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Primary hyperaldosteronism
Published in Nadia Barghouthi, Jessica Perini, Endocrine Diseases in Pregnancy and the Postpartum Period, 2021
Vivek Alaigh, Amanda Fernandes
Mineralocorticoid receptor antagonists such as spironolactone and eplerenone are typically first-line agents in treatment of primary hyperaldosteronism. However, because spironolactone can cross the placenta, there is a concern with its use during pregnancy due to the theoretical risk of feminization of male fetuses based on animal models. Thus, mineralocorticoid receptor antagonists are not recommended for use in pregnancy and should be discontinued approximately one month before conception.23 In the limited cases of spironolactone use during pregnancy for primary hyperaldosteronism, no feminization or malformations were noted in male infants.4 There was a single case of sexual ambiguity in a female fetus in the setting of maternal use of spironolactone until the 5th month of pregnancy.30 No significant data exists regarding the use of eplerenone during pregnancy.19
Resistant Hypertension: Medical Treatment
Published in Giuseppe Mancia, Guido Grassi, Konstantinos P. Tsioufis, Anna F. Dominiczak, Enrico Agabiti Rosei, Manual of Hypertension of the European Society of Hypertension, 2019
Michel Azizi, Laurence Amar, Aurélien Lorthioir, Anne-Marie Madjalian
The fourth-line treatment should involve a mineralocorticoid receptor (MR) antagonist, such as spironolactone (Class I A recommendation) (3) or eplerenone. Eplerenone is a short-acting MR antagonist better tolerated but less potent than spironolactone (34,35). However, eplerenone has not been approved for use to treat hypertension in many European countries.
Basic pharmacology of cardiac drugs
Published in John Edward Boland, David W. M. Muller, Interventional Cardiology and Cardiac Catheterisation, 2019
The aldosterone antagonists are commonly used in concert with thiazide or other diuretics in the treatment of fluid retention or hypertension. Spironolactone is frequently added to other diuretics as a means of preventing excessive potassium loss and used in management of primary (rare) or secondary hyperaldosteronism. Spironolactone has been shown to be of benefit added to other therapies in severe chronic heart failure. The mechanism is not entirely clear but may relate to an anti-fibrosis effect obtained by inhibiting aldosterone. The role of eplerenone in heart failure is also promising.
Adherence and blood pressure control in patients with primary aldosteronism
Published in Blood Pressure, 2022
Thi Minh Phuong Nikrýnová Nguyen, Branislav Štrauch, Ondřej Petrák, Zuzana Krátká, Robert Holaj, Ivana Kurcová, Věra Marešová, Alena Pilková, Jan Hartinger, Petr Waldauf, Tomáš Zelinka, Jiří Widimský
Our study indicated very good blood pressure control in conservatively treated patients with PA which is also related to excellent adherence. These data correspond with previous data showing effective blood pressure reduction and correction of hypokalaemia in patients with PA [29,30]. Average dose of spironolactone in our study was 46 ± 21 mg/d and thus a marked proportion of PA patients were treated with low dose spironolactone in agreement with previous observation [30]. Prescription of eplerenone to our patients was common, mainly in males. Due to shorter half-life and inferior antihypertensive efficacy in comparison with spironolactone [31], we had to administer eplerenone twice a day and in higher doses (average dose was 80 ± 31 mg). In contrast with other studies, we were unable to manage hypertension in our patients with MR antagonist monotherapy [30]. Combination antihypertensive therapy was necessary in all patients. One of the potential explanations could be relatively higher age of our patients and/or presence of comorbidities like obesity, diabetes mellitus and/or renal dysfunction. Calcium-channel blockers and thiazide/thiazide-like diuretics were mainly used in combination with MR antagonists which is in accordance with other data [32]. Other antihypertensive classes were also used (RAS blockers, beta-blockers, alpha-blockers and centrally acting agents) depending on blood pressure values and/or individual clinical profile of our patients (for example presence of coronary artery disease, prostatic hyperplasia).
Optimal cardiovascular medical therapy: current guidelines and new developments
Published in Baylor University Medical Center Proceedings, 2022
Shirley Cotty Reed, Nikita Dhir, R. Jay Widmer
Both AHA/ACC and ESC recommend the use of aldosterone antagonists (spironolactone or eplerenone) in patients with LVEF ≤35% or after MI if LVEF ≤40% with heart failure symptoms or diabetes mellitus.2,3 The RALES (Randomized Aldactone Evaluation Study) trial was the first to demonstrate a reduction in all-cause mortality (30%) in patients with heart failure and LVEF <35% with the use of spironolactone.25 Subsequent trials EPHESUS (Eplerenone Post-AMI Heart Failure Efficacy and Survival Study) and EMPHASIS-HF (Eplerenone in Mild Patients Hospitalization and Survival Study in Heart Failure) investigated the use of eplerenone in heart failure with reduced ejection fraction post-MI and treatment of heart failure symptoms and demonstrated similar benefits.26,27
Eplerenone nanocrystals engineered by controlled crystallization for enhanced oral bioavailability
Published in Drug Delivery, 2021
Muhammad Ayub Khan, Muhammad Mohsin Ansari, Sadia Tabassam Arif, Abida Raza, Ho-Ik Choi, Chang-Wan Lim, Ha-Yeon Noh, Jin-Su Noh, Salman Akram, Hafiz Awais Nawaz, Muhammad Ammad, Abir Abdullah Alamro, Amani Ahmed Alghamdi, Jin-Ki Kim, Alam Zeb
Eplerenone (EPL) is an aldosterone receptor antagonist and is utilized to manage hypertension and chronic heart failure (Seferovic et al., 2015). Like other BCS class II drugs, EPL also possesses low aqueous solubility and dissolution-dependent absorption with the resultant low oral bioavailability (Ozdemir et al., 2018). Therefore, its solubilizing capability needs to be enhanced for achieving efficient absorption and sufficient bioavailability. The current work is intended to develop and optimize eplerenone nanocrystals (EPL-NCs) by using a D-optimal mixture design process. EPL-NCs were prepared by using a novel bottom-up, controlled crystallization technique during freeze-drying, and the optimized formulation was subsequently studied for different physicochemical properties. The in vitro saturation solubility and dissolution profile of EPL-NCs was measured in 0.1 N HCl solution as a gastric fluid. The in vivo pharmacokinetic parameters were determined after oral administration of EPL-NCs to rats. Furthermore, a single-dose acute oral toxicity study on the developed EPL-NCs was conducted in mice for 14 days. The graphical summary of our study is presented in Supplementary Fig. 1.