依普利酮什么时候上市呢？

(eplerenone) is the first selective aldosterone receptor antagonist. It has been used to treat hypertension and left ventricular dysfunction after acute myocardial infarction. It can effectively lower blood pressure, improve cardiac function, and reduce myocardial damage. The chemical formula of eplerenone (EPL) is 9,11-epoxy-17-hydroxy-3-oxo-γ-lactone-4-pregnene-7,21-dicarboxylic acid methyl ester.

Eplerenone selectively acts on aldosterone receptors and is highly selective for mineralocorticoid receptors, but has less effect on androgen and progesterone receptors. Its affinity for mineralocorticoids is 15 to 20 times that of spironolactone, while its affinity for androgen and progesterone receptors is 500 times smaller than that of spironolactone, so sex hormone-related adverse reactions are less likely to occur.

Aldosterone has a variety of pathophysiological effects, including causing central hypertension, accelerating endothelial damage (catecholamines enhance its effects), reducing heart rate variability, inducing ventricular arrhythmia, promoting sodium retention, potassium and magnesium loss, promoting myocardial fibrosis, necrosis and inflammation, and damaging the fibrinolytic system.

In a study of systolic hypertension in the elderly, 269 patients were treated with eplerenone (50-200) mg daily and amlodipine (2.5-10) mg daily. The results showed that both drugs had the same effect in lowering systolic blood pressure, while amlodipine lowered diastolic blood pressure more significantly. In terms of target organ protection, both drugs improved carotid-femoral and carotid-radial pulse rates after 24 weeks of treatment. In terms of the incidence of adverse reactions, 19.9% ​​of the amlodipine group developed peripheral edema, while only 2.7% of the eplerenone group developed hyperkalemia. 0.4% of the amlodipine group developed hyperkalemia, and 0.9% of the eplerenone group developed hyperkalemia.

When was eplerenone launched on the market?

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. In 2002, eplerenone was approved for clinical use by the State Food and Drug Administration, but it has not been marketed in my country, so Chinese patients cannot currently buy this drug in domestic pharmacies.