Alderon®

Heart failure:

When initiating therapy for any of the heart failure indications below, verify the following: serum potassium <5 mEq/L and either serum creatinine ≤2.5 mg/dL in men and ≤2 mg/dL in women or eGFR >30 mL/minute/1.73 m2. If patient develops hyperkalemia (serum potassium >5.5 mEq/L), reduce the dose, change to every-other-day dosing, or discontinue therapy. If renal function worsens, consider dose reduction or discontinuation

Oral: Initial: 25 mg once daily; may double the dose after 4 weeks if serum potassium remains <5 mEq/L and renal function is stable, to a maximum target dose of 50 mg once daily. Some experts recommend up-titrating therapy only if serum potassium is ≤4.5 mEq/L

Post myocardial infarction, complicated by reduced ejection fraction:

Note: Should be considered for use following acute myocardial infarction in patients with left ventricular ejection fraction ≤40% plus symptoms of heart failure or diabetes. Use in addition to other pharmacologic therapies.

Oral: Initial: 25 mg once daily; may double the dose after 4 weeks if serum potassium remains <5 mEq/L and renal function is stable, up to a maximum target dose of 50 mg once daily.

Hypertension, chronic:

Note: Not recommended for initial management but may be considered as additional therapy for resistant hypertension in patients who do not respond adequately to combination therapy with preferred agents.

Oral: Initial: 50 mg once daily; evaluate response after ~2 to 4 weeks and titrate dose, as needed, to a maximum of 50 mg twice daily. Twice daily dosing is usually required for adequate BP lowering. Patients with severe asymptomatic hypertension and no signs of acute end organ damage should be evaluated for medication titration within 1 week.

Contraindications:

Serum potassium >5.5 mEq/L at initiation; CrCl ≤30 mL/minute; concomitant use of strong CYP3A4 inhibitors (eg, ketoconazole, itraconazole, nefazodone, troleandomycin, clarithromycin, ritonavir, nelfinavir).

The following additional contraindications apply to patients with hypertension: Type 2 diabetes mellitus (noninsulin dependent, NIDDM) with microalbuminuria; serum creatinine >2.0 mg/dL in males or >1.8 mg/dL in females; CrCl <50 mL/minute; concomitant use with potassium supplements or potassium-sparing diuretics (eg, amiloride, spironolactone, triamterene).

Per the Endocrine Society clinical practice guidelines, use in patients with Addison disease is contraindicated

Interactions:

Angiotensin II Receptor Blockers: Eplerenone may enhance the hyperkalemic effect of Angiotensin II Receptor Blockers. Risk C: Monitor therapy

Angiotensin-Converting Enzyme Inhibitors: Eplerenone may enhance the hyperkalemic effect of Angiotensin-Converting Enzyme Inhibitors. Risk C: Monitor therapy

Antipsychotic Agents (Second Generation [Atypical]): Blood Pressure Lowering Agents may enhance the hypotensive effect of Antipsychotic Agents (Second Generation [Atypical]). Risk C: Monitor therapy

Barbiturates: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy

Pregnancy and Lactation:

Chronic maternal hypertension is associated with adverse events in the fetus/infant. The risk of birth defects, low birth weight, premature delivery, stillbirth, and neonatal death may be increased with chronic hypertension in pregnancy. Actual risks may be related to duration and severity of maternal hypertension. The use of mineralocorticoid receptor antagonists for the treatment of hypertension in pregnancy is generally not recommended

It is not known if eplerenone is present in breast milk.

Warning and Precaution:

• Diabetes: Use with caution in patients with heart failure post-myocardial infarction with diabetes (especially if patient has proteinuria); risk of hyperkalemia is increased.
• Heart failure: When evaluating a heart failure patient for eplerenone treatment, eGFR should be >30 mL/minute/1.73 m2 or creatinine should be ≤2.5 mg/dL (men) or ≤2 mg/dL (women) with no recent worsening and potassium <5 mEq/L with no history of severe hyperkalemia. Serum potassium levels require close monitoring and management if elevated. The American College of Cardiology Foundation/American Heart Association recommends considering discontinuation upon the development of serum potassium >5.5 mEq/L or worsening renal function with careful evaluation of the entire medical regimen. Avoid triple therapy with the combined use of an ACE inhibitor, ARB, and eplerenone. Therapy may need to be modified during an episode of diarrhea or dehydration or when loop diuretic therapy is interrupted.
• Hepatic impairment: Use with caution in patients with moderate to severe hepatic impairment.
• Renal impairment: Risk of hyperkalemia is increased with declining renal function. Use with caution in patients with mild renal impairment; based on indication and degree of impairment use may be contraindicated (refer to contraindications field).

Adverse Reactions:

Hyperkalemia, hypertriglyceridemia, Dizziness, fatigue, Hyponatremia, Diarrhea, abdominal pain, abnormal vaginal hemorrhage

Storage:

Store below 30 and protect from light and moisture.