Eplerenone

Eplerenone is a medicine known as a diuretic (water pill). It is mainly used in the treatment of heart failure and high blood pressure. It is also used to reduce swelling (oedema) caused by some other conditions.

Eplerenone can be taken with or without food, but you should take it in the same way each time to get the most benefit. Taking it with food can reduce some side effects and taking it early in the day can prevent you from having to get up at night to go to the toilet.

Eplerenone is a potassium-sparing diuretic. It lowers blood pressure and swelling by removing the extra water and electrolytes from the body without loss of potassium.

• Hypertension: May be used alone or in combination with other antihypertensive agents.
• Heart Failure: Used for congestive heart failure after an acute myocardial infarction.
• Edema: Used to reduce swelling caused by fluid retention.

Potassium-sparing diuretics & Aldosterone antagonists

Aldosterone Receptor Blocker (Potassium-sparing Diuretic)

Eplerenone is a blocker of aldosterone binding at the mineralocorticoid receptor. It binds to the mineralocorticoid receptor and blocks the binding of aldosterone, a component of the renin-angiotensin-aldosterone-system (RAAS). Aldosterone synthesis, which occurs primarily in the adrenal gland, is modulated by multiple factors, including angiotensin II and non-RAAS mediators such as adrenocorticotropic hormone and potassium.

Aldosterone binds to mineralocorticoid receptors in both epithelial (e.g. kidney, GI tract) and nonepithelial (e.g. heart, blood vessels, brain) tissues; causing increases in blood pressure by inducing sodium reabsorption, vascular remodeling, water retention and possibly other mechanisms. Eplerenone is a relatively selective mineralocorticoid receptor antagonist, blocking binding of aldosterone and reducing blood pressure.

Adult Dose:

• Hypertension: Initial 50 mg PO qDay; may increase to 50 mg PO q12hr. Full therapeutic response may take up to four weeks.
• Heart Failure Post MI: Initial 25 mg PO qDay; may titrate to maximum of 50 mg once daily within 4 weeks as tolerated.
• Hepatic Impairment: Dose adjustment not necessary.

Renal Dose: Contraindicated if CrCl <30 mL/min or serum creatinine >2 mg/dL (males) or >1.8 mg/dL (females).

Take this medicine in the dose and duration as advised by your doctor. Swallow it as a whole. Do not chew, crush or break it. Eplerenone may be taken with or without food, but it is better to take it at a fixed time.

If you miss a dose of Eplerenone, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular schedule. Do not double the dose.

Common Side Effects:

• Dizziness
• Diarrhea
• Nausea
• Cough
• Flu-like symptoms
• Fatigue
• Increased potassium level in blood
• Increased creatinine level in blood
• Abdominal pain
• Headache

Precautions:

• Eplerenone may decrease alertness, affect your vision or make you feel sleepy and dizzy. Do not drive if these symptoms occur.
• It can make you feel dizzy for the first few days. Do not drive or do anything requiring concentration until you know how it affects you.
• It may increase the level of potassium in your blood. Avoid taking potassium supplements and potassium-rich foods such as banana and broccoli.
• Your doctor will regularly check your kidney function and the amount of potassium in your blood.
• Notify your doctor if you experience dizziness, diarrhea, vomiting, fast or irregular heartbeat, swelling in feet, or difficulty breathing.
• Inform your doctor if you are pregnant, planning pregnancy or breastfeeding.

Contraindications:

• Serum potassium >5.5 mEq/L at initiation
• CrCl <30 mL/min
• Concomitant use of strong CYP3A4 inhibitors (ketoconazole, itraconazole, nefazodone, troleandomycin, clarithromycin, ritonavir, nelfinavir)
• Patients with type 2 DM with microalbuminuria (for hypertension patients)
• Serum creatinine >2 mg/dL (male) or >1.8 mg/dL (female)
• Concomitant use of potassium supplements or potassium-sparing diuretics

Drug Interactions:

• CYP3A4 Inhibitors (ketoconazole, voriconazole, itraconazole, fluconazole, clarithromycin, diltiazem, saquinavir, verapamil, ritonavir): May increase serum concentrations of Eplerenone.
• CYP3A4 Inducers (rifampicin, carbamazepine, phenytoin, phenobarbital): May decrease Eplerenone efficacy.
• ACE inhibitors, ARBs, potassium-sparing diuretics: May enhance hyperkalaemic effect.
• NSAIDs: May reduce antihypertensive and/or diuretic effects and increase risk of hyperkalaemia.
• Lithium: Toxicity reported when used with ACE inhibitors or diuretics.

Food Interactions: Eplerenone may cause excessive drowsiness with alcohol. Avoid alcohol.

Use in Pregnancy: Eplerenone is generally considered safe to use during pregnancy. Animal studies have shown low or no adverse effects to the developing baby; however, there are limited human studies. Should be used only if clearly needed.

Use in Lactation: Information regarding the use of Eplerenone during breastfeeding is not available. Consult your doctor.

Pediatric Use: Safety and effectiveness in pediatric patients have not been established.

Geriatric Use: No differences in overall incidence of effectivity or safety was observed in elderly patients.

Renal Impairment: Use with caution. Dose adjustment may be needed. Not recommended in patients with severe kidney disease.

Hepatic Impairment: Use with caution. Dose adjustment may be needed. Not recommended in patients with severe liver disease due to limited data.

Overdose: Overdose may cause electrolyte imbalance, hyperkalemia, nausea, dizziness. In case of overdose, seek immediate medical attention and symptomatic treatment.

Storage: Store below 30°C in a cool and dry place, protected from light and moisture. Keep out of children's reach.

Eplerenone