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Eplerenone
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Eplerenone
Eplerenone, sold under brand name Inspra among others, is an aldosterone antagonist used primarily in the treatment of heart failure with reduced ejection fraction (HFrEF), particularly following myocardial infarction. It may also be considered as an add-on therapy in resistant hypertension; however, the majority of evidence in this setting supports the use of spironolactone (another drug in a same class), with fewer studies directly evaluating eplerenone.
It is also a steroidal antimineralocorticoid of the spirolactone group and a selective aldosterone receptor antagonist (SARA).
Eplerenone and other mineralocorticoid receptor antagonists have been demonstrated to reduce the risk of death and hospitalisation in patients with heart failure with reduced ejection fraction (HFrEF) who have a left ventricular ejection fraction (LVEF) of 40% or less. It has also been demonstrated to increase LVEF by an average of 4.95%. These benefits are seen when used with other cornerstone heart failure therapies such as an ACE inhibitor or Angiotensin II receptor blocker, beta blocker, and a diuretic .
Eplerenone lowers blood pressure in patients with primary hypertension. Eplerenone also reduces arterial stiffness and vascular endothelial dysfunction.
For persons with resistant hypertension, eplerenone is safe and effective for reducing blood pressure, particularly in persons with resistant hypertension due to hyperaldosteronism.
Eplerenone is often prescribed for people with central serous chorioretinopathy (CSC). However, the most recent and largest randomized controlled trial showed that eplerenone has no significant effect on chronic CSC that has been untreated for four months. There was one relatively large prospective, interventional case-control study that was tested in acute CSC that showed improved resolution of subretinal fluid in treatment group vs observational group (which is standard of care) with 45% resolution at end of 1st month, 55% at end of 2nd month, and 62% at end of 3rd month (vs 10%, 21%, and 31% in standard of care group). Study also showed faster resolution of visual acuity at the end of each month with 92% and 100% in the first two months vs 74% and 86% with resolution reaching 100% after the third month in standard of care group.
Common adverse drug reactions (ADRs) associated with the use of eplerenone include: hyperkalaemia, hypotension, dizziness, and reduced renal clearance. Eplerenone is associated with a lower incidence of sexual side effects, such as gynecomastia, impotence, and low sex drive, compared to spironolactone, likely due to its more selective action on the aldosterone receptor. This is because other antimineralocorticoids have structural elements of the progesterone molecule, causing progestogenic and antiandrogenic outcomes. When considering taking these medicines, it is important to note the variations in their ability to offset the nongenomic effects of aldosterone.
There is not enough evidence available from the randomized controlled trials on side effects of eplerenone to do a benefit versus risk assessment in people with primary hypertension.
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Eplerenone
Eplerenone, sold under brand name Inspra among others, is an aldosterone antagonist used primarily in the treatment of heart failure with reduced ejection fraction (HFrEF), particularly following myocardial infarction. It may also be considered as an add-on therapy in resistant hypertension; however, the majority of evidence in this setting supports the use of spironolactone (another drug in a same class), with fewer studies directly evaluating eplerenone.
It is also a steroidal antimineralocorticoid of the spirolactone group and a selective aldosterone receptor antagonist (SARA).
Eplerenone and other mineralocorticoid receptor antagonists have been demonstrated to reduce the risk of death and hospitalisation in patients with heart failure with reduced ejection fraction (HFrEF) who have a left ventricular ejection fraction (LVEF) of 40% or less. It has also been demonstrated to increase LVEF by an average of 4.95%. These benefits are seen when used with other cornerstone heart failure therapies such as an ACE inhibitor or Angiotensin II receptor blocker, beta blocker, and a diuretic .
Eplerenone lowers blood pressure in patients with primary hypertension. Eplerenone also reduces arterial stiffness and vascular endothelial dysfunction.
For persons with resistant hypertension, eplerenone is safe and effective for reducing blood pressure, particularly in persons with resistant hypertension due to hyperaldosteronism.
Eplerenone is often prescribed for people with central serous chorioretinopathy (CSC). However, the most recent and largest randomized controlled trial showed that eplerenone has no significant effect on chronic CSC that has been untreated for four months. There was one relatively large prospective, interventional case-control study that was tested in acute CSC that showed improved resolution of subretinal fluid in treatment group vs observational group (which is standard of care) with 45% resolution at end of 1st month, 55% at end of 2nd month, and 62% at end of 3rd month (vs 10%, 21%, and 31% in standard of care group). Study also showed faster resolution of visual acuity at the end of each month with 92% and 100% in the first two months vs 74% and 86% with resolution reaching 100% after the third month in standard of care group.
Common adverse drug reactions (ADRs) associated with the use of eplerenone include: hyperkalaemia, hypotension, dizziness, and reduced renal clearance. Eplerenone is associated with a lower incidence of sexual side effects, such as gynecomastia, impotence, and low sex drive, compared to spironolactone, likely due to its more selective action on the aldosterone receptor. This is because other antimineralocorticoids have structural elements of the progesterone molecule, causing progestogenic and antiandrogenic outcomes. When considering taking these medicines, it is important to note the variations in their ability to offset the nongenomic effects of aldosterone.
There is not enough evidence available from the randomized controlled trials on side effects of eplerenone to do a benefit versus risk assessment in people with primary hypertension.