Angiotensin-converting enzyme (ACE) inhibitors significantly reduce cardiovascular events in patients with established or at high risk for coronary artery disease; however, the favorable effect appears to be modest.1 Although early after initiation of therapy ACE inhibition reduces plasma levels of both angiotensin II and aldosterone, during prolonged ACE inhibition aldosterone levels may incre...

Blocking brain mineralocorticoid receptors (MRs) reduces the high circulating levels of tumor necrosis factor (TNF)in heart failure (HF) rats. TNFand other proinflammatory cytokines activate neurons in the paraventricular nucleus (PVN) of hypothalamus, including corticotropin-releasing hormone (CRH) neurons, by inducing cyclooxygenase (COX)-2 activity and synthesis of prostaglandin E2 by periva...

AIMS Cardiovascular hospitalization (CVH) in patients with heart failure (HF) is associated with a high post-discharge rate of early re-admission and CV death. Eplerenone might be effective in reducing the incidence of these adverse clinical outcomes during this period. METHODS AND RESULTS The EMPHASIS-HF trial compared eplerenone with placebo added to standard therapy in 2737 patients with N...

Article history: Received 24 March 2016 Accepted 16 April 2016 Available online 22 April 2016 Background: Despite rapid reperfusion, mortality and morbidity in patients with an acute myocardial infarction remain significant. Therefore, novel pharmacological strategies to further limit ischemia–reperfusion (IR) injury are warranted. In animal models of myocardial infarction, mineralocorticoid re...

Eplerenone, a BCS class II drug with low bioavailability and t1/2 of 3-6 hrs is primarily used to treat Congestive Heart Failure (CHF) hypertension. So, develop the biological performance solid dispersion along oral disintegrates was prepared by employing HP ?-Cyclodextrin ?-Cyclodextrin. Eplerenone dispersions were repared various carriers in varying ratios carrier respectively (0.5:1, 1:1 1.5...

Few data are available on effects of aldosterone antagonism in patients with mild-to-moderate heart failure (HF). In this multicenter, randomized, double-blind, placebo-controlled study, patients with mild-to-moderate HF and left ventricular (LV) systolic dysfunction were randomly assigned to receive eplerenone 50 mg/d versus placebo in addition to contemporary background therapy. The primary e...

Recently we reported a cytoplasmic sodium overload to cause a severe osmotic oedema in Duchenne muscular dystrophy (DMD). Our results suggested that this dual overload of sodium ions and water precedes the dystrophic process and persists until fatty muscle degeneration is complete. The present paper addresses the questions as to whether these overloads are important for the pathogenesis of the ...

Two unknown impurities were observed during the process development for multigram-scale synthesis of eplerenone (Inspra®). The new process-related impurities were identified and fully characterized as the corresponding (7β,11α,17α)-11-hydroxy- and (7α,11β,17α)-9,11-dichloroeplerenone derivatives 12a and 13. Seven other known but poorly described in the literature eplerenone impurities, includin...