OBJECT DRUGS

• Eplerenone (Inspra)

PRECIPITANT DRUGS

Antidepressants:

• Fluvoxamine (Luvox, etc.)
• Nefazodone

Comment:

Eplerenone is metabolized primarily by CYP3A4, and potent inhibitors of CYP3A4 may produce marked increases the serum levels of eplerenone. This may increase the risk of eplerenone toxicity, and the manufacturer states that eplerenone is contraindicated with potent CYP3A4 inhibitors. Nefazodone is a potent CYP3A4 inhibitor, and fluvoxamine is a moderate inhibitor.

Class 2: Use Only if Benefit Felt to Outweigh Risk

• Use Alternative:Sertraline (Zoloft), citalopram (Celexa), escitalopram (Lexapro), venlafaxine (Effexor), and paroxetine (Paxil) appear less likely to inhibit CYP3A4 than fluvoxamine. Fluoxetine: (Prozac) appears to be a weak inhibitor of CYP3A4, but little is known about the effect of other antidepressants on eplerenone.
• Monitor: If CYP3A4 inhibitors are used with eplerenone, monitor for excessive eplerenone effects such as hypotension and hyperkalemia; reduce eplerenone dose as needed.