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スピロノラクトン

スピロノラクトン 化学構造式
52-01-7
CAS番号.
52-01-7
化学名:
スピロノラクトン
别名:
スピロノラクトン;アポラスノン;スピラクトン;スピロラング;アルダクトンA;ノイダブル;メルラクトン;ヨウラクトン;ラクデーン;ラッカルミン;マカシーA;(7α,17R)-7-(アセチルチオ)-17-ヒドロキシ-3-オキソプレグナ-4-エン-21-カルボン酸γ-ラクトン;ウルソニン;アルマトール;ベロスピロン;ピロラクトン;アルダクトン;スピロノラクトン (JP17)
英語化学名:
Spironolactone
英語别名:
Dira;Altex;Aldace;Acelat;Osiren;Osyrol;sc9420;Almatol;Aldopur;Alderon
CBNumber:
CB9743463
化学式:
C24H32O4S
分子量:
416.57
MOL File:
52-01-7.mol

スピロノラクトン 物理性質

融点 :
207-208 °C(lit.)
比旋光度 :
-37 º (c=1, CHCl3)
沸点 :
504.87°C (rough estimate)
比重(密度) :
1.1061 (rough estimate)
屈折率 :
-36 ° (C=1, CHCl3)
貯蔵温度 :
Store at RT
溶解性:
Practically insoluble in water, soluble in ethanol (96 per cent).
外見 :
Powder
色:
White to yellow-white
水溶解度 :
practically insoluble
Merck :
14,8760
CAS データベース:
52-01-7(CAS DataBase Reference)
NISTの化学物質情報:
Spironolactone(52-01-7)
EPAの化学物質情報:
Pregn-4-ene-21-carboxylic acid, 7-(acetylthio)-17-hydroxy- 3-oxo-, .gamma.-lactone, (7.alpha.,17.alpha.)-(52-01-7)
安全性情報
  • リスクと安全性に関する声明
  • 危険有害性情報のコード(GHS)
主な危険性  T,Xn,Xi
Rフレーズ  60-40-36/37/38
Sフレーズ  53-22-36/37/39-45-36-26
WGK Germany  3
RTECS 番号 TU4725000
TSCA  Yes
HSコード  29321900
有毒物質データの 52-01-7(Hazardous Substances Data)
毒性 LD50 in rats, mice, rabbits (mg/kg): 790, 360, 870 i.p. (IARC, 1980)
絵表示(GHS)
注意喚起語
危険有害性情報
コード 危険有害性情報 危険有害性クラス 区分 注意喚起語 シンボル P コード
H302 飲み込むと有害 急性毒性、経口 4 警告 P264, P270, P301+P312, P330, P501
H360 生殖能または胎児への悪影響のおそれ 生殖毒性 1A, 1B 危険
注意書き
P201 使用前に取扱説明書を入手すること。
P280 保護手袋/保護衣/保護眼鏡/保護面を着用するこ と。
P308+P313 暴露または暴露の懸念がある場合:医師の診断/手当てを 受けること。
P405 施錠して保管すること。

スピロノラクトン 価格 もっと(20)

メーカー 製品番号 製品説明 CAS番号 包装 価格 更新時間 購入
富士フイルム和光純薬株式会社(wako) W01LKTS6235 スピロノラクトン
Spironolactone
52-01-7 250mg ¥8800 2018-12-26 購入
富士フイルム和光純薬株式会社(wako) W01CHDASB-00019347 スピロノラクトン
Spironolactone
52-01-7 50mg ¥30000 2018-12-26 購入
東京化成工業 S0260 スピロノラクトン >98.0%(HPLC)
Spironolactone >98.0%(HPLC)
52-01-7 5g ¥19600 2018-12-04 購入
東京化成工業 S0260 スピロノラクトン >98.0%(HPLC)
Spironolactone >98.0%(HPLC)
52-01-7 1g ¥6900 2018-12-04 購入
関東化学株式会社(KANTO) 20746-1A スピロノラクトン 99%
Spironolactone 99%
52-01-7 1g ¥10700 2018-12-13 購入

