Medical Ingredient Eplerenone CAS 107724-20-9 for Acute Myocardial Infarction

Description
 

Eplerenone, sold under the brand name Inspra, is a steroidal antimineralocorticoid of the spirolactone group that is used as an adjunct in the management of chronic heart failure and high blood pressure, particularly for patients with resistant hypertension due to elevated aldosterone. Classed as a selective aldosterone receptor antagonist (SARA), it is similar to the diureticspironolactone, though it is much more selective for the mineralocorticoid receptor in comparison (i.e., does not possess any antiandrogen, progestogen, glucocorticoid, or estrogenic effects), and is specifically marketed for reducing cardiovascular risk in patients following myocardial infarction. Eplerenone is a potassium-sparing diuretic, meaning that it helps the body get rid of water but still keep potassium.

Medical uses

Heart failure

Eplerenone is specifically indicated for the reduction of risk of cardiovascular death in people with heart failure and left ventricular dysfunction within 3-14 days of an acute myocardial infarction, in combination with standard therapies and as treatment against hypertension. A variant of the spirolactone group, Eplerenone was developed to contradict the depletion of essential potassiumand magnesium levels that are common amongst other mineralocorticoid receptor antagonists.^[9]It is a more expensive alternative to spironolactone.

Hypertension

Eplerenone can be used individually or in combination with other medications to treat hypertension. In an 8-week trial with 417 patients with mild to moderate hypertension, eplerenone decreased systolic and diastolic blood pressure in a dose-dependent manner.However, A 2017 Cochrane systematic review on eplerenone did not find any clinically important dose response in decreasing blood pressure for doses 50 to 400 mg daily. According to their meta-analysis, eplerenone lowered systolic blood pressure by 9.21 mmHg and diastolic blood pressure by 4.18 mmHg in people with primary hypertension. Eplerenone effectively reduces blood pressure compared to agents such as spironolactone, enalapril, losartan and amlodipine, but its effect on mortality is still generally unknown.

For persons with resistant hypertension, aldosterone antagonists (including eplerenone) were safe and in comparative studies reduced systolic blood pressure by 24 mm Hg and diastolic blood pressure by about 8 mm Hg. Specifically, eplerenone is likely to be particularly effective in persons with resistant hypertension due to hyperaldosteronism, as indicated by a high blood plasma aldosterone and a low plasma renin activity.

Central serous retinopathy

Eplerenone is being explored as a treatment for central serous retinopathy.It is expected that as an antimineralocorticoid, eplerenone can inhibit over-activation of the mineralocorticoid receptor pathway in the choroid. Separate trials are underway to determine if there are beneficial effects of eplerenone for acute and chronic CSR.

Other uses

Eplerenone, in contrast to spironolactone, does not have antiandrogenic effects, and hence is not useful in feminizing hormone therapy for transgender women and related indications.

Packaging and transportation 

Packing: this product is double-packed: the inner layer is sealed with edible polythene plastic bags, and the outer packaging is in cardboard boxes.The net content of each case is 25kg. It can also be packed according to customers' needs.

Transportation: light loading and unloading.Prevent the sun, rain, can not be mixed with toxic, harmful goods, this product is not dangerous goods, can be transported according to the general chemicals.
Storage: it should be stored in a dry, clean and dark environment. It is strictly prohibited to mix with toxic substances to avoid pollution.The shelf life is two years.


Packaging