Verospiron

Approved Indications:

• Edema associated with congestive heart failure, liver cirrhosis, or nephrotic syndrome
• Primary hyperaldosteronism (for diagnosis and treatment)
• Hypertension (adjunctive therapy)
• Heart failure with reduced ejection fraction (HFrEF) to reduce morbidity and mortality
• Prevention and treatment of hypokalemia, especially in patients on potassium-wasting diuretics
• Ascites due to liver cirrhosis

Off-label (Clinically Accepted) Uses:

• Management of androgen-related conditions such as hirsutism and acne in women
• Polycystic ovary syndrome (PCOS) symptoms including hirsutism
• Pediatric nephrotic syndrome (adjunct therapy)
• Resistant hypertension

Adults:

• Edema: 25–200 mg per day orally in single or divided doses, titrated according to clinical response
• Hypertension: 25–100 mg per day orally; may increase up to 200 mg/day if necessary
• Primary hyperaldosteronism: 100–400 mg per day divided doses
• Heart failure: 12.5–50 mg once daily
• Prevention of hypokalemia: 25–100 mg per day

Pediatrics:

• Dosing individualized; commonly 1–3 mg/kg/day divided doses; use under specialist supervision

Elderly:

• Initiate at lower doses; monitor renal function and electrolytes due to increased risk of hyperkalemia

Special Populations:

• Renal impairment: Use with caution; avoid if severe renal dysfunction (eGFR <30 mL/min)
• Hepatic impairment: Use cautiously; monitor fluid and electrolyte status

Administration:

• Oral route, tablets taken with or without food
• Consistent daily timing recommended for steady blood levels

Spironolactone is a potassium-sparing diuretic and competitive antagonist of aldosterone at mineralocorticoid receptors in the distal convoluted tubules of the kidney. By blocking aldosterone, it reduces sodium and water reabsorption while promoting potassium and hydrogen ion retention, thus preventing hypokalemia and reducing fluid overload. Additionally, spironolactone exhibits antiandrogenic effects by antagonizing androgen receptors and inhibiting androgen biosynthesis, beneficial in conditions like hirsutism.

• Absorption: Well absorbed orally; peak plasma concentration occurs 2–4 hours post-dose
• Distribution: Approximately 90% bound to plasma proteins
• Metabolism: Extensively metabolized in the liver to active metabolites such as canrenone
• Elimination: Primarily renal excretion of metabolites; minor biliary elimination
• Half-life: Parent drug 1.3–1.5 hours; active metabolites have half-lives up to 16 hours
• Bioavailability: Variable due to first-pass hepatic metabolism

• Pregnancy: FDA Category C — Animal studies suggest potential risks; use only if benefits outweigh risks
• Lactation: Excreted in breast milk in low concentrations; potential antiandrogenic effects unknown; caution advised when administering to nursing mothers

• Potassium-sparing diuretic
• Aldosterone receptor antagonist
• Antiandrogen (off-label use)

• Known hypersensitivity to spironolactone or formulation excipients
• Hyperkalemia (serum potassium >5.5 mEq/L)
• Severe renal impairment or anuria
• Addison’s disease or other conditions with elevated potassium levels
• Acute renal insufficiency
• Concurrent use of potassium supplements or potassium-sparing diuretics without monitoring

• Risk of life-threatening hyperkalemia; monitor serum potassium regularly
• Use cautiously in patients with renal or hepatic impairment
• May cause endocrine side effects such as gynecomastia, breast tenderness, and menstrual irregularities
• Avoid use during pregnancy unless clearly necessary
• Monitor fluid status carefully in heart failure and cirrhosis patients
• Risk of hyponatremia and dehydration; monitor electrolytes during treatment

Common:

• Hyperkalemia
• Gynecomastia and breast tenderness
• Menstrual irregularities and amenorrhea
• Gastrointestinal disturbances (nausea, vomiting, diarrhea)
• Dizziness and headache

Rare/Serious:

• Rash, photosensitivity
• Hepatotoxicity (rare)
• Stevens-Johnson syndrome (very rare)
• Electrolyte imbalances including hyponatremia

• ACE inhibitors, ARBs, NSAIDs: Increased risk of hyperkalemia
• Potassium supplements, potassium-sparing diuretics: Additive hyperkalemia risk
• Lithium: Increased lithium toxicity potential
• Digoxin: Risk of digoxin toxicity due to electrolyte changes
• CYP3A4 inhibitors: May increase spironolactone plasma concentrations
• Other diuretics: May alter electrolyte balance, requiring monitoring

• Recommended by heart failure guidelines (AHA/ACC/ESC) as class IA therapy for HFrEF to improve survival and reduce hospitalizations
• Emphasis on frequent potassium monitoring due to risk of hyperkalemia, especially in patients on concomitant RAAS inhibitors
• Increasing clinical use in dermatology for androgen-related disorders, supported by recent studies
• Caution advised when combining with newer potassium-sparing agents and RAAS modulators

• Store at 20°C to 25°C (68°F to 77°F)
• Protect from moisture and light
• Keep tablets in original container tightly closed
• No refrigeration required
• Keep out of reach of children