スピロノラクトン 化学特性,用途語,生産方法

外観

白色~うすい黄褐色, 結晶~粉末

溶解性

エタノール、メタノール及びアセトンに溶け、水にほとんど溶けない。

用途

スピロノラクトン (spironolactone) はカリウム保持性利尿薬(抗アルドステロン薬)のひとつ。主に心不全、肝硬変性腹水、高血圧治療薬としてフロセミドやクロロチアジドと併用される。

用途

抗アルドステロン剤です。ア ルドステロンに拮抗し、ナトリウム排泄を促 進し、ナトリウム- カリウムイオン交感反応 抑制作用を示します。

用途

特に、アルドステロン分泌が異常亢進する原発性アルドステロン症では第一選択の治療薬である。

用途

アルドステロン拮抗作用物質 です。

効能

血圧降下薬, 利尿薬, アルドステロン拮抗薬

商品名

アルダクトン (ファイザー); スピロノラクトン (キョーリンリメディオ)

化学的特性

White to Off White Solid

使用

It is a synthetic 17-lactone steroid which is a renal competitive aldosterone antagonist in a class of pharmaceuticals called potassium-sparing diuretics, used primarily to treat ascites in patients with liver disease, low-renin hypertension, hypokalemia

使用

diuretic, aldosterone antagonist

使用

Spironolactone, an aldosterone-, and competitive androgen-receptor-antagonist and 5-alpharductase- inhibitor, indicated for the treatment of androgen dependent hirsutism, ideally in doses of 50 to 200 mg per day accompanying the intake of oral contraceptives with the same seven day break in between. Side effects concerning the length of the menstrual cycle, the increase of blood pressure or potassium levels may occur. Spironolactone is the number one drug in the treatment of hirsutism in the US (Farquhar et al., 2003). In other countries the prescription of spironolactone for the treatment of hirsutism may be off-label.

定義

ChEBI: A steroid lactone that is 17alpha-pregn-4-ene-21,17-carbolactone substituted by an oxo group at position 3 and an alpha-acetylsulfanyl group at position 7.

適応症

Spironolactone (Aldactone) is a compound originally developed as a mineralocorticoid antagonist and is used as a diuretic and antihypertensive agent. However, at high doses spironolactone binds to the androgen receptor. In clinical practice it is a weak androgen antagonist used to treat hirsutism in women by blocking testosterone binding to androgen receptors in hair follicles. Use of spironolactone in women for the treatment of hirsutism or male pattern baldness can result in elevated serum potassium levels; these levels should be checked within 1 month of starting the medication.

brand name

Aldactone (Searle);Airolactone;Aldactide 25;Aldactone-a;Aldazida;Aldonorm;Aldospirone;Alpamed;Altexide;Aporasnon;Carditan;Crk 635;Ct-spiro;Digi-aldopur;Dilakton;Hexalacton;Hokulaton;Hokuraton;Hydrospiron;Idrolattone;Lacilactone;Laralmin;Lasitone;Loractone;Mf 218d;Noidouble;Novospiroton;Novospirozine;Novosprioton;Novospriozine;Penantin;Pirolacton;Pirolcaton;Plarenil;Practon 50;Raudazida;Risicordin;Rolactone microfine;Sali-spiroctan;Sas 1060;Servilactone;Spiractin;Spiridazide;Spirix;Spiro comp;Spiro50-d;Spirodigital;Spiro-f;Spironomocompren;Spironone;Spironothiazide;Spiropal;Spirostada;Spirotone;Suprapuren;Synureticum;Tensoflex;Urosonine;Xenalone;Xeualon.

世界保健機関(WHO)

Spironolactone, an aldosterone antagonist, has been widely used for over 25 years in the treatment of hypertension and in the management of refractive oedema. Evidence that long-term administration of high doses are tumorigenic in the rat has recently led to restriction of its use by some national regulatory authorities although the significance of this finding with respect to clinical use is not certain. In 1987 spironolactone was transferred from the main list to the complementary list of the WHO Model List of Essential Drugs. (See also WHO comments for canrenone and potassium canrenoate). (Reference: (WHODI) WHO Drug Information, 2(1), , 1988)

生物学の機能

Spironolactone (Aldactone) is structurally related to aldosterone and acts as a competitive inhibitor to prevent the binding of aldosterone to its specific cellular binding protein. Spironolactone thus blocks the hormone-induced stimulation of protein synthesis necessary for Na+ reabsorption and K+ secretion. Spironolactone, in the presence of circulating aldosterone, promotes a modest increase in Na+ excretion associated with a decrease in K+ elimination. The observations that spironolactone is ineffective in adrenalectomized patients and that the actions of spironolactone can be reversed by raising circulating al-dosterone blood levels (surmountable antagonism) support the conclusion that spironolactone acts by competitive inhibition of the binding of aldosterone with receptor sites in the target tissue. Spironolactone acts only when mineralocorticoids are present.

