Eplerenone

Indications
 Oral
Congestive Heart Failure Post-Myocardial Infarction
Adult: Initial: 25 mg once daily; titrate to recommended dose of 50 mg once daily within 4 wk as tolerated. Dose adjustment based on serum potassium level (SPK); <5 meq/L: Increase 25 mg every other day to 25 mg once daily; or 25 mg once daily to 50 mg once daily. SPK 5-5.4 mEq/L: No dosage adjustment. SPK 5.5-5.9 mEq/L: Decrease from 50 mg once daily to 25 mg once daily; or from 25 mg once daily to 25 mg every other day; or 25 mg every other day to withhold therapy. SPK ≥6 mEq/L: Withhold therapy; to restart dose at 25 mg every other day when potassium levels fall to <5.5 mEq/L.
Oral
Hypertension
Adult: May be used alone or in combination with other antihypertensives. Initial: 50 mg once daily. May increase to 50 mg bid based on response; full antihypertensive effect usually occur within 4 wk. Doses >100mg/day have no greater benefit and associated with increased risk of hyperkalaemia. If used concurrently with moderate CYP3A4 inhibitors (e.g. verapamil, erythromycin, saquinavir, fluconazole): Initial: 25 mg once daily.
Contraindications
 For all patients: Serum potassium >5.5 mEq/L at initiation; CrCl ≤30 mL/min; concomitant use of strong CYP3A4 inhibitors (e.g. ketoconazole, itraconazole, nefazodone, troleandomycin, clarithromycin, ritonavir, nelfinavir). For patients treated for hypertension: Patients with type 2 DM with microalbuminuria; serum creatinine >2 mg/dL (male), or >1.8 mg/dL (female); CrCl <50 mL/min; concomitant use of potassium supplements or potassium-sparing diuretics (e.g. amiloride, spironolactone, or triamterene).
Warnings / Precautions
 Measure serum potassium levels before starting therapy, within the first wk, and periodically thereafter. Increased risk of hyperkalaemia in patients with impaired renal functions; diabetic patients with CHF post-MI (especially those with proteinuria); or concurrent use of agents affecting the rennin-angiotensin-aldosterone system. Safety and efficacy not established in patients with severe hepatic impairment; or paediatric patients <18 yr. Elderly. Pregnancy and lactation.
Adverse Reactions
 Hyperkalaemia, hyponatraemia, dizziness, headache, abdominal pain, diarrhoea, cough, fatigue, influenza-like symptoms, abnormal vaginal bleeding, gynaecomastia, mastodynia, myocardial infarction, angina pectoris, hypercholesterolaemia, hypertriglyceridaemia, albuminuria, increased creatinine, elevated liver enzymes, increased uric acid, rash and angioneurotic oedema.
Overdose Reactions
 Most likely symptoms of human overdosage: Hypotension or hyperkalaemia; provide supportive treatment and monitoring. Eplerenone is non-dialysable; binds extensively to charcoal.
Drug Interactions
 Concomitant use with CYP3A4 Inhibitors (e.g. ketoconazole, voriconazole, itraconazole, fluconazole, clarithromycin, diltiazem saquinavir, verpamil, ritonavir) may increase serum concentrations of Eplerenone. CYP3A4 inducers (e.g. rifampicin, carbamazepine, phenytoin, phenobarbital) may decrease Eplerenone efficacy. Eplerenone may enhance hyperkalaemic effect of ACE inhibitors, angiotensin II receptor blockers, potassium-sparing diuretics or potassium salts. Concomitant use with diazoxide, MAOIs, pentoxifylline, prostacyclin analogues may enhance hypotensive effect of antihypertensives. NSAIDs may possibly reduce the antihypertensive and/or diuretic effects of potassium-sparing diuretics and may increase risk of hyperkalaemia. Lithium toxicity has been reported when used with ACE inhibitors or diuretics; monitor lithium levels when used with Eplerenone.
See Below for More eplerenone Drug Interactions
Food Interactions
 Avoid grapefruit juice as it may increase serum levels of Eplerenone. St. Johns wort may decrease serum levels of Eplerenone.
Mechanism of Actions
 Aldosterone binds to mineralocorticoid receptors in both epithelial (e.g. kidney, GI tract) and nonepithelial (e.g. heart, blood vessels, brain) tissues; causing increases in blood pressure by inducing sodium reabsorption, vascular remodeling, water retention and possibly other mechanisms. Eplerenone is a relatively selective mineralocorticoid receptor antagonist, blocking binding of aldosterone and reducing blood pressure. Eplerenone also appears to have cardioprotective effect in patients with congestive heart failure (CHF) after myocardial infarction (MI).
Absorption: Absolute bioavailability: About 69%. Mean Tmax: Approx 1.5 hr.
Distribution: Protein binding: About 50% (mainly to α1-acid glycoproteins). Vd: About 43-90 L.
Metabolism: Hepatic metabolism mainly via CYP3A4 to inactive metabolites.
Excretion: About 67% is excreted in urine and 32% in faeces following a single oral dose. <5% is excreted unchanged in urine and faeces. Elimination half-life: About 4-6 hr. Apparent plasma clearance: Approx 10 L/hr.
Administration
 May be taken with or without food.
Storage Conditions
 Oral: Store at 25°C (77<247>F); excursions permitted to 15-30°C (59-86°F).
ATC Classification
 C03DA04 - eplerenone ; Belongs to the class of aldosterone antagonists. Used as potassium-sparing diuretics.
Storage
 Oral: Store at 25°C (77<247>F); excursions permitted to 15-30°C (59-86°F).
Available As
  • Eplerenone 25 mg
  • Eplerenone 50 mg

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