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Eplerenone

Eplerenone
Drug information
Systematic (IUPAC) name
IUPAC namepregn-4-ene-7,21-dicarboxylic acid, 9,11-epoxy-17-hydroxy-3-oxo, γ-lactone, methyl ester (7α, 11α, 17α)
Chemical data
Mol. mass414.49
Bioavailability69%
Metabolismhepatic (CYP3A4)
Half-life6-8 hours
Excretion67% renal
32% biliary
Therapeutic considerations
Pregnancy cat B3 (Aust)
Legal status Schedule 4 (Aust), Rx only (US)
Routesoral

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Eplerenone (INN) (c-eniconɛpˈlɛrənoʊn) is an aldosterone antagonist used as an adjunct in the management of chronic heart failure. It is similar to the diuretic 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 is a potassium-sparing diuretic, meaning that it helps the body get rid of water but still keep potassium.

Eplerenone Video

Dr. George L. Bakris reports that two aldosterone receptor blocking drugs spironolactone and eplerenone have swiftly become important, second-line antihypertensive drugs for obese patients. Mitchel Zoler of Elsevier Global Medical News (EGMN) reports from a meeting of the American Diabetes Association in New York.
3.68 min. | 0 user rating		 Eplerenone reduced the risk of death and hospitalization in patients with mild heart failure in the EMPHASIS trial, Dr. Faiez Zannad explains. See the related Internal Medicine News story at tinyurl.com
5.03 min. | 0 user rating		 The aldosterone antagonist eplerenone worked equally well across all risk levels in patients with mild heart failure, according to a sub-analysis of the EMPHASIS-HF trial. Dr. Bertram Pitt discusses the results.
3.65 min. | 0 user rating		 www.theheart.org Dr Melissa Walton-Shirley sits down with Dr James Young to talk about the success of eplerenone, the benefits of CRT, the future of AV-delay--optimization techniques, the potential of the new HeartWare LVAD, and whether or not the end has come for natriuretic peptides.
23.08 min. | 5.0 user rating		 www.theheart.org Dr Bertram Pitt (University of Michigan, Ann Arbor) discusses the effect of eplerenone vs placebo on cardiovascular mortality or heart-failure hospitalization in subjects with NYHA class 2 chronic systolic heart failure: An analysis of the high-risk groups in the study population with Dr Robert Byrne (German Heart Center, Munich). Filmed during ESC 2011 in Paris on August 28.
7.27 min. | 0 user rating
Dr. Frank Lehmann-Horn speaks on periodic paralysis in Orlando, Florida at the Periodic Paralysis Association 2012 Conference. He addresses aspects of pathophysiology and management.
24.80 min. | 0 user rating		 www.cincinnatichildrens.org/story Sometimes Andrew Steele looks up his condition on the Internet and reads about other kids with Duchenne muscular dystrophy. Most boys who have the inherited muscular disease don't live past their 20s. But 12-year-old Andrew doesn't see himself as someone whose life is half over. He sees half a life left to figure out a cure. He is part of a research study at Cincinnati Children's testing a drug that could stall heart damage and buy time until researchers come up with a better treatment. "I believe one day there just might be a cure," Andrew says. "I'm that hopeful." Watch Andrew, his dad and his pediatric cardiologist talk about dealing with Duchenne muscular dystrophy.
2.60 min. | 5.0 user rating		 track.moreniche.com @# Endocrinology And Gynecomastia. What could you do when you woke up using a firmer chest tomorrow? Take into consideration the method that you would feel, experiencing possibly initially since childhood, forget about embarrassment. No reason to realize that heavy sweater...
1.28 min. | 0 user rating