一般的な説明

Spironolactone, 7α-(acetylthio)-17α-hydroxy-3-oxopregn-4-ene-3-one-21-carboxylic acidγ-lactone (Aldactone) is an aldosterone antagonist of greatmedical importance because of its diuretic activity.

危険性

Questionable carcinogen.

生物活性

Competitive mineralocorticoid (aldosterone) receptor antagonist that exhibits antihypertensive activity in vivo . Also displays antiandrogen activity and inhibits steroid hormone biosynthesis.

薬理学

Spironolactone (Aldactone) is the only diuretic that has been shown in a double-blind multicenter prospective clinical trial to improve survival in CHF. The addition of spironolactone to digitalis and an angiotensinconverting enzyme (ACE) inhibitor significantly improved survival among patients with chronic severe heart failure.
Spironolactone competitively inhibits the binding of aldosterone to cytosolic mineralocorticoid receptors in the epithelial cells in the late distal tubule and collecting duct of the kidney. Aldosterone enhances salt and water retention at the expense of enhanced renal K and H excretion. Spironolactone enhances diuresis by blocking sodium and water retention while retaining potassium. An obvious potential side effect is hyperkalemia, which is aggravated by the potassium-retaining properties of the ACE inhibitors. The likely concomitant use of the loop diuretic furosemide, which depletes K , dictates careful monitoring of serum potassium to avoid life-threatening rhythm disturbances.
There is also evidence for the existence of mineralocorticoid receptors on cardiac myocytes. This raises the intriguing possibility that spironolactone could mediate important direct effects on the myocardium in CHF.

臨床応用

Spironolactone has been used clinically in the following conditions:
1. Primary hyperaldosteronism. Used as an aid in preparing patients with adrenal cortical tumors for surgery.
2. Hypokalemia. Used in patients with low serum K+ resulting from diuretic therapy with other agents. Its use should be restricted to patients who are unable to supplement their dietary K+ intake or adequately restrict their salt intake or who cannot tolerate orally available KCl preparations.
3. Hypertension and congestive heart failure. Although spironolactone may be useful in combination with thiazides, the latter remain the drugs of first choice. Fixed-dose combinations of spironolactone and a particular thiazide (e.g., Aldactazide) generally offer no therapeutic advantage over either component given separately and tend to restrict the ability of the clinician to determine the optimal dosage of each drug for a particular patient.
4. Cirrhosis and nephrotic syndrome. Spironolactone is a mild diuretic and may be useful in treating the edema that occurs in these two clinical conditions, that is, when excessive K+ loss is to be avoided.

副作用

Serum electrolyte balance should be monitored periodically, since potentially fatal hyperkalemia may occur,especially in patients with impaired renal function or excessive K+ intake (including the K+ salts of coadministered drugs, e.g., potassium penicillin). Spironolactone can induce hyponatremia and in cirrhotic patients, metabolic acidosis.A variety of gastrointestinal disturbances may accompany spironolactone administration. These include diarrhea, gastritis, gastric bleeding, and peptic ulcers. Spironolactone is contraindicated in patients with peptic ulcers. Spironolactone may also cause elevated blood urea nitrogen, drowsiness, lethargy, ataxia, confusion, and headache. Gynecomastia and menstrual irregularity in males and females, respectively, can occur. Painful gynecomastia (directly related to dosage level and duration of therapy), which is generally reversible, may necessitate termination of therapy. Animal studies demonstrating tumorigenic potential support the clinical judgment that spironolactone alone or in combination should not be used for most patients who require diuretic therapy and its unnecessary use should be avoided.

