Abstract
Spironolactone was first developed over 50 years ago as a potent mineralocorticoid receptor antagonist with undesirable side effects; it was followed a decade ago by eplerenone, which is less potent but much more mineralocorticoid receptor-specific. From a marginal role as a potassium-sparing diuretic, spironolactone has been shown to be an extraordinarily effective adjunctive agent in the treatment of progressive heart failure. Also, spironolactone is safe and protective in arterial hypertension, particularly in patients with so-called resistant hypertension. Eplerenone is the second oral aldosterone antagonist available for the treatment of arterial hypertension and heart failure. Treatment with eplerenone has been associated with decreased blood pressure and improved survival for patients with heart failure and reduced left ventricular ejection fraction. Due to the selectivity of eplerenone for the aldosterone receptor, severe 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 common and potentially dangerous side effect of spironolactone - hyperkalemia - is also observed with eplerenone but the findings from clinical trials do not indicate more hyperkalemia induced drug withdrawals. Treatment with eplerenone should be initiated at a dosage of 25 mg once daily and titrated to a target dosage of 50 mg once daily preferably within 4 weeks. Serum potassium levels and renal function should be assessed prior to initiating eplerenone therapy, and periodic monitoring is recommended, especially in patients at high risk of developing hyperkalemia.
| Original language | English |
|---|---|
| Pages (from-to) | 25-29 |
| Number of pages | 5 |
| Journal | International Journal of Cardiology |
| Volume | 200 |
| DOIs | |
| Publication status | Published - Sep 23 2015 |
Fingerprint
Keywords
- Aldosterone
- Eplerenone
- Mineralocorticoid receptors
- Spironolactone
ASJC Scopus subject areas
- Cardiology and Cardiovascular Medicine
Cite this
Safety profile of mineralocorticoid receptor antagonists : Spironolactone and eplerenone. / Lainscak, Mitja; Pelliccia, Francesco; Rosano, Giuseppe; Vitale, Cristiana; Schiariti, Michele; Greco, Cesare; Speziale, Giuseppe; Gaudio, Carlo.
In: International Journal of Cardiology, Vol. 200, 23.09.2015, p. 25-29.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Safety profile of mineralocorticoid receptor antagonists
T2 - Spironolactone and eplerenone
AU - Lainscak, Mitja
AU - Pelliccia, Francesco
AU - Rosano, Giuseppe
AU - Vitale, Cristiana
AU - Schiariti, Michele
AU - Greco, Cesare
AU - Speziale, Giuseppe
AU - Gaudio, Carlo
PY - 2015/9/23
Y1 - 2015/9/23
N2 - Spironolactone was first developed over 50 years ago as a potent mineralocorticoid receptor antagonist with undesirable side effects; it was followed a decade ago by eplerenone, which is less potent but much more mineralocorticoid receptor-specific. From a marginal role as a potassium-sparing diuretic, spironolactone has been shown to be an extraordinarily effective adjunctive agent in the treatment of progressive heart failure. Also, spironolactone is safe and protective in arterial hypertension, particularly in patients with so-called resistant hypertension. Eplerenone is the second oral aldosterone antagonist available for the treatment of arterial hypertension and heart failure. Treatment with eplerenone has been associated with decreased blood pressure and improved survival for patients with heart failure and reduced left ventricular ejection fraction. Due to the selectivity of eplerenone for the aldosterone receptor, severe 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 common and potentially dangerous side effect of spironolactone - hyperkalemia - is also observed with eplerenone but the findings from clinical trials do not indicate more hyperkalemia induced drug withdrawals. Treatment with eplerenone should be initiated at a dosage of 25 mg once daily and titrated to a target dosage of 50 mg once daily preferably within 4 weeks. Serum potassium levels and renal function should be assessed prior to initiating eplerenone therapy, and periodic monitoring is recommended, especially in patients at high risk of developing hyperkalemia.
AB - Spironolactone was first developed over 50 years ago as a potent mineralocorticoid receptor antagonist with undesirable side effects; it was followed a decade ago by eplerenone, which is less potent but much more mineralocorticoid receptor-specific. From a marginal role as a potassium-sparing diuretic, spironolactone has been shown to be an extraordinarily effective adjunctive agent in the treatment of progressive heart failure. Also, spironolactone is safe and protective in arterial hypertension, particularly in patients with so-called resistant hypertension. Eplerenone is the second oral aldosterone antagonist available for the treatment of arterial hypertension and heart failure. Treatment with eplerenone has been associated with decreased blood pressure and improved survival for patients with heart failure and reduced left ventricular ejection fraction. Due to the selectivity of eplerenone for the aldosterone receptor, severe 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 common and potentially dangerous side effect of spironolactone - hyperkalemia - is also observed with eplerenone but the findings from clinical trials do not indicate more hyperkalemia induced drug withdrawals. Treatment with eplerenone should be initiated at a dosage of 25 mg once daily and titrated to a target dosage of 50 mg once daily preferably within 4 weeks. Serum potassium levels and renal function should be assessed prior to initiating eplerenone therapy, and periodic monitoring is recommended, especially in patients at high risk of developing hyperkalemia.
KW - Aldosterone
KW - Eplerenone
KW - Mineralocorticoid receptors
KW - Spironolactone
UR - http://www.scopus.com/inward/record.url?scp=84941961020&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=84941961020&partnerID=8YFLogxK
U2 - 10.1016/j.ijcard.2015.05.127
DO - 10.1016/j.ijcard.2015.05.127
M3 - Article
C2 - 26404748
AN - SCOPUS:84941961020
VL - 200
SP - 25
EP - 29
JO - International Journal of Cardiology
JF - International Journal of Cardiology
SN - 0167-5273
ER -