Eplerenone

Drug #2220

Eplerenone, a blocker of aldosterone binding at the mineralocorticoid receptor. It is chemically described as Pregn-4-ene-7,21-dicarboxylic acid, 9,11-epoxy-17-hydroxy-3-oxo-,gama -lactone, methyl ester, (7alpha,11alpha,17alpha). Its empirical formula is C24H30O6.

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Primary Characteristics

It belongs to Aldosterone antagonist pharmacological group on the basis of mechanism of action.

Molecular Weight: 414.5 · Solubility in Water: slightly · Non-proprietary name: Eplerenone.

Pharmacokinetics

Absorption: Eplerenone has an oral bioavailability is 69%.

Distribution: Eplerenone has a volume of distribution is 43 to 90L. plasma protein binding is 50%.

Elimination: it is metabolised via CYP3A4, plasma half-life is 4-6 hours, renal excretion is 67% and 32% in feces.

Indications

Eplerenone is primarily indicated in conditions like Hypertension.

Eplerenone is also indicated for secondary conditions like Congestive heart failure post MI, Left ventricular dysfunction.

Contraindications

Eplerenone is contraindicated in conditions like Hyperkalaemia, Severe renal impairment.

Dosage

Eplerenone's dosage details are as follows:

Dose	Single Dose	Frequency	Route	Instructions
Adult Dosage
37.5 mg	37.5 mg	Every 24h	PO	CHF Post-MI Initial: 25 mg once daily; titrate to recommended dose of 50 mg once daily within 4 wk as tolerated. Adjust dose based on serum potassium level; reduce or withdraw therapy if hyperkalaemia develops
50 mg	50 mg	Every 24h	PO	Hypertension, Initial with 50 mg once daily; may increase to 50 mg twice daily based on response. Initiate at lower dose of 25 mg once daily if used concurrently with moderate CYP3A4 inhibitors.
50 mg	50 mg	Every 12h	PO	Hypertension, Initial with 50 mg once daily; may increase to 50 mg twice daily based on response.
Paediatric Dosage (20kg)
No data.
Neonatal Dosage (3kg)
No data.

Drug Interactions

4 interactions

Major2 interactions

Moderate1 interaction

Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.

Side Effects

Eplerenone in overdosage may give rise to further complications which include Angioneurotic edema, Albuminuria , Vaginal bleeding , Gynecomastia.

Eplerenone produces potentially life-threatening effects which include Myocardial infarction, Anaphylactic reactions, Shortness of breath. Careful monitoring is needed with proper medical management.

The signs and symptoms that are produced after acute overdosage of Eplerenone are Hypotension, Hyperkalemia.

Eplerenone is known to cause more or less tolerable side effects which are usually transient. These include Cough , Diarrhea, Dizziness, Faintness , Hypotension , Light headedness, Nausea, Vomiting .

Warnings / Precautions

Monitor patients for the development of hyperkalemia until the effect of eplerenone is established. Patients who develop hyperkalemia ( > 5.5 mEq/L) may continue eplerenone therapy with proper dose adjustment. Dose reduction decreases potassium levels. Patients with hypertension who have serum creatinine levels > 2.0 mg/dL (males) or > 1.8 mg/dL (females) or creatinine clearance = 50 mL/min should not be treated with it. Patients with CHF post-MI who have serum creatinine levels > 2.0 mg/dL (males) or > 1.8 mg/dL (females) or creatinine clearance = 50mL/min should be treated with eplerenone with caution. Diabetic patients with CHF post-MI should also be treated with caution, especially those with proteinuria. Safety and efficacy not established in patients with severe hepatic impairment; or paediatric patients <18 yr. Pregnancy and lactation.

Available Brands

Click on a strength to view available brands.

Single Ingredient

Tabs

25 mg 50 mg

Storage Conditions

Eplerenone should be stored tablet.

Drug Classification

1.16.3 — Potassium sparing diuretics

Manufacturers

Manufacturers of Eplerenone in Pakistan:

Macter Platinum Tabros