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Eplerenone

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Overview

What is Eplerenone?

Eplerenone tablets contain eplerenone, a blocker of aldosterone binding at the mineralocorticoid receptor.

Eplerenone is chemically described as Pregn-4-ene-7,21-dicarboxylic acid, 9,11-epoxy-17-hydroxy-3-oxo-, γ-lactone, methyl ester, (7α,11α,17α)-. Its empirical formula is CHO and it has a molecular weight of 414.50. The structural formula of eplerenone is represented below:

Eplerenone is an odorless, white to off-white crystalline powder. It is very slightly soluble in water, with its solubility essentially pH-independent. The octanol/water partition coefficient of eplerenone is approximately 7.1 at pH 7.0.

Eplerenone tablets for oral administration contain 25 mg or 50 mg of eplerenone and the following inactive ingredients: lactose, microcrystalline cellulose, croscarmellose sodium, hypromellose, sodium lauryl sulfate, talc, magnesium stearate, titanium dioxide, polyethylene glycol, polysorbate 80, and iron oxide yellow and iron oxide red.



What does Eplerenone look like?



What are the available doses of Eplerenone?

Tablets: 25 mg, 50 mg ()

What should I talk to my health care provider before I take Eplerenone?

How should I use Eplerenone?

Eplerenone is indicated to improve survival of stable patients with left ventricular (LV) systolic dysfunction (ejection fraction ≤40%) and clinical evidence of congestive heart failure (CHF) after an acute myocardial infarction (MI).

Initiate treatment at 25 mg once daily and titrate to the recommended dose of 50 mg once daily, preferably within 4 weeks as tolerated by the patient.

Once treatment with eplerenone has begun, adjust the dose based on the serum potassium level as shown in Table 1.


What interacts with Eplerenone?

Sorry No Records found


What are the warnings of Eplerenone?

Sorry No Records found


What are the precautions of Eplerenone?

Sorry No Records found


What are the side effects of Eplerenone?

Sorry No records found


What should I look out for while using Eplerenone?

For all patients:

For the treatment of hypertension:


What might happen if I take too much Eplerenone?

No cases of human overdosage with eplerenone have been reported. Lethality was not observed in mice, rats, or dogs after single oral doses that provided C exposures at least 25 times higher than in humans receiving eplerenone 100 mg/day. Dogs showed emesis, salivation, and tremors at a C 41 times the human therapeutic C, progressing to sedation and convulsions at higher exposures.

The most likely manifestation of human overdosage would be anticipated to be hypotension or hyperkalemia. Eplerenone cannot be removed by hemodialysis. Eplerenone has been shown to bind extensively to charcoal. If symptomatic hypotension should occur, supportive treatment should be instituted. If hyperkalemia develops, standard treatment should be initiated.


How should I store and handle Eplerenone?

Eplerenone tablets, 25 mg, are yellow diamond biconvex film-coated tablets. They are debossed with "G" on one side and "25mg" on the other. They are supplied as follows:Eplerenone tablets, 50 mg, are yellow diamond biconvex film-coated tablets. They are debossed with "G" on one side and "50mg" on the other. They are supplied as follows:Eplerenone tablets, 25 mg, are yellow diamond biconvex film-coated tablets. They are debossed with "G" on one side and "25mg" on the other. They are supplied as follows:Eplerenone tablets, 50 mg, are yellow diamond biconvex film-coated tablets. They are debossed with "G" on one side and "50mg" on the other. They are supplied as follows:


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Clinical Information

Chemical Structure

No Image found
Clinical Pharmacology

Eplerenone binds to the mineralocorticoid receptor and blocks the binding of aldosterone, a component of the renin-angiotensin-aldosterone-system (RAAS). Aldosterone synthesis, which occurs primarily in the adrenal gland, is modulated by multiple factors, including angiotensin II and non-RAAS mediators such as adrenocorticotropic hormone (ACTH) and potassium. Aldosterone binds to mineralocorticoid receptors in both epithelial (e.g., kidney) and nonepithelial (e.g., heart, blood vessels, and brain) tissues and increases blood pressure through induction of sodium reabsorption and possibly other mechanisms.

Eplerenone has been shown to produce sustained increases in plasma renin and serum aldosterone, consistent with inhibition of the negative regulatory feedback of aldosterone on renin secretion. The resulting increased plasma renin activity and aldosterone circulating levels do not overcome the effects of eplerenone.

Eplerenone selectively binds to human mineralocorticoid receptors relative to its binding to recombinant human glucocorticoid, progesterone, and androgen receptors.

Non-Clinical Toxicology
For all patients:

For the treatment of hypertension:

See .

The following adverse reactions are discussed in greater detail in other sections of the labeling:

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Reference

This information is obtained from the National Institute of Health's Standard Packaging Label drug database.
"https://dailymed.nlm.nih.gov/dailymed/"

While we update our database periodically, we cannot guarantee it is always updated to the latest version.

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Professional

Clonazepam Description Each single-scored tablet, for oral administration, contains 0.5 mg, 1 mg, or 2 mg Clonazepam, USP, a benzodiazepine. Each tablet also contains corn starch, lactose monohydrate, magnesium stearate, microcrystalline cellulose, and povidone. Clonazepam tablets USP 0.5 mg contain Yellow D&C No. 10 Aluminum Lake. Clonazepam tablets USP 1 mg contain Yellow D&C No. 10 Aluminum Lake, as well as FD&C Blue No. 1 Aluminum Lake. Chemically, Clonazepam, USP is 5-(o-chlorophenyl)-1,3-dihydro-7-nitro-2H-1,4-benzodiazepin-2-one. It is a light yellow crystalline powder. It has the following structural formula: C15H10ClN3O3 M.W. 315.72
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Interactions

Interactions

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