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Eplerenone



Eplerenone
Systematic (IUPAC) name
pregn-4-ene-7,21-dicarboxylic acid, 9,11-epoxy-17-hydroxy-3-oxo, γ-lactone, methyl ester (7α, 11α, 17α)
Identifiers
CAS number 107724-20-9
ATC code C03DA04
PubChem 5282131
DrugBank APRD00707
Chemical data
Formula C24H30O6 
Mol. mass 414.49
Pharmacokinetic data
Bioavailability 69%
Metabolism hepatic (CYP3A4)
Half life 3–5 hours
Excretion 67% renal
32% biliary
Therapeutic considerations
Pregnancy cat.

B3 (Aust)

Legal status

Schedule 4 (Aust)

Routes oral

Eplerenone (INN) (pronounced /ɛpˈlɛrənoʊn/) is an aldosterone antagonist used as an adjunct in the management of chronic heart failure. It is similar to spironolactone, though it may be more specific for the mineralocorticoid receptor and is specifically marketed for reducing cardiovascular risk in patients following myocardial infarction. It is marketed by Pfizer under the trade name Inspra.

Additional recommended knowledge

Contents

Clinical use

Indications

Eplerenone is specifically indicated for the reduction of risk of cardiovascular death in patients with heart failure and left ventricular dysfunction within 3–14 days of an acute myocardial infarction, in combination with standard therapies and as treatment against hypertension.

Contraindications

Eplerenone is contraindicated in patients with hyperkalaemia, severe renal impairment (creatinine Cl less than 30 ml/min), or severe hepatic impairment (Child-Pugh C). The manufacturer of eplerenone also contraindicates ( relative C.I. ) concomitant treatment with ketoconazole, itraconazole or other potassium-sparing diuretics (though the manufacturer still considers taking these drugs to be absolute C.I.) Potential benefits should be weighted against possible risks.

Adverse effects

Common adverse drug reactions (ADRs) associated with the use of eplerenone include: hyperkalaemia, hypotension, dizziness, altered renal function, and increased creatinine concentration.[1]

Drug interactions

Eplerenone is primarily metabolised by the cytochrome P450 enzyme CYP3A4. Thus the potential exists for adverse drug interactions with other drugs that induce or inhibit CYP3A4. Specifically, the concomitant use of the CYP3A4 potent inhibitors ketoconazole and itraconazole is contraindicated. Other CYP3A4 inhibitors including erythromycin, saquinavir, and verapamil should be used with caution. Other drugs that increase potassium concentrations may increase the risk of hyperkalaemia associated with eplerenone therapy, including salt substitutes,[2] potassium supplements and other potassium-sparing diuretics.

General considerations

Due to the high risk of elevated potassium levels in individuals taking eplerenone, The United States FDA suggests routine checks on the individual's potassium level to screen for hyperkalemia.

See also

References

  1. ^ Rossi S, editor. Australian Medicines Handbook 2006. Adelaide: Australian Medicines Handbook; 2006
  2. ^ LoSalt Advisory Statement (PDF)
 
This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Eplerenone". A list of authors is available in Wikipedia.
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