aldosterone antagonists

アルドステロン拮抗薬

WordNet

1. a drug that neutralizes or counteracts the effects of another drug
2. a muscle that relaxes while another contracts; "when bending the elbow the triceps are the antagonist"
3. a corticosteroid hormone that is secreted by the cortex of the adrenal gland; regulates salt (sodium and potassium) and water balance

PrepTutorEJDIC

1. 対立する人,敵対者,競争相手(opponent)

Wikipedia preview

出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2014/12/29 14:11:21」(JST)

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Skeletal formulae of the aldosterone antagonists

An anti-mineralocorticoid, or an aldosterone antagonist, refers to a diuretic drug which antagonizes the action of aldosterone at mineralocorticoid receptors. This group of drugs is often used as adjunctive therapy, in combination with other drugs, for the management of chronic heart failure. Spironolactone, the first member of the class, is also used in the management of hyperaldosteronism (including Conn's syndrome) and female hirsutism.

Mechanism of Action

Aldosterone antagonists are, as the name suggests, receptor antagonists at the mineralocorticoid receptor. Antagonism of these receptors inhibits sodium resorption in the collecting duct of the nephron in the kidneys. This interferes with sodium/potassium exchange, reducing urinary potassium excretion and weakly increasing water excretion (diuresis).

In congestive heart failure, they are used in addition to other drugs for additive diuretic effect, which reduces edema and the cardiac workload.

Examples

Members of this class in clinical use include:

• Spironolactone
• Eplerenone - more specific than spironolactone on target
• Canrenone (canrenoate potassium)
• Prorenone (prorenoate potassium)
• Mexrenone (mexrenoate potassium)

See also

• Potassium-sparing diuretic
• Mineralocorticoid
• Corticosteroid
• Antiglucocorticoid

References

External links

• Aldosterone Antagonists at the US National Library of Medicine Medical Subject Headings (MeSH)
• MeSH list of agents 82000451

UpToDate Contents

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• 1. 収縮期心不全におけるアルドステロン拮抗剤の使用 use of aldosterone antagonists in systolic heart failure
• 2. 周産期心筋症：治療および予後 peripartum cardiomyopathy treatment and prognosis
• 3. 治療抵抗性高血圧の治療 treatment of resistant hypertension
• 4. 原発性アルドステロン症の治療 treatment of primary aldosteronism
• 5. 収縮能障害による心不全の治療の概要 overview of the therapy of heart failure due to systolic dysfunction

English Journal

• Reduced Risk of Hyperkalemia During Treatment of Heart Failure With Mineralocorticoid Receptor Antagonists by Use of Sacubitril/Valsartan Compared With Enalapril: A Secondary Analysis of the PARADIGM-HF Trial.

• Desai AS1, Vardeny O2, Claggett B1, McMurray JJ3, Packer M4, Swedberg K5, Rouleau JL6, Zile MR7, Lefkowitz M8, Shi V8, Solomon SD1.
• JAMA cardiology.JAMA Cardiol.2016 Nov 14. doi: 10.1001/jamacardio.2016.4733. [Epub ahead of print]
• Importance: Consensus guidelines recommend the use of mineralocorticoid receptor antagonists (MRAs) for selected patients with symptomatic heart failure and reduced ejection fraction (HFrEF) to reduce morbidity and mortality; however, the use of MRAs in combination with other inhibitors of the renin
• PMID 27842179

• Steroidal and Novel Non-steroidal Mineralocorticoid Receptor Antagonists in Heart Failure and Cardiorenal Diseases: Comparison at Bench and Bedside.

• Kolkhof P1, Jaisser F2, Kim SY3, Filippatos G4, Nowack C3, Pitt B5.
• Handbook of experimental pharmacology.Handb Exp Pharmacol.2016 Nov 10. [Epub ahead of print]
• Characterization of mice with cell-specific deletion or overexpression of the mineralocorticoid receptor (MR) shed a new light on its role in health and disease. Pathophysiological MR activation contributes to a plethora of deleterious molecular mechanisms in the development of cardiorenal diseases
• PMID 27830348

• Pharmacotherapy of Hypertension in Chronic Dialysis Patients.

• Georgianos PI1, Agarwal R2,3.
• Clinical journal of the American Society of Nephrology : CJASN.Clin J Am Soc Nephrol.2016 Nov 7;11(11):2062-2075. Epub 2016 Oct 24.
• Among patients on dialysis, hypertension is highly prevalent and contributes to the high burden of cardiovascular morbidity and mortality. Strict volume control via sodium restriction and probing of dry weight are first-line approaches for the treatment of hypertension in this population; however, a
• PMID 27797886

Japanese Journal

• Temporal Trends in Clinical Characteristics, Management and Prognosis of Patients With Symptomatic Heart Failure in Japan　– Report From the CHART Studies –

• Circulation Journal 79(11), 2396-2407, 2015
• NAID 130005104900

• Temporal Trends in Clinical Characteristics, Management and Prognosis of Patients With Symptomatic Heart Failure in Japan　– Report From the CHART Studies –

• Circulation Journal advpub(0), 2015
• NAID 130005098458

• Improved Long-Term Prognosis of Dilated Cardiomyopathy With Implementation of Evidenced-Based Medication　– Report From the CHART Studies –

• Circulation Journal 79(6), 1332-1341, 2015
• NAID 130005073161

Related Links

• Aldosterone Receptor Antagonists: Diuretics for Heart Failure

How It Works Aldosterone receptor antagonists are medicines that help the body get rid of extra water (diuretics). They also have other properties that can prevent heart failure from becoming worse, along with improving symptoms of heart failure

• Aldosterone Antagonists in the Treatment of Heart Failure

Purpose: The clinical benefits, adverse effects, pharmacokinetics, and recommendations for the appropriate use of the aldosterone antagonists spironolactone and eplerenone in patients with heart failure are reviewed. ...

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