eplerenone (e-ple-re-none) Inspra

 Indications

Hypertension (alone, or with other agents). LV systolic

dysfunction and evidence of HF post-MI.

Action

Blocks the effects of aldosterone by attaching to mineralocorticoid

receptors. Therapeutic Effects: Lowering

of BP. Improves survival in patients with evidence

of HF post-MI.

Pharmacokinetics

Absorption: Well absorbed following oral administration.

Distribution: Unknown.

Metabolism and Excretion: Mostly metabolized

by the liver (CYP3A enzyme system); 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

Contraindications/Precautions

Contraindicated in: Serum potassium 5.5 mEq/

L; Type 2 diabetes with microalbuminuria (for patients

with HTN;qrisk 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;

Geri:qrisk of hyperkalemia due to age-relatedpin renal

function; OB: Use only if clearly needed; Pedi: Safety

not established.

Adverse Reactions/Side Effects

CNS: dizziness, fatigue. GI: abnormal liver function

tests, abdominal pain, diarrhea. GU: albuminuria.

Endo: abnormal vaginal bleeding, gynecomastia. F

and E: HYPERKALEMIA.Metab: hypercholesterolemia,

hypertriglyceridemia. Misc: flu-like symptoms.

Interactions

Drug-Drug: Concurrent use of strong CYP3A inhibitors,

including ketoconazole, itraconazole, nefazodone,

clarithromycin, ritonavir, or nelfinavir significantlyqeffects

of eplerenone; concurrent use

contraindicated. Concurrent use of moderate CYP3A inhibitors,

including erythromycin, saquinavir, fluconazole,

or verapamil mayqlevels;pdose of eplerenone.

NSAIDs maypantihypertensive effects.

Concurrent use of ACE inhibitors or Angiotensin II

receptor blockers mayqrisk of hyperkalemia.

Route/Dosage

Hypertension

PO (Adults): 50 mg daily initially; may beqto 50 mg

twice daily; Patients receiving concurrent moderate

CYP3A4 inhibitors (erythromycin, saquinavir, verapamil,

fluconazole)—25 mg once daily initially; may

beqto 25 mg twice daily . 

HF Post-MI

PO (Adults): 25 mg daily initially;qin 4 wk to 50 mg

daily; Patients receiving concurrent moderate

CYP3A4 inhibitors (erythromycin, saquinavir, verapamil,

fluconazole)—Do not exceed 25 mg daily.

Availability (generic available)

Tablets: 25 mg, 50 mg.