Eplerenone Tablets for Hypertension Treatment

Eplerenone is a film-coated tablet medication primarily used to treat hypertension (high blood pressure). By lowering blood pressure, it reduces the risk of serious cardiovascular events such as strokes and heart attacks. It works as an aldosterone antagonist that helps regulate salt and water balance to lower blood pressure.

Eplerenone Tablets are prescribed to treat hypertension in adults. Managing high blood pressure with eplerenone helps reduce the risk of fatal and nonfatal cardiovascular events like strokes and myocardial infarctions. Treatment is part of a broader cardiovascular risk management approach including lifestyle changes and possibly additional medications.

Eplerenone

Eplerenone selectively blocks mineralocorticoid receptors, preventing aldosterone—the hormone that increases blood pressure by promoting sodium retention—from binding. This blockade reduces sodium retention and lowers blood pressure. It acts on the body's renin-angiotensin-aldosterone system (RAAS) to achieve these effects without significant interaction with other steroid receptors.

Adults with Hypertension

• Start with 50 mg once daily.
• If blood pressure response is inadequate, increase to 50 mg twice daily.
• Do not exceed 100 mg total daily dose due to increased hyperkalemia risk without added benefit.

Patients Taking Moderate CYP3A Inhibitors

• Start at 25 mg once daily.
• If blood pressure response is inadequate, may increase up to 25 mg twice daily.

Monitoring

• Check serum potassium before starting therapy, within the first week, one month after initiation or dose adjustments, and periodically thereafter.
• Monitor serum potassium and creatinine within 3–7 days after starting moderate CYP3A inhibitors, angiotensin receptor blockers, or NSAIDs.

• Serum potassium >5.5 mEq/L at treatment initiation.
• Creatinine clearance ≤30 mL/min.
• Concomitant use of strong CYP3A inhibitors (ketoconazole, itraconazole, clarithromycin, ritonavir, etc.).
• For hypertension treatment: type 2 diabetes with microalbuminuria.
• Serum creatinine >2.0 mg/dL in males or >1.8 mg/dL in females.
• Creatinine clearance <50 mL/min in hypertensive patients.
• Use of potassium supplements or potassium-sparing diuretics (amiloride, spironolactone, triamterene) during hypertension treatment.

Hyperkalemia Risk

Eplerenone can increase potassium levels, especially in patients with impaired kidney function, diabetes, proteinuria, or those taking ARBs, NSAIDs, or moderate CYP3A inhibitors. Careful selection of patients and regular monitoring of serum potassium are essential. Patients developing mild hyperkalemia (5.5–5.9 mEq/L) may continue eplerenone with dose adjustments.

Contraindications

• Serum potassium >5.5 mEq/L at treatment start.
• Severe renal impairment (creatinine clearance ≤30 mL/min).
• Concurrent use with strong CYP3A inhibitors (e.g., ketoconazole, itraconazole, clarithromycin, ritonavir).
• For hypertension treatment: type 2 diabetes with microalbuminuria, high serum creatinine levels (males >2.0 mg/dL, females >1.8 mg/dL), creatinine clearance <50 mL/min, or use with potassium supplements or potassium-sparing diuretics.

Common Adverse Reactions

• Headache
• Dizziness
• Angina pectoris or myocardial infarction
• Increased gamma-glutamyl transferase (GGT)
• Gynecomastia (reported with longer use)
• Abnormal vaginal bleeding (reported with longer use)

Postmarketing

• Skin reactions: angioedema, rash

Hyperkalemia incidence increases with higher doses; potassium level increases were dose-related.

• CYP3A Inhibitors: Strong inhibitors are contraindicated. Moderate inhibitors require starting at reduced dose (25 mg once daily) with possible increase to 25 mg twice daily.
• Angiotensin Receptor Blockers (ARBs): Increase hyperkalemia risk; monitor potassium closely.
• Nonsteroidal Anti-Inflammatory Drugs (NSAIDs): May reduce antihypertensive effects and increase hyperkalemia risk; monitor blood pressure and potassium.
• Lithium: No formal studies; lithium toxicity reported with diuretics. Monitor lithium levels frequently if used together.
• Grapefruit Juice: Increases eplerenone exposure by about 25%.
• St. John's Wort: Decreases eplerenone exposure by about 30%.

No clinically significant interactions were seen with digoxin, simvastatin, warfarin, oral contraceptives, and several other listed drugs.

Pregnancy

Data on eplerenone use during pregnancy are insufficient to determine risk, but animal studies show no major teratogenic effects at high exposures. Hypertension during pregnancy poses risks to mother and fetus. Pregnant women using eplerenone should be closely monitored.

Lactation

It is unknown whether eplerenone is excreted in human milk. It is found in rat milk, so use with caution during breastfeeding.

Reports of human overdose are not available. Expected symptoms are hypotension and hyperkalemia. Eplerenone is not dialyzable. Treatment is supportive and includes standard measures to manage hyperkalemia.

Store at 25°C (77°F); permitted excursions are 15–30°C (59–86°F). Store tablets in their original blister pack and do not use if the blister is torn or broken.