依普利酮的获批适应症

(eplerenone) is a new type of selective aldosterone receptor antagonist. It was approved for clinical use by the State Food and Drug Administration in 2002. The pure product is white or off-white crystal. It has a stronger antagonistic effect on aldosterone than spironolactone, and has extremely low affinity for androgen and progesterone receptors. It has few adverse reactions. It has definite efficacy in the treatment of hypertension, heart failure and myocardial infarction. It has fewer adverse reactions and good tolerance. It is a good alternative drug to spironolactone.

Eplerenone is used for the treatment of congestive heart failure, hypertension, etc. after acute myocardial infarction.

Eplerenone can be used alone or in combination with other antihypertensive drugs to treat hypertension. The recommended dose for adults is the initial dose: 50 mg orally once daily. Maintenance dose: 50 mg orally, 1-2 times 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 doses for adults with congestive heart failure: Initial dose: 25 mg orally, once daily; gradually increase to target dose within 4 weeks as tolerated by the patient. Target dose: 50 mg orally once daily.

Subgroup analysis of the EPHESUS study also showed that the effect on reducing overall mortality was more obvious for patients with hypertension. A comparative study on the efficacy and tolerability of 499 patients with grade 1 or 2 hypertension who were randomized to receive enalapril or eplerenone showed that at 6 months, enalapril was as effective as eplerenone in reducing systolic blood pressure (eplerenone decreased by 14.5 mmHg; enalapril decreased by 12.7 mmHg; P=0.199) and diastolic blood pressure (eplerenone decreased by 11.2 mmHg; enalapril decreased by 11.3 mm). Hg; P=0.910). In the eplerenone group, the reduction in blood pressure was independent of renin levels, unlike enalapril. Both groups could reduce proteinuria above normal levels, but the eplerenone group was more significant (-61.5% vs -25.7%; P=0.01).