依普利酮是治疗什么病症的药？

It is a new generation of selective aldosterone antagonist, developed by Pfizer/Pharmacia, with the trade name Inspra. So, what disease is eplerenone used to treat?

Indications of eplerenone:

1. Congestive heart failure after acute myocardial infarction: Eplerenone can improve the quality of life of patients with left ventricular dysfunction (ejection fraction ≤ 40%). Clinical trials have proven that eplerenone can also be used for congestive heart failure after acute myocardial infarction;

2. Anti-hypertensive: Eplerenone can be used alone or in combination with other anti-hypertensive drugs for the treatment of hypertension.

Drug metabolism of eplerenone:

Eplerenone lowers blood pressure by binding to aldosterone receptors and blocking aldosterone in the renin-angiotensin-aldosterone system (RAAS).

The average time to peak efficacy after oral administration of eplerenone is approximately 1.5 hours. Peak concentration (Cmax) and T area of ​​the curve (AUC) increase in proportion to the dose within the dose range of 25 to 100 mg. When the dose exceeds 100 mg, AUC becomes inversely proportional to the dose.

The plasma protein binding rate of eplerenone is approximately 50%, and it is mainly bound to α1, acidic glycoprotein. In healthy volunteers and hypertensive patients, the apparent volume of distribution ranges from 43 to 90 L at steady state.

Eplerenone is metabolized primarily by the CYP3A4 enzyme. No active metabolites were detected in human serum, and approximately 5% of unmetabolized eplerenone could be detected in urine and feces. After a single oral dose of radiolabeled eplerenone, approximately 32% of the drug is excreted in the feces and approximately 67% of the drug is excreted in the urine. The elimination half-life of eplerenone is approximately 4 to 6 hours. The apparent plasma clearance is approximately 10L/h.

It has minimal interaction with androgen and progesterone receptors and has a long half-life. Taking it orally once a day can effectively control hypertension, reduce damage to target organs such as the heart, brain, and kidneys, and improve microalbuminuria in patients with type 2 diabetes. The incidence of side effects is similar to that of placebo, and it is well tolerated.