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
O6 
Mol. mass 414.49
Pharmacokinetic data
Bioavailability 69%
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 (Pfizer under the trade name Inspra.

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 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 hyperkalaemia, hypotension, dizziness, altered renal function, and increased creatinine concentration.[1]

Drug interactions

Eplerenone is primarily metabolised by the 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)
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