Eplerenone

DEA Class; Rx

Common Brand Names; Inspra

Selective aldosterone receptor antagonist (SARA)
Used to treat hypertension; also used to treat heart failure in post-myocardial infarction patients
Metabolized by CYP3A4; associated with a risk of hyperkalemia

Indicated for the treatment of hypertension, either as monotherapy or in combination with other antihypertensive agents.

Hypersensitivity

For all patients: Serum potassium >5.5 mEq/L at initiation Creatinine clearance ≤30 mL/min Concomitant use with strong CYP3A inhibitors For the treatment of hypertension: Type 2 diabetes with microalbuminuria Serum creatinine >2.0 mg/dL in males, >1.8 mg/dL in females Creatinine clearance <50 mL/min Concomitant use of potassium supplements or potassium-sparing diuretics

• Hyperkalemia (2-10%)
• Increased risk of hyperkalemia with presence of renal dysfunction
• Dizziness
• Fatigue/malaise
• Abdominal pain
• Diarrhea
• Albuminuria
• Hypercholesterolemia
• Hypertriglyceridemia
• Cough
• Abnormal vaginal bleeding
• Gynecomastia
• Mastodynia

Hyperkalemia, liver dysfunction, metabolic or respiratory acidosis, renal impairment, hypersensitivity to spironolactone

The risk of hyperkalemia is higher in patients with impaired renal function, proteinuria , diabetes and those concomitantly treated with ACEs, ARBs, NSAIDs and moderate CYP3A inhibitors

Patients taking moderate CYP3A inhibitors that cannot be avoided should have their dose of eplerenone reduced

Available data from published case reports on eplerenone use during pregnancy are insufficient to establish a drug-associated risk of major birth defects, miscarriage, adverse maternal or fetal outcomes

There are no human data available on whether eplerenone is present in human milk, or has effects on breastfed infants or on milk production; eplerenone was present in milk of lactating rats; when a drug is present in animal milk, it is likely that the drug will be present in human milk