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{{drugbox |
__NOTOC__
|width=200
{{Eplerenone}}
|image=eplerenone_structure.png
{{CMG}}; {{AE}} {{SS]]
|IUPAC_name =  pregn-4-ene-7,21-dicarboxylic acid, 9,11-epoxy-17-hydroxy-3-oxo, γ-lactone, methyl ester (7α, 11α, 17α)
|CAS_number = 107724-20-9
| ATC_prefix=C03
| ATC_suffix=DA04
| PubChem=5282131
| DrugBank=APRD00707
| C=24 | H=30 | O=6
|molecular_weight = 414.49
|bioavailability = 69%
|metabolism = [[hepatic]] ([[CYP3A4]])
|elimination_half-life = 3–5 hours
|excretion = 67% [[renal]]<br />32% [[biliary]]
|pregnancy_category = B3 ([[Australia|Aust]])
|legal_status = Schedule 4 ([[Australia|Aust]])
|routes_of_administration = oral
}}
{{CMG}}


'''''For patient information about Eplerenone, click [[Eplerenone (patient information)|here]].'''''


{{SB}} INSPRA<sup>®</sup>


==[[Eplerenone (patient information)|For patient information, click here]]==
==Overview==


'''Eplerenone''' ([[International Nonproprietary Name|INN]]) ({{pronEng|ɛpˈlɛrənoʊn}}) is an [[aldosterone antagonist]] used as an adjunct in the management of [[chronic heart failure]]. It is similar to [[spironolactone]], though it may be more specific for the [[mineralocorticoid receptor]] and is specifically marketed for reducing [[cardiovascular]] risk in patients following [[myocardial infarction]]. It is marketed by [[Pfizer]] under the trade name '''Inspra'''.
'''Eplerenone''' ([[International Nonproprietary Name|INN]]) ({{pronEng|ɛpˈlɛrənoʊn}}) is an [[aldosterone antagonist]] used as an adjunct in the management of [[chronic heart failure]]. It is similar to [[spironolactone]], though it may be more specific for the [[mineralocorticoid receptor]] and is specifically marketed for reducing [[cardiovascular]] risk in patients following [[myocardial infarction]]. It is marketed by [[Pfizer]] under the trade name '''Inspra'''.


==Clinical use==
==Category==
===Indications===
Eplerenone is specifically indicated for the reduction of risk of [[cardiovascular]] death in patients with [[heart failure]] and [[left ventricle|left ventricular]] dysfunction within 3–14 days of an acute [[myocardial infarction]], in combination with standard therapies and as treatment against hypertension.


===Contraindications===
[[Aldosterone antagonists]];[[Pfizer]];[[Lactones]];[[Epoxides]];[[Cardiovascular Drugs]]
Eplerenone is contraindicated in patients with [[hyperkalaemia]], severe [[renal impairment]] (creatinine Cl less than 30 ml/min), or severe hepatic impairment (Child-Pugh C). The manufacturer of eplerenone also contraindicates ( relative C.I. ) concomitant treatment with [[ketoconazole]], [[itraconazole]] or other [[potassium-sparing diuretic]]s (though the manufacturer still considers taking these drugs to be absolute C.I.) Potential benefits should be weighted against possible risks.


===Adverse effects===
==FDA Package Insert==
Common [[adverse drug reaction]]s (ADRs) associated with the use of eplerenone include: [[hyperkalaemia]], [[hypotension]], dizziness, altered renal function, and increased creatinine concentration.<ref>Rossi S, editor. [[Australian Medicines Handbook]] 2006. Adelaide: Australian Medicines Handbook; 2006</ref>


===Drug interactions===
====INSPRA (eplerenone) tablet, film coated ====
Eplerenone is primarily metabolised by the [[Cytochrome P450 oxidase|cytochrome P450]] enzyme [[CYP3A4]]. Thus the potential exists for adverse drug interactions with other drugs that induce or inhibit CYP3A4. Specifically, the concomitant use of the CYP3A4 potent inhibitors [[ketoconazole]] and [[itraconazole]] is contraindicated. Other CYP3A4 inhibitors including [[erythromycin]], [[saquinavir]], and [[verapamil]] should be used with caution. Other drugs that increase [[potassium]] concentrations may increase the risk of hyperkalaemia associated with eplerenone therapy, including salt substitutes,<ref>LoSalt [http://www.losalt.com/docs/lo_salt_web_advice.pdf Advisory Statement] (PDF)</ref> potassium supplements and other [[potassium-sparing diuretic]]s.


