Eplerenone

A to Z Drug Facts

 Action Binds to mineralocorticoid receptor, blocking the binding of aldosterone.

 Indications Treatment of hypertension.

 Contraindications Patients with serum potassium greater than 5.5 mEq/L, type 2 diabetes with microalbuminuria, serum creatinine greater than 2 mg/dL in men or greater than 1.8 mg/dL in women, Ccr less than 50 mL/min; patients treated concurrently with potassium supplements, potassium-sparing diuretics (eg, spironolactone), or strong inhibitors of CYP 3A4 (eg, ketoconazole).

 Route/Dosage

Adults: PO Initial dose 50 mg once daily. The full therapeutic effect is seen within 4 wk. Patients with an inadequate BP response to 50 mg once daily may be increased to 50 mg bid (max, 100 mg/day). Patients receiving weak CYP3A4 inhibitors (eg, saquinavir) start with 25 mg once daily.

 Interactions

ACE Inhibitors May increase the risk of hyperkalemia.

CYP3A4 inhibitors (eg, erythromycin, saquinavir, verapamil) Elevated plasma levels of eplerenone, increasing the risk of side effects.

St. John's wort Reduced plasma levels of eplerenone, decreasing the therapeutic effect.

 Adverse Reactions

CARDIOVASCULAR: Angina pectoris; MI. CNS: Headache; dizziness; fatigue. GI: Diarrhea; abdominal pain. GU: Albuminuria; mastodynia (males); abnormal vaginal bleeding; gynecomastia (males). METABOLIC: Hyponatremia; hypercholesterolemia; hypertriglyceridemia; increased BUN; increased uric acid; increase serum creatinine; increased ALT; hyperkalemia. RESPIRATORY: Coughing. OTHER: Flu-like symptoms.

 Precautions

Pregnancy Category B. Lactation Undetermined. Children Safety and efficacy not established. Hyperkalemia Hyperkalemia may occur.

 Administration/Storage

• Administer with or without food. Administer with food if GI upset occurs.
• Give 50 mg dose once daily. Give a 100 mg dose as 50 mg bid.
• Administer alone or in combination with other antihypertensives.
• Store tablets at controlled room temperature (59° to 86°F).

 Assessment/Interventions

• Obtain patient history, including drug history and any known allergies. Note concurrent use of ACE inhibitors, angiotensin II receptor antagonists, or weak CYP3A4 inhibitors (eg, fluconazole).
• Review patient's health history for any condition that could contraindicate eplerenone therapy: serum potassium greater than 5.5 mEq/L; type 2 diabetes with microalbuminuria; serum creatinine greater than 1.8 mg/dL in women or 2 mg/dL in men; Ccr less than 50 mL/min; concurrent use of potassium supplements, potassium-sparing diuretics, or strong inhibitors of CYP3A4 (eg, ketoconazole).
• Use reduced starting dose (eg, 25 mg) in patients receiving weak CYP3A4 inhibitors.
• Ensure that serum electrolytes are monitored periodically. Notify health care provider if serum potassium is noted to be greater than 5 mEq/L.
• Monitor and record BP and pulse. Should hypotension result, hold medication and notify health care provider.
• Take safety precautions if orthostatic hypotension occurs.

 Patient/Family Education

• Explain name, dose, action, and potential side effects of drug.
• Advise patient to take medication every day as prescribed, without regard to meals. Advise patient to take with food if GI upset occurs.
• Advise patient to try to take each dose at about the same time each day.
• Inform patient that drug controls but not does cure hypertension and to continue taking drug as prescribed even when BP is not elevated.
• Caution patient not to change the dose or stop taking unless advised to do so by health care provider.
• Instruct patient to continue taking other BP medications as prescribed by health care provider.
• Instruct patient in BP and pulse measurement skills.
• Advise patient to monitor and record BP and pulse at home and to inform health care provider should abnormal measurements be noted. Also advise patient to take record of BP and pulse to each follow-up visit.
• Instruct patient to lie or sit down if experiencing dizziness or lightheadedness when standing.
• Emphasize to hypertensive patients the importance of the following other modalities on BP: weight control, regular exercise, smoking cessation, and moderate intake of alcohol and salt.
• Instruct female patient to notify health care provider if pregnant, planning on becoming pregnant, or are breastfeeding.
• Caution patient to not take any prescription or OTC medications, salt substitutes, potassium supplements, or dietary supplements unless advised by health care provider.
• Advise patient that follow-up visits and lab tests may be required to monitor therapy and to keep appointments.

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Copyright © 2003 Facts and Comparisons
David S. Tatro
A to Z Drug Facts