利尿劑 (K sparing diuretics)，治療心肌梗塞後心衰竭、高血壓
Heart failure - Myocardial infarction with complication; Hypertension<2021/7/27>
#仿單變更2021

Potassium sparing Diuretic:
Eplerenone selectively blocks mineralocorticoid receptors reducing blood pressure in a dose-dependent manner and appears to prevent myocardial and vascular fibrosis.

Absorption:
Bioavailability, oral: 69%
Distribution:
Vd: 42 to 90 L
Metabolism:
Hepatic: Extensive via CYP3A4 pathway
Excretion:
Renal: 67%, less than 5% unchanged
Dialyzable: No, 10%
Elimination Half Life:
3 to 6 hours

1. Concomitant use with strong CYP3A4 inhibitors (eg, clarithromycin, itraconazole, ketoconazole, nefazodone, nelfinavir, ritonavir, troleandomycin)
2. CrCl of 30 mL/min or less
3. Serum potassium greater than 5.5 mEq/L at initiation

Hypertensive patient:
1. Concomitant use with potassium supplements or potassium-sparing diuretics (eg, amiloride, spironolactone, triamterene)
2. CrCl of less than 50 mL/min<2021/7/27> or serum creatinine greater than 2 mg/dL in males or greater than 1.8 mg/dL in females
3. Type 2 diabetes with microalbuminuria

B (FDA)

Infant risk cannot be ruled out. (MDX)

Common:
Endocrine metabolic: Hyperkalemia, hypertriglyceridemia
Renal: Serum creatinine raised
Serious:
Cardiovascular: Angina pectoris, Myocardial infarction
Postmarketing:
Angioedema, increased blood urea nitrogen, increased liver enzymes, increased uric acid, skin rash

Heart failure (Myocardial infarction with complication):
(Oral) Initial, 25 mg once daily; titration preferably within 4 weeks to 50 mg once daily
Systolic heart failure (Mild):
(Oral) 25 mg once daily, followed by an increase to 50 mg once daily after 4 weeks if potassium level no more than 5 mmol/L was administered in a clinical trial
Hypertension:
(Oral) initial, 50 mg once daily; allow 4 weeks to achieve optimum antihypertensive effect; may increase to MAX 50 mg twice daily for inadequate response <2021/7/27>

Safety and efficacy not established in children; ineffective among hypertensive pediatric patients aged 4 to 17 years

Heart failure:
1. eGFR 50 or greater: No initial dose adjustment necessary.
2. eGFR 30-49 : Initial, 25 mg every other day, may double the dose after 4 weeks if serum potassium remains <5 mEq/L and renal function is stable; maximum 25 mg once daily
3. eGFR 30 or less: Contraindicated
Hypertension:
1. CrCl 50 mL/min or greater: No dosage adjustments provided in the manufacturer's labeling
2. CrCl <50 mL/min or serum creatinine >2 mg/dL in men or >1.8 mg/dL in women: Contraindicated