Aldosterone receptor antagonists bind to and block the activation of aldosterone (mineralocorticoid) receptors on the epithelial cells in the late distal tubule and collecting duct of the kidney, thus preventing the synthesis of aldosterone-induced proteins which enhance Na+ retention and K+ and H+ secretion. A selective aldosterone receptor antagonist. Aldosterone receptor antagonists have recently been added to the American College of Cardiology/American Heart Association/Heart Failure Society of America 2017 guideline update for serving a role in the reduction in morbidity in patients with heart failure with preserved ejection fraction and an ejection fraction greater than 45%. “Upstream therapy” refers to the use of non-antiarrhythmic drugs (non-AADs) that modify the atrial substrate or target-specific mechanisms of AF to prevent the occurrence or recurrence of the arrhythmia. A selective aldosterone receptor antagonist. However, steroidal mineralocorticoid receptor antagonists (MRA) have a low safety profile, especially in CKD patients due to the high incidence of hyperkalemia. Aldosterone antagonists include: Eplerenone (Inspra) Spirinolactone (Aldactone) Be aware: Generic names are listed first. Concepts Eplerenone has a much lower affinity for progesterone and androgen receptors, resulting in a several-fold decrease in progestogenic and … Blockade of the biological effects of aldosterone has mostly been achieved with spironolactone and … RAAS Blockers, aldosterone receptor antagonists and statins have an … Eplerenone is used in the treatment of hypertension and congestive heart failure. Spironolactone is a nonselective aldosterone antagonist, and eplerenone is selective to the aldosterone receptor. Eplerenone binds to the mineralocorticoid receptor and blocks the binding of aldosterone, thereby decreasing sodium resorption and subsequently increasing water outflow. This leads to a decrease in blood pressure. Eplerenone is used in the treatment of hypertension and congestive heart failure. They also have other properties that can prevent heart failure from becoming worse, along with improving symptoms of heart failure. Aldosterone antagonists are diuretics or “water pills.” They may also be called aldosterone receptor blockers. Canadian brand names are in … Eplerenone binds to the mineralocorticoid receptor and blocks the binding of aldosterone, thereby decreasing sodium resorption and subsequently increasing water outflow. This group of drugs is often used as adjunctive therapy, in combination with other drugs, for the management of chronic heart failure. The aldosterone receptor antagonist (ARA) spironolactone contains elements of the progesterone molecule, and its use can be accompanied by progestogenic and antiandrogenic adverse effects, such as painful gynecomastia and other sexual side effects. These medicines cause the kidneys to get rid of extra water and they help to retain potassium by inhibiting secretion of potassium into distal tubule of the nephron[1]. This leads to a decrease in blood pressure. Eplerenone is a selective aldosterone receptor antagonist derived from spironolactone but with limited affinity for the progesterone and androgen receptors and therefore lacks sex-related adverse side effects (the Table). Blocking the mineralocorticoid receptor (MR) is one of the most effective ways of reducing blood pressure in patients with resistant hypertension and improving cardiovascular prognosis in patients with heart failure with reduced ejection fraction and left ventricular dysfunction after myocardial infarction. Action-blocks aldosterone receptors, binds with receptors fo some steroid hormones. Spironolactone Adverse Effects Adverse Effects-hyperkalemia, gynecomastia, menstrual irregularities, impotence, hirsutism, deepening of voice. Eplerenone is metabolized by cytochrome P450 (isoenzyme CYP3A4); inhibitors of CYP3A4, including ketoconazole, itraconazole, ribonavir, and clarithromycin, are associated with significant … An antimineralocorticoid, also known as a mineralocorticoid receptor antagonist (MCRA) or aldosterone antagonist, is a diuretic drug which antagonizes the action of aldosterone at mineralocorticoid receptors. Aldosterone receptor antagonists (ARAs) are a type of diuretic used in patients with CHF. There are currently two aldosterone antagonists commercially available in the United States, spironolactone and eplerenone. Blocking the aldosterone receptor therefore represents an important pharmacological strategy to avoid the clinical conditions deriving from heart failure (CHF) and chronic kidney disease (CKD).
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