Eplerenone

Croom, Katherine F; Perry, Caroline M.

doi:10.2165/00129784-200505010-00007

Cited by 34 publications

(4 citation statements)

References 38 publications

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“…By contrast, drugs that block the MR (ie, spironolactone, eplerenone, and newer aldosterone receptor antagonists) cause an increase in aldosterone production. 28,29 The MR knockout mouse has shown increased circulating aldosterone levels, and no reports were found of involution of aldosterone-producing cells. 30 …”

Section: Discussionmentioning

confidence: 99%

Preclinical and Early Clinical Profile of a Highly Selective and Potent Oral Inhibitor of Aldosterone Synthase (CYP11B2)

et al. 2017

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Section: Discussionmentioning

confidence: 99%

Preclinical and Early Clinical Profile of a Highly Selective and Potent Oral Inhibitor of Aldosterone Synthase (CYP11B2)

et al. 2017

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“…This rise in BP with age contributes substantially to the incidence of heart attack, stroke, atrial fibrillation and kidney and heart failure in the aging population worldwide [18, 42]. MRA therapy has been effective in the treatment of congestive heart failure and hypertension in several clinical trials [3, 12, 15] and has clearly been shown to decrease cardiovascular risk and significantly impact morbidity and mortality. Recent advances in our understanding of the specific role for SMC MR signaling in aging may help elucidate the beneficial effects of MRA therapy.…”

Section: Smc Mr As a Global Regulator Of Vascular Agingmentioning

confidence: 99%

Smooth muscle cell mineralocorticoid receptors: role in vascular function and contribution to cardiovascular disease

McCurley

McGraw

Pruthi

et al. 2013

Pflugers Arch - Eur J Physiol

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The mineralocorticoid receptor (MR), a member of the steroid receptor family, regulates blood pressure by mediating the effects of the hormone aldosterone on renal sodium handling. In recent years, it has become clear that MR is expressed in vascular smooth muscle cells (SMC) and interest has grown in understanding the direct role of SMC MR in regulating vascular function. This interest stems from multiple clinical studies where MR inhibitor treatment reduced the incidence of cardiovascular events and mortality. This review summarizes the most recent advances in our understanding of SMC MR in regulating normal vascular function and in promoting vascular disease. Many new studies suggest a role for SMC MR-activation in stimulating vascular contraction, and contributing to vessel inflammation, fibrosis, and remodeling. These detrimental vascular effects of MR activation appear to be independent of changes in blood pressure and are synergistic with the presence of endothelial dysfunction or damage. Thus, in humans with underlying cardiovascular disease or cardiovascular risk factors, SMC MR activation may promote hypertension, atherosclerosis, and vascular aging. Further exploration of the molecular mechanisms for the effects of SMC MR activation has the potential to identify novel therapeutic targets to prevent or treat common cardiovascular disorders.

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“…MRAs inhibit aldosterone from binding to its receptor and make it transcriptionally inactive. Consequently, aldosterone-induced sodium reabsorption is prevented, thus leading to blood pressure decrease [5,6].…”

Section: Introductionmentioning

confidence: 99%

Mineralocorticoid Receptor Antagonists Eplerenone and Spironolactone Modify Adrenal Cortex Morphology and Physiology

et al. 2021

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Mineralocorticoid receptor antagonists (MRAs) are a class of anti-hypertensive drugs that act by blocking aldosterone action. The aim of this study was to evaluate whether the MRAs spironolactone and eplerenone influence adrenal cortical physiology and morphology. Spontaneous hypertensive rats (SHR, n = 18) and normotensive rats (WKY, n = 18) were randomly exposed to a daily dose of spironolactone (n = 6), eplerenone (n = 6), or no drug (n = 6) over 28 days. After that, aldosterone, corticosterone, and 11-deoxycorticosterone plasma concentrations were quantified. Adrenal glands were subjected to morphological analysis to assess lipid droplets content, capsular width, cell proliferation, and steroidogenic proteins expression. The adrenal cortex in untreated SHR showed higher lipid droplet content as than in WKY. In SHR, MRA treatment was associated with higher circulating aldosterone levels and Ki-67 expression in aldosterone-secreting cells. In WKY, the only difference observed after MRA spironolactone treatment was a narrower capsule. There was no difference in abundance of steroidogenic enzyme between groups. In conclusion, MRAs modify adrenal gland function and morphology in SHR. The effects observed within the adrenal glomerulosa with aldosterone-secreting cell proliferation and higher circulating aldosterone levels suggests that MRA treatment provokes activation of the renin angiotensin system. The prognostic value of hyperaldosteronism secondary to MRAs blockade requires further investigation.

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Eplerenone

Cited by 34 publications

References 38 publications

Preclinical and Early Clinical Profile of a Highly Selective and Potent Oral Inhibitor of Aldosterone Synthase (CYP11B2)

Preclinical and Early Clinical Profile of a Highly Selective and Potent Oral Inhibitor of Aldosterone Synthase (CYP11B2)

Smooth muscle cell mineralocorticoid receptors: role in vascular function and contribution to cardiovascular disease

Mineralocorticoid Receptor Antagonists Eplerenone and Spironolactone Modify Adrenal Cortex Morphology and Physiology

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