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Eplerenone

Pronunciation: (eh-PLER-en-ohn)
Class: Selective aldosterone receptor antagonists

Trade Names:
Inspra
- Tablets 25 mg
- Tablets 50 mg

Pharmacology

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Binds to mineralocorticoid receptor, blocking the binding of aldosterone.

Pharmacokinetics

Absorption

T _max is 1.5 h.

Distribution

Approximately 50% is protein bound (primarily to alpha 1-acid glycoprotein). The Vd is 43 to 90 L (at steady state).

Metabolism

Metabolized by CYP3A4; no active metabolites formed.

Elimination

The elimination t _½ is approximately 4 to 6 h. Approximately 32% is excreted in feces and approximately 67% is excreted in urine. Less than 5% is excreted as unchanged drug. The plasma Cl is approximately 10 L/h.

Special Populations

Renal Function Impairment

AUC and C _max increased 38% and 24%, respectively, in those with severe renal function impairment.

Hepatic Function Impairment

C _max and AUC increased 3.6% and 42%, respectively, in those with moderate hepatic function impairment.

Elderly

C _max increased 22% and AUC increased 45%.

Race

C _max decreased 19% and AUC decreased 26% in black patients.

Indications and Usage

Treatment of hypertension; improve survival of stable patients with left ventricular systolic dysfunction and clinical evidence of CHF after an acute MI.

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 30 mL/min or less, patients treated concurrently with potassium supplements, potassium-sparing diuretics (eg, spironolactone), or strong inhibitors of CYP3A4 (eg, ketoconazole).

Dosage and Administration

CHF Post-MI
Adults

PO Start with 25 mg every day and titrate to target dose of 50 mg every day within 4 wk as tolerated by the patient.

Dosage Adjustment in CHF
Adults

PO If serum potassium is less than 5 mEq/L, increase dose from 25 mg every day to 50 mg every day; if potassium levels are between 5 and 5.4 mEq/L, maintain dose; if potassium levels are between 5.5 and 5.9 mEq/L, decrease dose from 50 mg every day to 25 mg every day, or 25 mg every day to 25 mg every other day, or 25 mg every other day to withhold; if potassium levels are 6 mEq/L or greater, withhold the dose. When potassium levels have fallen below 5.5 mEq/L, restart dose at 25 mg every other day.

Hypertension
Adults

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

General Advice

Administer with or without food. Administer with food if GI upset occurs.

Storage/Stability

Store tablets at controlled room temperature (59° to 86°F).

Drug Interactions

ACE inhibitors and angiotensin II receptor antagonists

May increase the risk of hyperkalemia.

CYP3A4 inhibitors (eg, clarithromycin, nefazodone, ritonavir)

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.

Genitourinary

Albuminuria; abnormal vaginal bleeding; mastodynia, gynecomastia (men).

Metabolic

Hyponatremia; hypercholesterolemia; hypertriglyceridemia; increased BUN; increased uric acid; increase serum creatinine; increased ALT; hyperkalemia.

Respiratory

Coughing.

Miscellaneous

Flu-like symptoms.

Precautions

Pregnancy

Category B .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Hyperkalemia

Hyperkalemia may occur. Risk can be minimized by patient selection, avoidance of certain drugs, and monitoring. Ensure that serum potassium is determined before starting therapy, within the first week, and at 1 mo after the start of therapy or dose adjustment. Periodically assess serum potassium thereafter.

Overdosage

Symptoms

Hypotension, hyperkalemia.

Patient Information

Advise patient to take 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 does not cure hypertension and to continue taking it as prescribed even when BP is not elevated.
Caution patient not to change the dose or stop taking unless advised 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 patient importance of the following other modalities on BP: weight control, regular exercise, smoking cessation, moderate intake of alcohol and salt.
Caution patient not to take any prescription or OTC medications, salt substitutes, potassium supplements, or dietary supplements unless advised by health care provider.