e-PLE-re-none

• Hypertension (alone, or with other agents).
• LV systolic dysfunction and evidence of HF post-MI.

• Blocks the effects of aldosterone by attaching to mineralocorticoid receptors.

• Lowering of BP.
• Improves survival in patients with evidence of HF post-MI.

Absorption: Well absorbed following oral administration.

Distribution: Unknown.

Metabolism/Excretion: Mostly metabolized by the liver (CYP3A enzyme system); <5% excreted unchanged by the kidneys.

Half-life: 4–6 hr.

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 (ketoconazole, itraconazole, nefazodone, clarithromycin, ritonavir, or nelfinavir)
• Lactation: Lactation.

Use Cautiously in:

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

Endo: abnormal vaginal bleeding, gynecomastia.

F and E: HYPERKALEMIA.

GI: abnormal liver function tests, abdominal pain, diarrhea.

GU: albuminuria.

Metab: hypercholesterolemia, hypertriglyceridemia.

Neuro: dizziness, fatigue.

Misc: flu-like symptoms.

Drug-Drug:

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

Hypertension

• PO (Adults): 50 mg once daily initially; may be ↑ to 50 mg twice daily; Patients receiving concurrent moderate CYP3A4 inhibitors (erythromycin, saquinavir, verapamil, fluconazole) — 25 mg once daily initially; may be ↑ to 25 mg twice daily.

HF Post-MI

• PO (Adults): 25 mg daily once initially; ↑ in 4 wk to 50 mg once daily; Patients receiving concurrent moderate CYP3A4 inhibitors (erythromycin, saquinavir, verapamil, fluconazole) — Do not exceed 25 mg once daily.

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

Inspra

Therapeutic Classification: antihypertensives

Pharmacologic Classification: aldosterone antagonists

(Generic available)

• Tablets: 25 mg; 50 mg;

(antihypertensive effect)

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

• 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.

• Decreased cardiac output (Indications).
• Noncompliance (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 hypertension (weight reduction, discontinuation of smoking, moderation of alcohol consumption, regular exercise, stress management). Medication controls, but does not cure, hypertension.
• 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.
• Advise patient to notify health care professional if pregnancy is planned or suspected. Advise patient to avoid breast feeding during therapy.
• Emphasize the importance of follow-up exams to check serum potassium.

• Decrease in BP without appearance of side effects.
• Improvement in survival in patients with evidence of HF post-MI.

NDC Code^*

• 0025- G.D. Searle LLC Division of Pfizer Inc
  • 0025-1710- Inspra
    • 0025-1710-01- 30 TABLET, FILM COATED in 1 BOTTLE (0025-1710-01)

• 0025- G.D. Searle LLC Division of Pfizer Inc
  • 0025-1710- Inspra
    • 0025-1710-02- 90 TABLET, FILM COATED in 1 BOTTLE (0025-1710-02)

• 0025- G.D. Searle LLC Division of Pfizer Inc
  • 0025-1710- Inspra
    • 0025-1710-03- 100 BLISTER PACK in 1 BOX, UNIT-DOSE (0025-1710-03) > 1 TABLET, FILM COATED in 1 BLISTER PACK

• 0025- G.D. Searle LLC Division of Pfizer Inc
  • 0025-17,20- Inspra
    • 0025-17,20-01- 90 TABLET, FILM COATED in 1 BOTTLE (0025-17,20-01)

• 0025- G.D. Searle LLC Division of Pfizer Inc
  • 0025-17,20- Inspra
    • 0025-17,20-03- 30 TABLET, FILM COATED in 1 BOTTLE (0025-17,20-03)

• 0185- Eon Labs, Inc.
  • 0185-5368- Eplerenone
    • 0185-5368-09- 90 TABLET in 1 BOTTLE (0185-5368-09)

• 0185- Eon Labs, Inc.
  • 0185-5368- Eplerenone
    • 0185-5368-30- 30 TABLET in 1 BOTTLE (0185-5368-30)

• 0185- Eon Labs, Inc.
  • 0185-5369- Eplerenone
    • 0185-5369-09- 90 TABLET in 1 BOTTLE (0185-5369-09)

• 0185- Eon Labs, Inc.
  • 0185-5369- Eplerenone
    • 0185-5369-30- 30 TABLET in 1 BOTTLE (0185-5369-30)

• 0378- Mylan Pharmaceuticals Inc.
  • 0378-1030- Eplerenone
    • 0378-1030-77- 90 TABLET, FILM COATED in 1 BOTTLE, PLASTIC (0378-1030-77)

• 0378- Mylan Pharmaceuticals Inc.
  • 0378-1030- Eplerenone
    • 0378-1030-93- 30 TABLET, FILM COATED in 1 BOTTLE, PLASTIC (0378-1030-93)