安全性プロファイル

Poison by intraperitoneal route. Human reproductive effects by ingestion and possibly other routes: men, impotence and breast development; women, menstrual cycle changes or disorders, changes in the breasts and lactation. An experimental teratogen. Other experimental reproductive effects. Other human systemic effects by ingestion: agranulocytosis, kidney tubule damage, increased urine volume, and changes in blood sodium and calcium levels. Questionable carcinogen. When heated to decomposition it emits toxic fumes of SOx,. Used to treat hypertension, edema of congestive heart failure, cirrhosis, and kidney failure. 0

Veterinary Drugs and Treatments

Spironolactone may be used in patients with congestive heart failure who do not adequately respond to furosemide and ACE inhibitors, who develop hypokalemia on other diuretics, and are unwilling or unable to supplement with exogenous potassium sources. It may also be effective in treating ascites as it has less potential to increase ammonia levels than other diuretics.

代謝

Spironolactone is poorly absorbed after oral administration and has a delayed onset of action; it may take several days until a peak effect is produced. It has a somewhat slower onset of action than triamterene and amiloride (discussed later), but its natriuretic effect is modestly more pronounced, especially during long-term therapy. Spironolactone is rapidly and extensively metabolized, largely to the active metabolite canrenone. Canrenone and potassium canrenoate, its K+ salt, are available for clinical use in some countries outside the United States. Canrenone has a half-life of approximately 10 to 35 hours.The metabolites of spironolactone are excreted in both the urine and feces. New selective aldosterone receptor antagonists (SARA), such as eplerenone, have been developed but have not yet been introduced into clinical practice. Eplerenone and canrenone exhibit fewer steroidlike side effects (gynecomastia, hirsutism).

スピロノラクトン 上流と下流の製品情報

原材料

準備製品


スピロノラクトン 生産企業

Global( 198)Suppliers
名前 電話番号 ファックス番号 電子メール 国籍 製品カタログ 優位度
Rixing Chemical CO.,LTD
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Shenzhen Sendi Biotechnology Co.Ltd.
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Beijing Cooperate Pharmaceutical Co.,Ltd.
+86-10-60279497 +86(0)15646567669
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Henan Tianfu Chemical Co.,Ltd.
0371-55170693
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Mainchem Co., Ltd.
+86-0592-6210733
+86-0592-6210733 sales@mainchem.com CHINA 32452 55
Hefei TNJ Chemical Industry Co.,Ltd.
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Xiamen AmoyChem Co., Ltd
+86 (0)592-605 1114
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Shaanxi Yikanglong Biotechnology Co., Ltd.
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52-01-7(スピロノラクトン)キーワード:


  • 52-01-7
  • a-lactone,acetate
  • Aldace
  • Aldactide
  • Aldactone A
  • aldactonea
  • Alderon
  • Aldopur
  • Almatol
  • Altex
  • Aquareduct
  • cacidlactone
  • Deverol
  • Diatensec
  • Dira
  • Duraspiron
  • Euteberol
  • icacidlactone
  • Lacalmin
  • Lacdene
  • Laractone
  • Melarcon
  • Sprioderm
  • Supra-puren
  • Suracton
  • Uractone
  • Urusonin
  • Verospirone
  • Verospirone Opianin
  • Xenalon
  • 4,17ALPHA-PREGNEN-21-CARBOXYLIC ACID-17BETA-OL-3-ONE-7ALPHA-THIOL 21-17 GAMMA LACTONE 7-ACETATE
  • スピロノラクトン
  • アポラスノン
  • スピラクトン
  • スピロラング
  • アルダクトンA
  • ノイダブル
  • メルラクトン
  • ヨウラクトン
  • ラクデーン
  • ラッカルミン
  • マカシーA
  • (7α,17R)-7-(アセチルチオ)-17-ヒドロキシ-3-オキソプレグナ-4-エン-21-カルボン酸γ-ラクトン
  • ウルソニン
  • アルマトール
  • ベロスピロン
  • ピロラクトン
  • アルダクトン
  • スピロノラクトン (JP17)
  • 生化学
  • ステロイド
  • ステロイド (その他)
  • アルドステロン拮抗薬
  • 降圧薬
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