Eplerenone

CLINICAL USE

Aldosterone antagonist:Left ventricular dysfunction and heart failure

DOSE IN NORMAL RENAL FUNCTION

25–50 mg daily

PHARMACOKINETICS

Molecular weight :414.5

%Protein binding :50

%Excreted unchanged in urine : <5

Volume of distribution (L/kg) :43–57 litres

half-life – normal/ESRD (hrs) :3–6

DOSE IN RENAL IMPAIRMENT

GFR (mL/MIN)

20 to 50 : Dose as in normal renal function1

10 to 20 : Dose as in normal renal function1

<10 : Dose as in normal renal function1

DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

CAPD :Unknown dialysability. Dose as in GFR <10 mL/min

HD :10% dialysed.1 Dose as in GFR <10 mL/min

HDF/high flux :Unknown dialysability. Dose as in GFR <10 mL/min

CAV/VVHD :Unknown dialysability. Dose as in GFR=10-20 mL/min

IMPORTANT DRUG INTERACTIONS

Potentially hazardous interactions with other drugsACE inhibitors or AT-II antagonists: enhanced hypotensive effect; risk of severe hyperkalaemia

Anti-arrhythmics: concentration increased by amiodarone – reduce eplerenone dose

Antibacterials: concentration increased by clarithromycin and telithromycin – avoid concomitant use; concentration increased by erythromycin – reduce eplerenone dose; concentration reduced by rifampicin – avoid concomitant use; avoid concomitant use with lymecycline; increased risk of hyperkalaemia with trimethoprim

Antidepressants: concentration reduced by St John’s wort – avoid concomitant use; increased risk of postural hypotension with tricyclics; enhanced hypotensive effect with MAOIs

Anti-epileptics: concentration reduced by carbamazepine, phenytoin and phenobarbital – avoid concomitant use

Antifungals: concentration increased by itraconazole and ketoconazole – avoid concomitant use; concentration increased by fluconazole – reduce eplerenone doseAntihypertensives: enhanced hypotensive effect, increased risk of first dose hypotensive effect with post-synaptic alpha-blockers

Antivirals: concentration increased by nelfinavir and ritonavir – avoid concomitant use; concentration increased by saquinavir – reduce eplerenone dose

Ciclosporin: increased risk of hyperkalaemia and nephrotoxicityNSAIDs: increased risk of hyperkalaemia (especially with indometacin); increased risk of nephrotoxicity; antagonism of diuretic effect

Potassium salts: increased risk of hyperkalaemia

Lithium: reduced lithium excretion – avoid concomitant use

Tacrolimus: increased risk of hyperkalaemia and nephrotoxicityCYP3A4 inhibitors: Do not exceed a dose of 25 mg daily for eplerenoneCYP3A4 inducers: reduced eplerenone concentration – avoid concomitant use

ADMINISTRATION

Reconstition

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Route

Oral

Rate of Administration

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Comments

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OTHER INFORMATION

Monitor potassium levels regularly in people with renal impairment

See how to identify renal failure stages according to GFR calculation

See how to diagnose irreversible renal disease

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