依普利酮效果怎么样呢？

It 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.

In recent years, more and more evidence has shown that other tissues, especially the heart, brain and blood vessels, can also independently synthesize aldosterone. Not only that, it can also directly affect blood pressure and damage the heart, brain, kidneys and other organs. Overactivation of the renin-angiotensin-aldosterone system (RAAS) is an important factor that aggravates myocardial damage, myocardial remodeling, and promotes the progression of heart failure (heart failure). The degree of activation of this system affects patient prognosis and death. Blocking excessive activation of RAAS is an important measure to improve ventricular remodeling, heart failure prognosis, and reduce heart failure mortality. Eplerenone was the first selective aldosterone receptor blocker approved for marketing.

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.

The commonly used domestic aldosterone receptor antagonist spironolactone has a significant protective effect on the cardiovascular system, but its sex hormone-related side effects limit its application. As a new generation of selective aldosterone receptor antagonists, it provides a new method for the treatment of cardiovascular diseases.