依普利酮注意事项

It was developed by Pfizer of the United States and first launched in the United States in 2002. It is mainly used clinically to treat hypertension. In 2003, it was approved by the FDA for the treatment of heart failure after acute myocardial infarction. Eplerenone is a new type of selective aldosterone receptor antagonist.

The dosage for treating high blood pressure in adults is as follows: Eplerenone can be used alone or in combination with other antihypertensive drugs. Initial dose: 50 mg orally once daily, Maintenance dose: 50 mg orally once or twice daily, Maximum dose: 100 mg/day. Obvious antihypertensive effects appear within four weeks of taking the drug. Patients whose blood pressure responds inadequately to the initial dose may be increased to 50 mg twice daily.

Common side effects of eplerenone (>10%): Endocrine and metabolic: hyperkalemia ([Heart failure, post-myocardial infarction: >5.5meq/L: 16%; ≥6meq/L: 6%, [Hypertension, >5.5meq/L: 400mg: 9%; dose ≤200mg: ≤1%]), hypertriglyceridemia (1%-15%; dose related)

Eplerenone should be noted to be prohibited from use in the following situations:

Type 2 diabetes (non-insulin-dependent, NIDDM) with microalbuminuria; serum creatinine >2.0 mg/dL in men or >1.8 mg/dL in women; CrCl <50 mL/min; concurrent use of potassium supplements or potassium-sparing diuretics (such as amiloride, spironolactone, triantiline).

In accordance with the Endocrine Society Clinical Practice Guidelines, its use is contraindicated in patients with Addison's disease.

Hypersensitivity to eplerenone or any component of the formulation; initial serum potassium >5 meq/L; severe hepatic impairment (Child-Pugh class C); clinically significant hyperkalemia; concurrent use with potassium supplements or potassium-sparing diuretics.

The following additional contraindications apply to patients with hypertension: Serum creatinine >1.5 mg/dL [132 micromol/L] in men and >1.3 mg/dL [115 micromol/L] in women

Also avoid potassium supplements, potassium-containing salt substitutes, potassium-rich diets, or other medications that may cause hyperkalemia (eg, other potassium-sparing diuretics, nonsteroidal anti-inflammatory drugs). Concomitant use of potassium supplements or potassium-sparing diuretics is contraindicated in the treatment of hypertension.

Untreated hypertension and heart failure are both associated with adverse pregnancy outcomes. The use of mineralocorticoid receptor antagonists is not recommended for the treatment of chronic isolated hypertension in pregnant women and should generally be avoided in women of reproductive potential.