• 0378- Mylan Pharmaceuticals Inc.
  • 0378-1031- Eplerenone
    • 0378-1031-77- 90 TABLET, FILM COATED in 1 BOTTLE, PLASTIC (0378-1031-77)

• 0378- Mylan Pharmaceuticals Inc.
  • 0378-1031- Eplerenone
    • 0378-1031-93- 30 TABLET, FILM COATED in 1 BOTTLE, PLASTIC (0378-1031-93)

• 0832- Upsher-Smith Laboratories, LLC
  • 0832-0480- Eplerenone
    • 0832-0480-30- 30 TABLET in 1 BOTTLE (0832-0480-30)

• 0832- Upsher-Smith Laboratories, LLC
  • 0832-0480- Eplerenone
    • 0832-0480-90- 90 TABLET in 1 BOTTLE (0832-0480-90)

• 0832- Upsher-Smith Laboratories, LLC
  • 0832-0481- Eplerenone
    • 0832-0481-30- 30 TABLET in 1 BOTTLE (0832-0481-30)

• 0832- Upsher-Smith Laboratories, LLC
  • 0832-0481- Eplerenone
    • 0832-0481-90- 90 TABLET in 1 BOTTLE (0832-0481-90)

• 16729- Accord Healthcare, Inc.
  • 16729-293- Eplerenone
    • 16729-293-10- 30 TABLET, FILM COATED in 1 BOTTLE (16729-293-10)

• 16729- Accord Healthcare, Inc.
  • 16729-293- Eplerenone
    • 16729-293-15- 90 TABLET, FILM COATED in 1 BOTTLE (16729-293-15)

• 16729- Accord Healthcare, Inc.
  • 16729-294- Eplerenone
    • 16729-294-10- 30 TABLET, FILM COATED in 1 BOTTLE (16729-294-10)

• 16729- Accord Healthcare, Inc.
  • 16729-294- Eplerenone
    • 16729-294-15- 90 TABLET, FILM COATED in 1 BOTTLE (16729-294-15)

• 51991- Breckenridge Pharmaceutical, Inc.
  • 51991-877- EPLERENONE
    • 51991-877-11- 10 BLISTER PACK in 1 CARTON (51991-877-11) > 10 TABLET, FILM COATED in 1 BLISTER PACK (51991-877-99)

• 51991- Breckenridge Pharmaceutical, Inc.
  • 51991-877- EPLERENONE
    • 51991-877-33- 30 TABLET, FILM COATED in 1 BOTTLE (51991-877-33)

• 51991- Breckenridge Pharmaceutical, Inc.
  • 51991-877- EPLERENONE
    • 51991-877-90- 90 TABLET, FILM COATED in 1 BOTTLE (51991-877-90)

• 51991- Breckenridge Pharmaceutical, Inc.
  • 51991-878- EPLERENONE
    • 51991-878-11- 10 BLISTER PACK in 1 CARTON (51991-878-11) > 10 TABLET, FILM COATED in 1 BLISTER PACK (51991-878-99)

• 51991- Breckenridge Pharmaceutical, Inc.
  • 51991-878- EPLERENONE
    • 51991-878-33- 30 TABLET, FILM COATED in 1 BOTTLE (51991-878-33)

• 51991- Breckenridge Pharmaceutical, Inc.
  • 51991-878- EPLERENONE
    • 51991-878-90- 90 TABLET, FILM COATED in 1 BOTTLE (51991-878-90)

• 59762- Greenstone LLC
  • 59762-1710- Eplerenone
    • 59762-1710-1- 100 BLISTER PACK in 1 CARTON (59762-1710-1) > 1 TABLET, FILM COATED in 1 BLISTER PACK

• 59762- Greenstone LLC
  • 59762-1710- Eplerenone
    • 59762-1710-2- 30 TABLET, FILM COATED in 1 BOTTLE (59762-1710-2)

• 59762- Greenstone LLC
  • 59762-1710- Eplerenone
    • 59762-1710-3- 90 TABLET, FILM COATED in 1 BOTTLE (59762-1710-3)

• 59762- Greenstone LLC
  • 59762-17,20- Eplerenone
    • 59762-17,20-1- 30 TABLET, FILM COATED in 1 BOTTLE (59762-17,20-1)

• 59762- Greenstone LLC
  • 59762-17,20- Eplerenone
    • 59762-17,20-2- 90 TABLET, FILM COATED in 1 BOTTLE (59762-17,20-2)

• 60687- American Health Packaging
  • 60687-451- EPLERENONE
    • 60687-451-21- 30 BLISTER PACK in 1 BOX, UNIT-DOSE (60687-451-21) > 1 TABLET, FILM COATED in 1 BLISTER PACK (60687-451-11)

• 68084- American Health Packaging
  • 68084-948- Eplerenone
    • 68084-948-25- 30 BLISTER PACK in 1 BOX, UNIT-DOSE (68084-948-25) > 1 TABLET in 1 BLISTER PACK (68084-948-95)