Eplerenone (Inspra) is a selective aldosterone receptor antagonist, primarily indicated to improve survival in adult patients with heart failure symptoms following acute myocardial infarction, as well as to treat hypertension in adults.

What are the Precautions for Eplerenone (Inspra) Administration?

Strictly Adhere to Contraindications

For all patients: Serum potassium level > 5.5 mEq/L at the initiation of treatment; Creatinine clearance ≤ 30 mL/min; Concomitant use with potent CYP3A inhibitors (e.g., ketoconazole, itraconazole, clarithromycin, ritonavir, etc.).

Additional contraindications for hypertensive patients: Type 2 diabetes mellitus with microalbuminuria; Serum creatinine > 2.0 mg/dL in males or > 1.8 mg/dL in females; Creatinine clearance < 50 mL/min; Concomitant use with potassium supplements or potassium-sparing diuretics (e.g., amiloride, spironolactone, triamterene).

Administration in Special Populations

Elderly patients: Due to age-related decline in renal function, the risk of hyperkalemia is increased, requiring enhanced monitoring.

Pregnancy and lactation: Clinical data in pregnant women are limited; use only if the potential benefit outweighs the potential risk. The drug has been detected in the breast milk of lactating rats, while human data are lacking. Caution is recommended during lactation.

Men and women of childbearing potential: Animal studies have shown potential adverse effects on male fertility, and patients should be informed of the potential risks.

Pediatric patients: Efficacy in the treatment of hypertension has not been demonstrated in children. The safety and efficacy in pediatric patients with heart failure have not been established.

Pay Close Attention to Drug Interactions

CYP3A inhibitors: Concomitant use with potent CYP3A inhibitors is prohibited. When co-administered with moderate CYP3A inhibitors (e.g., verapamil, erythromycin, fluconazole), the daily dose should not exceed 25 mg in heart failure patients, and treatment should be initiated at a daily dose of 25 mg in hypertensive patients.

Concomitant use with ACEIs/ARBs: This combination increases the risk of hyperkalemia; close monitoring of serum potassium levels and renal function is required.

Concomitant use with non-steroidal anti-inflammatory drugs (NSAIDs): NSAIDs may attenuate the antihypertensive effect and induce hyperkalemia in patients with renal insufficiency. Blood pressure and serum potassium levels should be monitored.

Concomitant use with lithium preparations: This combination may increase the risk of lithium toxicity; frequent monitoring of serum lithium concentrations is required.

Monitoring for Eplerenone (Inspra) Administration

Pre-treatment Assessment

Measure serum potassium levels; 2. Evaluate renal function (serum creatinine, calculated creatinine clearance); 3. Confirm that the patient has no relevant contraindications.

Serum Potassium Monitoring

Recheck serum potassium levels within the first week after treatment initiation, one month later, and after each dose adjustment; 2. Conduct regular monitoring thereafter, especially in high-risk populations; 3. Adjust the dose based on serum potassium levels: Serum potassium < 5.0 mEq/L: Consider dose escalation; Serum potassium 5.0–5.4 mEq/L: Maintain the current dose; Serum potassium 5.5–5.9 mEq/L: Reduce the dose; Serum potassium ≥ 6.0 mEq/L: Discontinue administration temporarily; restart treatment at a lower dose after serum potassium levels return to < 5.5 mEq/L.

Renal Function Monitoring

Regularly test serum creatinine, especially when co-administered with drugs that may affect renal function; 2. If a patient starts treatment with moderate CYP3A inhibitors, ACEIs, ARBs or NSAIDs, recheck serum potassium and creatinine levels within 3–7 days.

Assessment of Blood Pressure and Clinical Response

For hypertensive patients, monitor blood pressure changes to evaluate treatment efficacy; 2. For heart failure patients, monitor symptoms, signs and overall clinical status.