Spironolactone: From Hypertension to Polycystic Ovary Syndrome

Spironolactone, also known by its brand name Aldactone, has been approved by the FDA since 1960 and is widely used for various medical conditions. It belongs to a class of medications called potassium-sparing diuretics, often referred to as “water pills.”

Use

Spironolactone is FDA-approved to treat:

• High blood pressure (hypertension)
• Heart failure
• Edema (fluid retention) associated with congestive heart failure, cirrhosis of the liver, and nephrotic syndrome (a rare kidney disease causing excessive protein in urine)
• Low potassium levels in the blood (hypokalemia)

Moreover, spironolactone is prescribed "off-label" for:

• Hormonal acne: Especially effective for women with acne driven by hormones and unresponsive to other treatments
• Hirsutism: Excessive hair growth in women, often due to elevated androgen levels, can be managed with spironolactone
• Polycystic ovary syndrome (PCOS): Used to alleviate symptoms like acne, hirsutism, and irregular menstrual cycles due to its anti-androgenic properties
• Female pattern hair loss (androgenetic alopecia): Spironolactone may be used to treat hair thinning and loss by reducing androgen levels

How It Works

Spironolactone works by blocking the action of aldosterone, a hormone produced by the adrenal glands located on top of each kidney. Aldosterone normally tells the kidneys to hold onto sodium and water while getting rid of potassium. By inhibiting aldosterone, spironolactone causes the body to release more sodium and water while keeping potassium levels stable.

This medication, often called a "water pill," acts as a diuretic, helping the body eliminate excess fluid and salt through urine. By blocking aldosterone's effects, spironolactone encourages the removal of sodium and water while maintaining potassium levels. This process can help reduce fluid retention and lower blood pressure.

Dosing and Administration

Spironolactone comes in tablet form, available in strengths of 25mg, 50mg, and 100mg, and can be taken orally, with or without food.

An oral suspension form, called CaroSpir, is also available for those who have difficulty swallowing. Store CaroSpir at room temperature and shake the bottle well before each use. For precise dosing, use the dosing cup or syringe provided by your pharmacy, as using household kitchen or measuring spoons may result in inaccurate dosing.

Please note that spironolactone tablets (Aldactone) and the oral suspension (CaroSpir) are not interchangeable and should not be substituted for each other.

Side Effects

Common Side Effects

• Increased urination, which may lead to dehydration, low blood pressure, or even kidney problems
• Dizziness
• Fatigue
• Nausea
• Vomiting
• Headache
• Diarrhea
• Enlargement of male breasts or breast pain or swelling in males and females
• Decreased sex drive or libido
• Sexual dysfunction
• Irregular or lack of menstrual periods
• Increased potassium levels
• Decreased sodium levels

If you are experiencing any of these side effects, talk with your healthcare provider to determine whether a dose adjustment or switching to a different medication would be beneficial for you.

Serious Side Effects

• Lightheadedness
• High potassium levels: Nausea, muscle weakness, tingling sensation, chest pain, difficulty breathing, irregular heartbeats, loss of movement
• Electrolyte imbalances: Increased thirst or urination, confusion, vomiting, muscle pain, slurred speech, severe weakness, numbness, loss of coordination
• Kidney failure: Decreased urination, muscle cramps, nausea, vomiting, tiredness, or swelling
• Severe skin reactions: Sore throat, fever, tiredness, difficulty swallowing, stinging sensation in the eyes, body aches, rash, itchiness, peeling or blistering of the skin
• Allergic reactions: Difficulty breathing or swallowing, swelling on your face, lips, mouth, or throat, peeling skin, rash, hives

If you are experiencing any of these serious side effects, immediately call your doctor and stop taking this medication.

Contraindications

Spironolactone should not be used in patients who:

• Have a known allergy or hypersensitivity to spironolactone or any of its components.
• Have acute kidney injury or severe renal impairment.
• Have hyperkalemia (high potassium levels in the blood).
• Are taking potassium-sparing diuretics, potassium supplements, or other medications that increase potassium levels in their blood, due to the risk of hyperkalemia.
• Have Addison's disease: A rare condition characterized by adrenal insufficiency. Spironolactone can exacerbate electrolyte imbalances.
• Are pregnant: Spironolactone may cause fetal harm, particularly in the first trimester.
• Are taking Eplerenone (Inspra), which is an aldosterone receptor antagonist that is often used for heart failure after a heart attack, as well as hypertension.

Warnings

Warnings associated with spironolactone include the following:

• Hyperkalemia (high blood potassium levels): Spironolactone can cause an increase in potassium levels in your blood, which may lead to serious health complications such as abnormal heart rhythms or even cardiac arrest.
• Breast pain or swelling (gynecomastia): Spironolactone can disrupt hormonal balance, leading to the development of breast tissue in males (gynecomastia) or breast pain and swelling in females, especially with higher doses of the medication. This effect is due to its anti- androgenic properties and may occur with prolonged use or at higher doses.
• Low blood pressure and kidney problems: Patients with existing kidney function may experience worsened kidney function when taking spironolactone or those concurrently taking medications known to affect kidney function, such as NSAIDs and specific antibiotics. Spironolactone's effects can lead to increased urination, potentially resulting in dehydration and worsening low blood pressure as well as kidney complications.
• Electrolyte imbalance: Besides hyperkalemia, spironolactone may also lead to imbalances in sodium, chloride, magnesium, and calcium levels in your blood.

Patients taking spironolactone should be aware of these potential risks and discuss any concerns with their doctor. Regular monitoring and follow-up appointments are essential to ensure the safe and effective use of this medication.

Interactions

Using potassium supplements or salt substitutes containing potassium while on spironolactone can result in high potassium levels in your blood, potentially leading to heart complications. These are recommended to be avoided unless instructed to do so by your healthcare provider.

Avoid using Spironolactone with medications that could increase your risk of certain side effects, including heart medications, such as Digoxin, mood stabilizers, such as lithium, or nonsteroidal anti-inflammatory drugs, known as NSAIDs, such as Ibuprofen or aspirin.

Pregnancy and Breastfeeding

Spironolactone is generally not recommended for use during pregnancy due to potential risks to the developing fetus. Studies in animals have shown reproductive toxicity, including birth defects. While data in humans is limited, there have been reports of spironolactone affecting the development of male genitals in male babies.

When it comes to breastfeeding, spironolactone can pass into breast milk. While the extent of its presence and its effects on nursing infants are not well studied, it is generally recommended to avoid spironolactone during breastfeeding, especially in newborns and preterm infants, due to potential adverse effects on electrolyte balance and hormones.

In certain situations where the benefits of spironolactone outweigh the risks, your healthcare provider may determine that its use during pregnancy or breastfeeding is necessary. In such cases, close monitoring of both the mother and the infant is essential to minimize potential adverse effects.

Speak with Your Doctor

Speaking with your doctor about spironolactone is important to understand its benefits and safety profile tailored to your condition. This ensures that you make well-informed decisions regarding the use of spironolactone and receive the appropriate monitoring and care throughout your treatment.