==General considerations==
'''  [[Eplerenone indications and usage|Indications and Usage]]'''
Due to the high risk of elevated potassium levels in individuals taking eplerenone, The United States FDA suggests routine checks on the individual's potassium level to screen for hyperkalemia.
'''| [[Eplerenone dosage and administration|Dosage and Administration]]'''
'''| [[Eplerenone dosage forms and strengths|Dosage Forms and Strengths]]'''
'''| [[Eplerenone contraindications|Contraindications]]'''
'''| [[Eplerenone warnings and precautions|Warnings and Precautions]]'''
'''| [[Eplerenone adverse reactions|Adverse Reactions]]'''
'''| [[Eplerenone drug interactions|Drug Interactions]]'''
'''| [[Eplerenone use in specific populations|Use in Specific Populations]]'''
'''| [[Eplerenone overdosage|Overdosage]]'''
'''| [[Eplerenone description|Description]]'''
'''| [[Eplerenone clinical pharmacology|Clinical Pharmacology]]'''
'''| [[Eplerenone nonclinical toxicology|Nonclinical Toxicology]]'''
'''| [[Eplerenone clinical studies|Clinical Studies]]'''
'''| [[Eplerenone how supplied storage and handling|How Supplied/Storage and Handling]]'''
'''| [[Eplerenone patient counseling information|Patient Counseling Information]]'''
'''| [[Eplerenone labels and packages|Labels and Packages]]'''


==See also==
==Mechanism of Action==
* [[Spironolactone]]
* [[Aldosterone antagonist]]


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 recombinant human mineralocorticoid receptors relative to its binding to recombinant human glucocorticoid, progesterone, and androgen receptors.
==References==
==References==
{{reflist|2}}


{{Reflist}}


{{Antihypertensives and diuretics}}
{{Diuretics}}
{{Mineralocorticoids}}


[[Category:Aldosterone antagonists]]
[[Category:Aldosterone antagonists]]
[[Category:Pfizer]]
[[Category:Lactones]]
[[Category:Epoxides]]
[[Category:Cardiovascular Drugs]]
[[Category:Drugs]]
[[Category:Drugs]]
{{WikiDoc Help Menu}}
{{WikiDoc Sources}}
[[de:Eplerenon]]

Revision as of 21:55, 28 February 2014

Eplerenone
INSPRA® FDA Package Insert
Indications and Usage
Dosage and Administration
Dosage Forms and Strengths
Contraindications
Warnings and Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Overdosage
Description
Clinical Pharmacology
Nonclinical Toxicology
Clinical Studies
How Supplied/Storage and Handling
Labels and Packages
Clinical Trials on Eplerenone
ClinicalTrials.gov

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: {{SS]]

For patient information about Eplerenone, click here.

Synonyms / Brand Names: INSPRA®

Overview

Eplerenone (INN) (Template:PronEng) is an aldosterone antagonist used as an adjunct in the management of chronic heart failure. It is similar to spironolactone, though it may be more specific for the mineralocorticoid receptor and is specifically marketed for reducing cardiovascular risk in patients following myocardial infarction. It is marketed by Pfizer under the trade name Inspra.

Category

Aldosterone antagonists;Pfizer;Lactones;Epoxides;Cardiovascular Drugs

FDA Package Insert

INSPRA (eplerenone) tablet, film coated

Indications and Usage | Dosage and Administration | Dosage Forms and Strengths | Contraindications | Warnings and Precautions | Adverse Reactions | Drug Interactions | Use in Specific Populations | Overdosage | Description | Clinical Pharmacology | Nonclinical Toxicology | Clinical Studies | How Supplied/Storage and Handling | Patient Counseling Information | Labels and Packages

Mechanism of Action

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

References

Template:Diuretics Template:Mineralocorticoids

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