eplerenone

Absorption: Well absorbed following oral administration.

Distribution: Unknown.

Metabolism/Excretion: Primarily metabolized by the liver via the CYP3A isoenzyme; <5% excreted unchanged by the kidneys.

Half-Life: 4–6 hr.

Time/Action Profile ⬆ ⬇

(antihypertensive effect)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	4 wk	unknown

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Serum potassium >5.5 mEq/L;
Type 2 diabetes with microalbuminuria (for patients with HTN; ↑ risk of hyperkalemia);
Serum creatinine >2 mg/dL in males or >1.8 mg/dL in females (for patients with HTN);
CCr ≤30 mL/min (for all patients); CCr <50 mL/min (for patients with HTN);
Concurrent use of potassium supplements or potassium-sparing diuretics (for patients with HTN);
Concurrent use of strong inhibitors of the CYP3A4 enzyme system;
Lactation: Lactation.

Use Cautiously in:

Moderate hepatic impairment;
OB: Use during pregnancy only if potential maternal benefit justifies potential fetal risk;
Pedi: Safety and effectiveness not established in children;
Geri: ↑risk of hyperkalemia in older adults due to age-related ↓ in renal function.

Adv. Reactions/Side Effects ⬆ ⬇

Endo: gynecomastia

F and E: HYPERKALEMIA

GI: ↑liver enzymes, abdominal pain, diarrhea

GU: abnormal vaginal bleeding, albuminuria

Metab: hypercholesterolemia, hypertriglyceridemia

Neuro: dizziness, fatigue

Misc: flu-like symptoms

Interactions ⬆ ⬇

Drug-drug:

Concurrent use of strong CYP3A inhibitors, including ketoconazole, itraconazole, nefazodone, clarithromycin, ritonavir, or nelfinavir may ↑ levels and risk of toxicity; concurrent use contraindicated.
Concurrent use of moderate CYP3A inhibitors, including erythromycin, fluconazole, or verapamil, may ↑ levels and risk of toxicity; ↓ eplerenone dose.
NSAIDs may ↓ antihypertensive effects.
Concurrent use of ACE inhibitors or angiotensin II receptor blockers may ↑ risk of hyperkalemia.

Route/Dosage ⬆ ⬇

Hypertension

PO (Adults ): 50 mg once daily initially; may ↑ to 50 mg twice daily; Concurrent use of moderate CYP3A4 inhibitors (erythromycin, verapamil, or fluconazole): 25 mg once daily initially; may ↑ to 25 mg twice daily.

Heart Failure with Reduced Ejection Fraction Post-Myocardial Infarction

PO (Adults ): 25 mg daily once initially; ↑ in 4 wk to 50 mg once daily; Concurrent use of moderate CYP3A4 inhibitors (erythromycin, verapamil, or fluconazole): Do not exceed 25 mg once daily.

Availability ⬆ ⬇

(Generic available)

Tablets: 25 mg; 50 mg

Assessment ⬆ ⬇

Monitor BP periodically during therapy.
Monitor prescription refills to determine adherence.

Lab Test Considerations:

May cause hyperkalemia. Monitor serum potassium levels prior to starting therapy, within the first wk, at 1 mo following start of therapy or dose adjustment, and periodically thereafter. Monitor serum potassium and serum creatinine in 3–7 days in patients who start taking a moderate CYP3A4 inhibitor.
- May cause ↓ serum sodium and ↑ serum triglyceride, cholesterol, ALT, GGT, creatinine, and uric acid levels.

Implementation ⬆ ⬇

Do not confuse Inspra with Spiriva.
PO: Administer once daily. May be increased to twice daily if response is inadequate.

Patient/Family Teaching ⬆ ⬇

Instruct patient to take medication as directed at the same time each day, even if feeling well.
Encourage patient to comply with additional interventions for HTN (weight reduction, discontinuation of smoking, moderation of alcohol consumption, regular exercise, stress management). Medication controls but does not cure HTN.
Instruct patient and family on correct technique for monitoring BP. Advise them to monitor BP at least weekly, and notify health care professional of significant changes.
Inform patient not to use potassium supplements, salt substitutes containing potassium, or other Rx, OTC, or herbal products without consulting health care professional.
May cause dizziness. Caution patient to avoid driving or other activities requiring alertness until response to medication is known.
Advise patient to notify health care professional if dizziness, diarrhea, vomiting, rapid or irregular heartbeat, lower extremity edema, or difficulty breathing occur.
Advise patient to inform health care professional of treatment regimen prior to treatment or surgery.
Rep: Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected. Advise patient to avoid breastfeeding during therapy. May impair male fertility.
Emphasize the importance of follow-up exams to check serum potassium.

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