health Organization (WHO) List of Essential Medicines.

Indications – When is Spironolactone Used?

Spironolactone is prescribed for a wide range of conditions:

Heart failure: To reduce fluid retention and improve cardiac function
Arterial hypertension (high blood pressure): As an add-on therapy, especially in primary hyperaldosteronism
Liver cirrhosis with ascites: To treat fluid accumulation in the abdominal cavity
Nephrotic syndrome: For fluid retention caused by kidney disease
Primary hyperaldosteronism (Conn syndrome): Excess aldosterone production from adrenal gland disorders
Acne and hirsutism in women: Due to its anti-androgenic effects
Polycystic ovary syndrome (PCOS): To manage symptoms related to elevated androgens

Mechanism of Action

Aldosterone is a hormone produced by the adrenal cortex that signals the kidneys to retain sodium (salt) and water while excreting potassium. Spironolactone blocks the aldosterone receptor in the kidneys (specifically in the distal tubule and collecting duct). This inhibits sodium reabsorption, promotes water excretion, and preserves potassium levels in the body -- hence the name potassium-sparing diuretic.

In addition, spironolactone has anti-androgenic properties because it also binds to androgen receptors, reducing the effects of male sex hormones such as testosterone. This accounts for its use in hormone-related skin conditions in women.

Dosage

The dosage of spironolactone depends on the indication and the individual response of the patient:

Heart failure: Typically 25--50 mg per day
Hypertension / hyperaldosteronism: Usually 50--200 mg per day
Liver cirrhosis with ascites: Often 100--400 mg per day, frequently combined with furosemide
Acne / hirsutism in women: Commonly 50--200 mg per day

Spironolactone is taken orally (as a tablet) and can be taken with or without food. The exact dosage is always determined by the treating physician.

Side Effects

Like all medications, spironolactone can cause side effects. Common and clinically relevant side effects include:

Hyperkalemia (elevated potassium levels in the blood): Especially in patients with kidney impairment or those taking other potassium-raising medications -- this can be dangerous
Gynecomastia (breast tissue enlargement in men): Due to its anti-androgenic and weakly estrogenic properties
Menstrual irregularities in women
Dizziness and low blood pressure, especially at the start of treatment
Gastrointestinal complaints: Nausea, vomiting, stomach pain
Fatigue and headache
Reduced libido and erectile dysfunction in men

Drug Interactions

Spironolactone can interact with various other medications:

ACE inhibitors and ARBs (e.g., ramipril, losartan): Increased risk of hyperkalemia
Other potassium-sparing diuretics (e.g., amiloride, triamterene): Further increased risk of hyperkalemia
Potassium supplements and potassium-rich diets: Use with caution
Non-steroidal anti-inflammatory drugs (NSAIDs) such as ibuprofen: May reduce the diuretic effect
Digoxin: Spironolactone may increase digoxin plasma levels

Contraindications – When Should Spironolactone Not Be Used?

Severe renal insufficiency (kidney failure)
Hyperkalemia (already elevated potassium levels)
Addison disease (adrenocortical insufficiency)
Pregnancy and breastfeeding
Hypersensitivity to spironolactone or any of its excipients

Important Note

Spironolactone is a prescription-only medication and must only be taken under the supervision of a qualified physician. Regular blood tests -- particularly to monitor potassium and kidney function -- are necessary during treatment.

References

World Health Organization (WHO) -- Model List of Essential Medicines, 23rd Edition (2023). Available at: https://www.who.int/publications/i/item/WHO-MHP-HPS-EML-2023.02
Pitt B. et al. -- The Effect of Spironolactone on Morbidity and Mortality in Patients with Severe Heart Failure. New England Journal of Medicine, 1999; 341(10): 709--717.
Funder JW. et al. -- The Management of Primary Aldosteronism: Case Detection, Diagnosis, and Treatment. Journal of Clinical Endocrinology and Metabolism, 2016; 101(5): 1889--1916.

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