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.


Adult Dose
Dose: 25 to 50 mg
Single Dose: 38 (37.5)
Frequency: 24 hourly
Route: PO
Instructions: 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
Neonatal
Paedriatic
Characteristics
It belongs to Aldosterone antagonist pharmacological group on the basis of mechanism of action. The Molecular Weight of Eplerenone is 414.50.
Contraindications
Eplerenone is contraindicated in conditions like Hyperkalaemia,Severe renal impairment.
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.
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.
Interactions
Eplerenone is known to interact with other drugs, the details of drug interactions is as follows:DrugDetailsSeverityOnsetManagementAspirinNSAIDs may possibly reduce the antihypertensive and/or diuretic effects of potassium-sparing diuretics and may increase risk of hyperkalaemia. DiazoxideConcomitant use with diazoxide, MAOIs, pentoxifylline, prostacyclin analogues may enhance hypotensive effect of antihypertensives.Enalapril (Maleate)Eplerenone may enhance hyperkalaemic effect of ACE inhibitors, angiotensin II receptor blockers, potassium-sparing diuretics or potassium salts.Monitor serum potassium levels and adjust doses.ErythromycinConcomitant use with moderate CYP3A4 Inhibitors (e.g. verapamil, erythromycin, saquinavir, fluconazole) may increase serum concentrations of Eplerenone ranging from 1.4-1.6 folds.ModerateIn patients with hypertension reduce the starting dose to 25mg once daily.KetoconazoleConcomitant use with strong CYP3A4 Inhibitors (e.g. ketoconazole) may increase serum concentrations of Eplerenone.MajorConcomittant use is contraindicated.LithiumCause lithium toxicity.MajorMonitor serum lithium levels frequently.VORICONAZOLEVoriconazole may increase the serum concentration of eplerenone by decreasing its metabolism. Concomitant therapy is contraindicated. These interactions are sometimes beneficial and sometimes may pose threats to life. Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.
Interfrence
Risks
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.
Storage
tablet Store Between 20°C-25°C. Protect from Sunlight, Moisture and Heat.
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
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