Eplerenone
Eplerenone Information

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Eplerenone

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About Eplerenone

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.

Indications

Eplerenone is primarily indicated in conditions like Hypertension, and can also be given in adjunctive therapy as an alternative drug of choice in Congestive heart failure post MI, Left ventricular dysfunction.

Contraindication

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

Side Effects

The severe or irreversible adverse effects of Eplerenone, which give rise to further complications include Angioneurotic edema, Albuminuria, Vaginal bleeding, Gynecomastia.Eplerenone produces potentially life-threatening effects which include Myocardial infarction, Anaphylactic reactions, Shortness of breath. which are responsible for the discontinuation of Eplerenone therapy.The signs and symptoms that are produced after the acute overdosage of Eplerenone include Hypotension, Hyperkalemia.The symptomatic adverse reactions produced by Eplerenone are more or less tolerable and if they become severe, they can be treated symptomatically, these include Dizziness, Nausea, Vomiting, Diarrhea, Hypotension, Cough, Light headedness, Faintness.

Warnings

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

High Risk Groups

Drug should not be given to Paediatrics, Pregnant Mothers, patients suffering from Kidney dysfunction, and Neonates.If prescribing authority justifies the benefits of the drug against the possible damages he/she should reevaluate them and consult the reference material and previous studies.

Dosage

Eplerenone Dosage for Adults

Dose 25 to 50 mg
Single Dose 38 (37.5)
Frequency 24 hourly
Route PO
Note: 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
Dose 50 to 50 mg
Single Dose 50 (50)
Frequency 24 hourly
Route PO
Note: 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.

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