WordNet
- a drug that neutralizes or counteracts the effects of another drug
- a muscle that relaxes while another contracts; "when bending the elbow the triceps are the antagonist"
- a cellular structure that is postulated to exist in order to mediate between a chemical agent that acts on nervous tissue and the physiological response
- hormone that is one of the steroids of the adrenal cortex that influences the metabolism of sodium and potassium
PrepTutorEJDIC
- 対立する人,敵対者,競争相手(opponent)
- =sense organ / 受信装置
Wikipedia preview
出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2014/04/10 20:21:48」(JST)
[Wiki en表示]
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.
Contents
- 1 Mechanism of Action
- 2 Examples
- 3 See also
- 4 References
- 5 External links
Mechanism of Action
Aldosterone antagonists are, as the name suggests, receptor antagonists at the mineralocorticoid receptor. Antagonism of these receptors inhibits sodium reabsorption 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). [1]
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
- ^ Rossi S, editor. Australian Medicines Handbook 2006. Adelaide: Australian Medicines Handbook; 2006.
External links
- Aldosterone Antagonists at the US National Library of Medicine Medical Subject Headings (MeSH)
- MeSH list of agents 82000451
Antihypertensives: diuretics (C03)
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Sulfonamides
(and etacrynic acid) |
CA inhibitors (at PT)
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Loop (Na-K-Cl at AL)
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- Furosemide#
- Bumetanide
- Etacrynic acid
- Etozoline
- Muzolimine
- Piretanide
- Tienilic acid
- Torasemide
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Thiazides (Na-Cl at DCT,
Calcium-sparing)
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- Hydrochlorothiazide#
- Bendroflumethiazide
- Hydroflumethiazide
- Chlorothiazide
- Polythiazide
- Trichlormethiazide
- Cyclopenthiazide
- Methyclothiazide
- Cyclothiazide
- Mebutizide
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Thiazide-likes (primarily DCT)
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- Quinethazone
- Clopamide
- Chlortalidone
- Mefruside
- Clofenamide
- Metolazone
- Meticrane
- Xipamide
- Indapamide
- Clorexolone
- Fenquizone
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Potassium-sparing (at CD) |
ESC blockers
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- Amiloride#
- Triamterene
- Benzamil
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Aldosterone antagonists
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- Spironolactone#
- Eplerenone
- Potassium canrenoate
- Canrenone
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Osmotic diuretics (PT, DL) |
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Vasopressin receptor antagonists
(DCT and CD) |
- vaptans: Conivaptan
- Mozavaptan
- Satavaptan
- Tolvaptan
- tetracyclines: Demeclocycline
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Other |
- mercurial diuretic (Mersalyl, Meralluride)
- Theobromine
- Cicletanine
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- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III
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anat (a:h/u/t/a/l,v:h/u/t/a/l)/phys/devp/cell/prot
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noco/syva/cong/lyvd/tumr, sysi/epon, injr
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proc, drug (C2s+n/3/4/5/7/8/9)
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UpToDate Contents
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- 1. 駆出率低下を伴う心不全における薬理療法:作用機序pharmacologic therapy of heart failure with reduced ejection fraction mechanisms of action [show details]
…detrimental systems such as the renin-angiotensin-aldosterone axis. Mineralocorticoid receptor antagonists – Mineralocorticoid receptor antagonist (MRA) therapy has diuretic and blood pressure lowering effects …
- 2. 治療抵抗性高血圧の治療treatment of resistant hypertension [show details]
…adding a mineralocorticoid receptor antagonist (spironolactone or eplerenone) A potassium-sparing diuretic (eg, amiloride, triamterene) is an alternative if a mineralocorticoid receptor antagonist cannot …
- 3. 原発性アルドステロン症の治療treatment of primary aldosteronism [show details]
…corrected with potassium supplementation or a mineralocorticoid receptor antagonist (MRA) (eg, spironolactone or eplerenone) . The blood pressure response to spironolactone preoperatively often predicts the blood …
- 4. 心不全患者における高血圧治療treatment of hypertension in patients with heart failure [show details]
…elsewhere . In addition to fluid removal with loop diuretics, mineralocorticoid receptor antagonists (spironolactone [25 mg] or eplerenone at a dose of 50 mg/day) have been shown to improve survival in …
- 5. 駆出率低下を伴う心不全(HFrEF)を患う成人患者への追加薬物療法secondary pharmacologic therapy in heart failure with reduced ejection fraction hfref in adults [show details]
…for mineralocorticoid receptor antagonist (MRA) therapy for HFrEF are described above. For patients with HFrEF who are candidates for MRA therapy, one of the two available MRAs (spironolactone or eplerenone) …
English Journal
- Pro- versus Antinociceptive Nongenomic Effects of Neuronal Mineralocorticoid versus Glucocorticoid Receptors during Rat Hind Paw Inflammation.
- Li X1, Shaqura M, Mohamed D, Beyer A, Yamada S, Mousa SA, Schäfer M.
- Anesthesiology.Anesthesiology.2018 Apr;128(4):796-809. doi: 10.1097/ALN.0000000000002087.
- PMID 29356757
- Clinical Presentation, Predictors, and Outcomes Among Mineralocorticoid Receptor Antagonist (MRA)-Eligible Acute Heart Failure Patients in the Heart Function Assessment Registry Trial in Saudi Arabia (HEARTS).
- AlShamiri MQ1, AlHabib KF1, AlHabeeb W1, Raslan IR1, Ullah A1, Elasfar AA2,3, Alshaer F1, Albackr H1, Mimish L4, Almasood A5, AlGhamdi S6, Ghabashi A7.
- Angiology.Angiology.2018 Apr;69(4):323-332. doi: 10.1177/0003319717720051. Epub 2017 Jul 28.
- PMID 28750542
Japanese Journal
- Double-Blind, Randomized, Placebo-Controlled Trial Evaluating the Efficacy and Safety of Eplerenone in Japanese Patients With Chronic Heart Failure (J-EMPHASIS-HF)
- Circulation journal : official journal of the Japanese Circulation Society 82(1), 148-158, 2018-01
- NAID 40021420316
- Effect of Eplerenone on the Glomerular Filtration Rate (GFR) in Primary Aldosteronism: Sequential Changes in the GFR During Preoperative Eplerenone Treatment to Subsequent Adrenalectomy
Related Links
- Spironolactone was first developed over 50 years ago as a potent mineralocorticoid receptor (MR) antagonist with undesirable side effects; it was followed a decade ago by eplerenone, which is less potent but much more ...
- Mineralocorticoid receptor antagonists: emerging roles in cardiovascular medicine John W FunderPrince Henry's Institute, Clayton, Victoria, AustraliaAbstract: Spironolactone was first developed over 50 years ago as a potent ...
★リンクテーブル★
[★]
- 英
- aldosterone antagonist
- 同
- 抗アルドステロン薬、アルドステロン遮断薬、抗アルドステロン剤
- 関
- mineralocorticoid receptor antagonist
[★]
- 英
- mineralocorticoid receptor antagonist MRA
[★]
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