Eplerenone Inspra

Eplerenone is an aldosterone receptor blocker, which is an antihypertensive, used to treat congestive heart failure after a heart attack, and is also used to treat high blood pressure (hypertension).

Eplerenone is available under the following different brand names: Inspra.

Dosage Forms and Strengths

Tablet

• 25 mg
• 50 mg

Dosage Considerations – Should be Given as Follows:

Hypertension (HTN)

• Adult and geriatric: Initial 50 mg orally once/day; may increase to 50 mg orally every 12 hours; may take up to four weeks for full therapeutic response; high blood potassium (hyperkalemia) may occur with doses greater than 100 mg/day

Heart Failure Post Myocardial Infarction (MI)

• Adult and geriatric: Initial 25 mg orally once/day; may titrate to maximum of 50 mg once daily within 4 weeks as tolerated
• Dose adjustments may be required based on potassium levels

Renal Impairment

• Contraindicated if CrCl less than 50 mL/min or serum creatinine greater than 2 mg/dL in males or greater than 1.8 mg/dL in females

Hepatic Impairment

• Dose adjustment not necessary

Dosing considerations

• In heart attack (myocardial infarction [MI]) congestive heart failure (CHF) patients taking a moderate CYP3A inhibitor, do not exceed 25 mg once daily; in patients with hypertension taking a moderate CYP3A inhibitor, initiate at 25 mg once daily; for inadequate blood pressure response, dosing may be increased to a maximum of 25 mg twice daily
• Pediatric: Safety and efficacy not established

Other Indications and Uses

• Improving survival of stable patients with LV systolic dysfunction (LVEF up to 40%) and congestive heart failure (CHF) after an acute heart attack (myocardial infarction [MI])

Common side effects of eplerenone Inspra include:

• High blood potassium (hyperkalemia)
• Increased risk of hyperkalemia with presence of renal dysfunction
• Dizziness
• Fatigue/malaise
• Abdominal/stomach pain
• Diarrhea
• Albuminuria
• High cholesterol
• High triglycerides
• Cough
• Headache
• Nausea
• Flu-like symptoms (such as fever, chills, body aches, unusual tiredness)
• Vaginal bleeding
• Breast swelling or tenderness

Serious side effects of eplerenone Inspra include:

• Abnormal vaginal bleeding
• Enlarged or sore breasts in males
• Symptoms of a high potassium blood level (such as muscle weakness, slow/irregular heartbeat)

This document does not contain all possible side effects and others may occur. Check with your physician for additional information about side effects.

If your doctor has directed you to use this medication, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider or pharmacist first.

• Severe interactions of eplerenone Inspra include:
  • itraconazole
  • nefazodone
  • saquinavir
• Serious interactions of eplerenone Inspra include:
  • amiloride
  • drospirenone
  • idelalisib
  • isoniazid
  • ivacaftor
  • ketoconazole
  • potassium acid phosphate
  • potassium chloride
  • potassium phosphates, IV
  • spironolactone
  • triamterene
• Eplerenone has moderate interactions with at least 52 different drugs.
• Eplerenone has mild interactions with at least 115 different drugs.

This information does not contain all possible interactions or adverse effects. Therefore, before using this product, tell your doctor or pharmacist of all the products you use. Keep a list of all your medications with you, and share this information with your doctor and pharmacist. Check with your health care professional or doctor for additional medical advice, or if you have health questions, concerns or for more information about this medicine.

Warnings

This medication contains eplerenone. Do not take Inspra if you are allergic to eplerenone or any ingredients contained in this drug.

Keep out of reach of children. In case of overdose, get medical help or contact a Poison Control Center immediately.

Contraindications

• Hypersensitivity
• For all patients
  • Serum potassium greater than 5.5 mEq/L at initiation
  • Creatinine clearance up to 30 mL/minute
  • Concomitant use with strong CYP3A inhibitors
• For the treatment of hypertension
  • Type 2 diabetes with microalbuminuria
  • Serum creatinine greater than 2.0 mg/dL in males, greater than 1.8 mg/dL in females
  • Creatinine clearance less than 50 mL/minute
  • Concomitant use of potassium supplements or potassium-sparing diuretics

Effects of Drug Abuse

• None

Short-Term Effects

• See "What Are Side Effects Associated with Using Eplerenone Inspra?"

Long-Term Effects

• See "What Are Side Effects Associated with Using Eplerenone Inspra?"

Cautions

• High blood potassium (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 angiotensin-converting-enzyme inhibitors (ACEs), angiotensin receptor blockers (ARBs), nonsteroidal anti-inflammatory drugs (NSAIDs) and moderate CYP3A inhibitors.
• Patients taking moderate CYP3A inhibitors that cannot be avoided should have their dose of eplerenone reduced.

Pregnancy and Lactation

• Eplerenone use during pregnancy may be acceptable. Either animal studies show no risk but human studies are not available or animal studies showed minor risks and human studies were done and showed no risk.
• It is unknown if eplerenone is excreted into breast milk; discontinue the drug or nursing.