eplerenone (beta-blocker used in treating asthma)
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Category：Active Pharmaceutical Ingredients Own Brand：MT /MOQ:100KG /From China/ B2B only.
Introduction
CAS NO.864070-44-0
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Property
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Details
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Chemical Name
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Eplerenone
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CAS Number
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107724-20-9
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Molecular Formula
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\(C_{24}H_{30}O_6\)
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Molecular Weight
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414.49
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Molecular Structure
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Eplerenone has a steroid – like structure. It consists of a cyclopentanoperhydrophenanthrene ring system with various functional groups attached. There are carbonyl groups and a specific side – chain configuration that is crucial for its interaction with the mineralocorticoid receptor.
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Appearance
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Appears as a white to off – white crystalline powder.
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Solubility
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Practically insoluble in water. It has better solubility in organic solvents such as chloroform, methanol, and ethanol. This solubility characteristic influences the formulation of eplerenone into pharmaceutical products, often requiring the use of solubilizing agents or specific formulation techniques.
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Pharmacological Class
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Aldosterone antagonist
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Mechanism of Action
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Eplerenone binds selectively to the mineralocorticoid receptor in the cytoplasm of target cells, mainly in the distal convoluted tubules of the kidneys. By blocking the binding of aldosterone to this receptor, it inhibits the aldosterone – induced sodium reabsorption and potassium excretion in the kidneys. This leads to increased sodium and water excretion (natriuresis and diuresis), which helps in reducing blood volume and blood pressure. In the context of heart failure, it also has beneficial effects on cardiac remodeling and reduces the risk of adverse cardiac events.
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Medical Applications
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Hypertension: Approved for the treatment of hypertension. It can be used alone or in combination with other antihypertensive drugs such as thiazide diuretics, calcium channel blockers, or angiotensin – converting enzyme (ACE) inhibitors. Heart Failure: Eplerenone is also indicated for the treatment of patients with left ventricular systolic dysfunction after myocardial infarction. It helps in reducing morbidity and mortality associated with heart failure by improving cardiac function and reducing the harmful effects of aldosterone – mediated cardiac remodeling.
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Stability
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Stable under normal storage conditions, typically at room temperature in a dry place protected from light. However, exposure to high humidity, extreme temperatures, or strong oxidizing or reducing agents may cause degradation of the drug, potentially affecting its potency and safety.
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Safety Considerations
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Common side effects include hyperkalemia (elevated potassium levels in the blood), which can be a serious concern, especially in patients with impaired renal function or those taking other medications that can increase potassium levels, such as potassium – sparing diuretics or ACE inhibitors. Other side effects may include dizziness, fatigue, diarrhea, and hypotension. Eplerenone may also interact with other drugs. For example, drugs that inhibit CYP3A4 (the enzyme responsible for metabolizing eplerenone) can increase its blood levels and the risk of adverse effects.
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Empagliflozin (BI 10773) is an effective, selective SGLT-2 inhibitor with IC50 of 3.1 nM, which is more than 300 times higher than that of SGLT-1, 4, 5 and 6. Phase 3.
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