Generic Name and Formulations:
Eplerenone 25mg, 50mg; tabs.
Company:
Pfizer Inc.
To improve survival of stable patients with left ventricular systolic dysfunction (ejection fraction ≤40%) and clinical evidence of CHF after acute MI.
Initially 25mg once daily; titrate within 4 weeks to 50mg once daily. Adjust based on serum K+ (see literature).
Not recommended.
Aldosterone receptor blocker (mineralocorticoid-selective).
Hyperkalemia (serum K+ >5.5mEq/L) at initiation, severe renal impairment (CrCl ≤30mL/min), or concomitant potent CYP3A4 inhibitors (eg, ketoconazole, itraconazole, nefazodone, troleandomycin, clarithromycin, ritonavir, nelfinavir).
Severe hepatic impairment. Renal dysfunction. Serum creatinine >2mg/dL (males) or >1.8mg/dL (females), CrCl ≤ 50mL/min, or diabetes with proteinuria. Monitor serum K+ at baseline, within 1st week, at 1 month after starting and after dose adjustment, then periodically. Elderly. Pregnancy (Cat.B). Nursing mothers: not recommended.
CYP3A4 inhibitors (see Contraindications and Dose). NSAIDs may antagonize antihypertensive effects. Angiotensin II receptor blockers, ACEIs increase hyperkalemia risk. Monitor lithium.
Hyperkalemia, dizziness, GI upset, abdominal pain, cough, flu-like symptoms, albuminuria; increased serum creatinine, triglycerides, cholesterol; decreased serum sodium; rare: sex hormone related effects, increased BUN, uric acid, liver enzymes.
Tabs—30, 90
Hypertension.
Initially 50mg once daily; may increase after 4 weeks to max 50mg twice daily. Concomitant weak CYP3A4 inhibitors (eg, erythromycin, verapamil, saquinavir, fluconazole): initially 25mg once daily. Adjust based on serum K+ (see literature).
Not recommended.
Aldosterone receptor blocker (mineralocorticoid-selective).
Hyperkalemia (serum K+ >5.5mEq/L) at initiation, severe renal impairment (CrCl ≤30mL/min), or concomitant potent CYP3A4 inhibitors (eg, ketoconazole, itraconazole, nefazodone, troleandomycin, clarithromycin, ritonavir, nelfinavir). Type 2 diabetes with microalbuminuria, CrCl<50mL/min, serum creatinine >2mg/dL (males), >1.8mg/dL (females), or concomitant K+ supplements or K+ sparing diuretics.
Severe hepatic impairment. Renal dysfunction. Monitor serum K+ at baseline, within 1st week, at 1 month after starting and after dose adjustment, then periodically. Elderly. Pregnancy (Cat.B). Nursing mothers: not recommended.
CYP3A4 inhibitors (see Contraindications and Dose). NSAIDs may antagonize antihypertensive effects. Angiotensin II receptor blockers, ACEIs increase hyperkalemia risk. Monitor lithium.
Hyperkalemia, dizziness, GI upset, abdominal pain, cough, flu-like symptoms, albuminuria; increased serum creatinine, triglycerides, cholesterol; decreased serum sodium; rare: sex hormone related effects, increased BUN, uric acid, liver enzymes.
Tabs—30, 90