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£1.50 A DAY HEART PILL TO HELP MORE VICTIMS - Express.co.uk Tweet this news
Express.co.uk---Eplerenone- is already available to treat certain patients. But makers Pfizer have announced that it has now been approved for use in those with chronic heart failure and LVEF, a specific type of heart failure. Heart failure patients could - Date : Wed, 04 Apr 2012 23:04:20 GMT
Adding eplerenone to standard therapy typically costs ¬£1.53 per day - PharmiWeb.com (press release) Tweet this news
PharmiWeb.com (press release)--[Walton Oaks], 4th April, 2012 – Pfizer today announced that Inspra (-eplerenone-), a selective aldosterone antagonist/mineralocorticoid receptor antagonist, has been approved in the UK for a new therapeutic indication - Date : Wed, 04 Apr 2012 15:07:10 GMT
화이자, 효자 상품 또 나왔네 - 헬스코리아뉴스 Tweet this news
헬스코리아뉴스--주민우 기자 화이자의 고혈압 치료제 '인스프라(Inspra/ -eplerenone-)'가 심부전질환에 효과가 있는 것으로 나타났다. 인스프라는 `알도스테론 수용체 차단제(Aldosterone Recepto - Date : Sun, 22 May 2011 23:45:58 GMT+00:00
Pfizer's Inspra shown to reduce AF in Ph IIIb trial - The Pharma Letter (subscription) Tweet this news
The Pharma Letter (subscription)--Global drugs behemoth Pfizer (NYSE: PFE) has reported results from a sub-analysis of the Phase IIIb EMPHASIS-HF trial (n=2737) showing that its already marketed Inspra (-eplerenone-) plus standard therapy statistically si - Date : Tue, 24 May 2011 09:05:22 GMT+00:00
Pfizer: Nearly 13000 Units Of Generic Drugs Stolen In Tennessee - Automated Trader Tweet this news
Automated Trader--The drugs included the antibiotic azithromycin, also known by its brand name Zithromax; the antidepressant sertraline, also known by its brand name Zoloft; and -eplerenone-, a treatment for high blood pressure. New York-based Pfizer is w - Date : Thu, 26 May 2011 16:46:46 GMT+00:00
Badanie EMPHASIS � eplerenon w łagodnej skurczowej niewydolności serca - Polskie Towarzystwo Kardiologiczne Tweet this news
Polskie Towarzystwo Kardiologiczne---Eplerenone- in patients with systolic heart failure and mild symptoms. N Engl J Med, 2011; 364: 11-21|17.01.2011 W przeprowadzonych przed kilku laty ... - Date : Mon, 17 Jan 2011 06:54:49 GMT+00:00
HFSA: Mixed Signals for Diastolic Heart Failure Drug - MedPage Today Tweet this news
MedPage Today--Diastolic function improved and markers of collagen turnover declined significantly after six months of treatment with -eplerenone- (Inspra). ... - Date : Thu, 16 Sep 2010 18:55:20 GMT+00:00
A Comparison of Outcomes in Patients in New York Heart Association Class II ... - Cardiosource Tweet this news
Cardiosource--The goal of the trial was to evaluate treatment with -eplerenone- compared to placebo among patients with mild to moderate heart failure that are at risk of ... - Date : Mon, 31 May 2010 02:16:03 GMT+00:00
Fármaco da Pfizer alcança objectivo em ensaio de fase final antes do previsto - RCM Pharma Tweet this news
RCM Pharma---...- doentes num ensaio de fase final que está a testar o seu medicamento Inspra® (-eplerenone-) como tratamento para a insuficiência cardíaca após aqueles que ... - Date : Fri, 28 May 2010 09:03:50 GMT+00:00
Проучване с препарат за сърдечна недостатъчност на Pfizer спряно предсрочно ... - DoctorBG.com Tweet this news
DoctorBG.com--Pfizer спира набирането на пациенти в проучването EMPHASIS-H, изследващо ефективността на селетивния алдостеронов инхибитор -eplerenone- (Inspra) п - Date : Sat, 29 May 2010 22:14:41 GMT+00:00

Antihypertensives: diuretics (C03)

Sulfonamides
(except EA)
CA inhibitors (at PT)Acetazolamide
Loop (Na-K-Cl at AL)Furosemide# * Bumetanide * Torasemide * Etacrynic acid
Thiazides (Na-Cl at DCT,
Calcium-sparing)		Hydrochlorothiazide# * Bendroflumethiazide * Hydroflumethiazide * Chlorothiazide * Polythiazide * Trichlormethiazide * Cyclopenthiazide * Methyclothiazide * Cyclothiazide * Mebutizide
Thiazide-likes (primarily DCT)Quinethazone * Clopamide * Chlortalidone * Mefruside * Clofenamide * Metolazone * Meticrane * Xipamide * Indapamide * Clorexolone * Fenquizone
Potassium-sparing (at CD)
ESC blockersAmiloride# * Triamterene * Benzamil
Aldosterone antagonistsSpironolactone# * Eplerenone * Potassium canrenoate * Canrenone
Osmotic diuretics (PT, DL)
Mannitol# * Urea
VAs (DCT and CD)
vaptans: Conivaptan * Mozavaptan * Satavaptan * Tolvaptan
tetracyclines: Demeclocycline
Other
mercurial diuretic (Mersalyl) * Theobromine * Cicletanine



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