アルドステロン拮抗薬
- 関
- Mineralocorticoid receptor antagonist(s)
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 corticosteroid hormone that is secreted by the cortex of the adrenal gland; regulates salt (sodium and potassium) and water balance
PrepTutorEJDIC
- 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)』「2014/11/28 08:20:45」(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 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). [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 |
- ethanol, isopropanol, 2M2B
- 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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English Journal
- Natural and synthetic corticosteroids inhibit uptake(2)-mediated transport in CNS neurons.
- Hill JE, Makky K, Shrestha L, Hillard CJ, Gasser PJ.SourceMarquette University, Department of Biomedical Sciences, Milwaukee, WI 53233, USA.
- Physiology & behavior.Physiol Behav.2011 Aug 3;104(2):306-11. Epub 2010 Nov 21.
- In addition to exerting actions via mineralocorticoid and glucocorticoid receptors, corticosteroids also act by inhibiting uptake(2), a high-capacity monoamine transport system originally described in peripheral tissues. Recent studies have demonstrated that uptake(2) transporters are expressed in t
- PMID 21081135
- Mineralocorticoid receptor blockade in chronic kidney disease.
- Volk MJ, Bomback AS, Klemmer PJ.SourceDepartment of Medicine, Division of Nephrology and Hypertension, University of North Carolina at Chapel Hill, Chapel Hill, NC, USA.
- Current hypertension reports.Curr Hypertens Rep.2011 Aug;13(4):282-8.
- Aldosterone antagonists have been highly successful in treating congestive heart failure and resistant hypertension. Until recently, therapies targeting the mineralocorticoid receptor in chronic kidney disease (CKD) have received little attention, largely because of the risk of hyperkalemia and the
- PMID 21465140
Japanese Journal
- 薬物治療--RAS系抑制薬とβ遮断薬 (特集 心不全診療--予防と治療の最前線)
- Inhibitory Effects of Dexamethasone on Hepatocyte Growth Factor–Induced DNA Synthesis and Proliferation in Primary Cultures of Adult Rat Hepatocytes
- Kimura Mitsutoshi,Moteki Hajime,Ogihara Masahiko
- Journal of Pharmacological Sciences 115(3), 390-398, 2011
- … The mineralcorticoid aldosterone (10−7 M) did not produce the same growth-inhibitory effects as dexamethasone (10−8 M). … The inhibitory effects of dexamethasone were reversed by treatment with the glucocorticoid-receptor antagonist mifepristone (RU486, 10−6 M) or a monoclonal antibody against glucocorticoid receptor (100 ng/mL). …
- NAID 130000663402
- SM-368229, a Novel Selective and Potent Non-steroidal Mineralocorticoid Receptor Antagonist With Strong Urinary Na+ Excretion Activity
- Nariai Tetsuro,Fujita Katsuya,Mori Masaya,Katayama Seiji,Hori Seiji,Matsui Kazuki
- Journal of Pharmacological Sciences 115(3), 346-353, 2011
- … In our search for safer and more effective MR antagonists, we identified SM-368229 as a novel non-steroidal MR antagonist. …
- NAID 130000663397
Related Links
- aldosterone [al-dos´ter-ōn, al´do-ster-ōn″] the main mineralocorticoid hormone secreted by the adrenal cortex, the principal biological activity of which is the regulation of electrolyte and water balance by promoting the retention of ...
- Aldosterone antagonist Aldosterone antagonist refers to drugs which antagonise the action of aldosterone at mineralocorticoid receptors. This group of drugs is ... Mode of action Aldosterone antagonists are, as the name suggests, receptor antagonists ...
Related Pictures
★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
- aldosterone antagonist
- 関
- アルドステロン拮抗薬、抗アルドステロン薬、アルドステロン遮断薬
[★]
- 英
- aldosterone antagonist
- 関
- アルドステロン拮抗薬、抗アルドステロン薬、抗アルドステロン剤
[★]
アルドステロン拮抗薬