How does eplerenone differ from spironolactone?
Andrew Davis Pharmacological differences between spironolactone and eplerenone include lower affinity of eplerenone for progesterone, androgen, and glucocorticoid receptors; more consistently demonstrated nongenomic properties for eplerenone; and the presence of long-acting metabolites for spironolactone.
What is the advantage of eplerenone over spironolactone?
A major advantage of eplerenone over the nonselective aldosterone receptor antagonist spironolactone is lack of binding to progesterone and androgen receptors, which is associated with drug-induced gynecomastia, breast pain, and impotence.
Is spironolactone more potent than eplerenone?
Spironolactone is More Effective Than Eplerenone at Lowering Blood Pressure in Patients With Primary Aldosteronism.
What type of diuretic is eplerenone?
Inspra (eplerenone) is a type of diuretic drug (“water pill”) available in tablet form used to treat high blood pressure in adults as well as heart failure following a heart attack.
What is spironolactone and eplerenone?
Aldactone (spironolactone) and eplerenone are aldosterone receptor blockers used to reduce fluid retention (edema) caused by heart, liver or kidney problems, and high blood pressure (hypertension). Aldactone is also used to treat certain patients with hyperaldosteronism.
Is eplerenone more expensive than spironolactone?
Therefore, eplerenone is approximately 6 to 7 times more expensive than spironolactone for the treatment of either hypertension or congestive heart failure.
Why is eplerenone associated with less gynecomastia than spironolactone?
Due to the selectivity of eplerenone for the aldosterone receptor, adverse effects such as gynecomastia and vaginal bleeding seem to be less likely in patients who take eplerenone than in those who take spironolactone. The most severe side effect of spironolactone, hyperkalemia, was also observed with eplerenone.
How does eplerenone help in heart failure?
In the Eplerenone Post–Acute Myocardial Infarction Heart Failure Efficacy and Survival Study (EPHESUS),3 the selective mineralocorticoid-receptor antagonist eplerenone, added to recommended medical therapy, reduced the rates of death from any cause and hospitalization for cardiovascular reasons among patients with …
Can you take spironolactone with eplerenone?
Using eplerenone together with spironolactone is not recommended. Combining these medications may significantly increase potassium levels in the blood.
Why is eplerenone used?
About eplerenone It’s used to treat heart failure and reduce the risk of you having other heart problems or a stroke. It also helps to stop heart failure getting worse. It can sometimes be used to treat a condition called hyperaldosteronism.
What is eplerenone made of?
Eplerenone is also known chemically as 9,11α-epoxy-7α-methoxycarbonyl-3-oxo-17α-pregn-4-ene-21,17-carbolactone and “was derived from spironolactone by the introduction of a 9α,11α-epoxy bridge and by substitution of the 17α-thoacetyl group of spironolactone with a carbomethoxy group.” The drug controls high blood …
What is the difference between Eplerenone and spironolactone?
Eplerenone is a steroidal antimineralocorticoid with the chemical formula of C24H30O6. It is manufactured and marketed by Pfizer under the trade name Inspra. Meanwhile, Spironolactone is an antiandrogen receptor with the chemical formula C24H32O4S. It is also manufactured and marketed by Pfizer under the trade name Aldactone.
Can spironolactone cause breast enlargement?
There is also a trial which discovered that spironolactone resulted to breast enlargement and pain among 10% of patients with heart failure while only 0.5% of patients with heart failure on eplerenone. This low prevalence with eplerenone is constant also in patients with hypertension.
Can Eplerenone and spironolactone be taken with thiazide or loop diuretics?
Nevertheless, the diuretic effects of eplerenone and spironolactone are marginal. Combination of these aldosterone antagonists with thiazide or loop diuretics will be highly more potent with the effect of thiazide or loop diuretics. In comparison to potassium supplement alone, this is more effective alternative.
Can eplerenone be used to treat gynecomastia?
Gynecomastia or breast pain was reported in 10% of male patients receiving spironolactone in a clinical trial in patients with HF.2 It is also noted that eplerenone should not be used in patients on concomitant therapy with a strong CYP 3A4 inhibitor (e.g., ketoconazole, itraconazole, nefazadone, clarithromycin, ritonavir, and nelfinavir).