ヒドロコルチゾン 化学特性,用途語,生産方法
外観
白色～ほとんど白色, 結晶性粉末～粉末
溶解性
水,エーテル,クロロホルムに難溶、エタノール(0.28mg/ml),メタノール,アセトンにやや可溶。メタノール、エタノール及びアセトンにやや溶けにくく、水に極めて溶けにくい。
解説
ヒドロコルチゾン，コルチゾールともいう．副じん皮質ホルモンの一つ．17α，21-ジヒドロキシプレグナ-4-エン-3,20-ジオンの微生物酸化で得られる．白色の結晶性粉末．分解点212～220 ℃．[α]"＋150～＋156°(ジオキサン)．メタノール，エタノール，アセトン，ジオキサンに微溶，エーテル，水に難溶．コルチゾンと同じく副じん皮質ホルモン作用，とくに糖質コルチコイド作用をもっているが，コルチゾンよりやや強い．リウマチ疾患，アレルギー性疾患，皮膚疾患などに用いられる．LD50 150 mg/kg(ラット，静注)．
用途
副腎皮質ホルモン剤です。
用途
薬理研究用。
用途
コルチゾールは、日本薬局方にはヒドロコルチゾンの名称で収載される、ステロイド系抗炎症薬（SAID）の1つとして臨床使用される。ステロイド系抗炎症薬は炎症反応を強力に抑制し、炎症の全ての過程に作用する。急性炎症、慢性炎症、自己免疫疾患、アレルギー性疾患、ショック、痛風、急性白血病、移植片拒絶反応などの治療に使用される。
効能
抗炎症薬, グルココルチコイド受容体作動薬
商品名
コートリル (ファイザー)
化学的特性
crystalline white powder
使用
Cortisol, or Hydrocortisone, is a steroid hormone, more specifically a glucocorticoid, produced by the zona fasciculata of the adrenal gland. Cortisol is released in response to stress and a low level
of blood glucocorticoids. Its primary functions are to increase blood sugar through gluconeogenesis; suppress the immune system; and aid in fat, protein and carbohydrate metabolism.
定義
ChEBI: A C21-steroid that is pregn-4-ene substituted by oxo groups at positions 3 and 20 and hydroxy groups at positions 11, 17 and 21. Cortisol is a corticosteroid hormone or glucocorticoid produced by zona fasciculata of the adrenal cortex,
which is a part of the adrenal gland. It is usually referred to as the "stress hormone" as it is involved in response to stress and anxiety, controlled by corticotropin-releasing hormone (CRH). It increases blood pressure and blood sugar, and reduces immun
responses
適応症
Hydrocortisone (Cortizone, Cortaid, Anusol-HC, Hytone, LactiCare-HC, Sarnol
HC, Penecort, Texacort, and many other branded products) may be purchased as a
generic drug.
一般的な説明
Hydrocortisone, 11β,17,21-trihydroxypregn-4-ene-3,20-dione, is the primary natural GCin humans. Despite the large number of synthetic GCs, hydrocortisone,its esters, and its salts remain a mainstay ofmodern adrenocortical steroid therapy and the standard forcomparison of all other GCs and MCs . It isused for all the indications mentioned previously.
健康ハザード
Cortisol Increases (1) protein catabolism (excepting liver) gluconeogenesis; (2) carbohydrate anabolism (liver); (3) blood sugar; (4) glucose absorption; (5) brain excitation; (6) spread of infections; (7)urinary glucose and nitrogen; (8) stress tolerance; (9) lactation; (10) water diuresis.
Regulates general adaptation syndrome, water balance, blood pressure, and hormone release.
Decreases (1) fat anabolism; (2) growth rate; (3) inflammation; (4) eosinophils; (5) lymphocytes; (6) antigen sensitivity; (7) respiratory quotient; (8) ketosis; (9) wound healing; (10) skin pigmentation; (11)RBC hemolysis.
接触アレルゲン
Hydrocortisone is the principal glucocorticoid hor-
mone produced by the adrenal cortex and is used topi-
cally or systemically. It belongs to the allergenic A
group. Marker of allergy is tixocortol pivalate.
作用機序
Hydrocortisone exhibits anti-shock, anti-allergy, and anti-inflammatory action. It raises
sugar content in the blood, increases potassium secretion, and lowers sodium excretion
from the body. It exhibits anti-metabolic action and reduces histamine synthesis in the
body.
臨床応用
Hydrocortisone is endogenous, and it has both glucocorticoid and mineralocorticoid activity. It is
the fundamental structure by which the glucocorticoid and mineralocorticoid activities of all other
corticosteroids are judged. Functional groups that are essential for both mineralocorticoid and
glucocorticoid activity include the pregnane skeleton with an all-trans backbone, the ring
A-en-one system (?4
-3-one ring A) and the 17β-ketol side chain (C-20-keto-C-21-hydroxy). The
glucocorticoid activity is enhanced by the C-11 and C-17 hydroxyl groups. Hydrocortisone can be
used to treat severe asthmatic attacks that do not respond to conventional treatment. It is
available as various ester forms.
安全性プロファイル
Poison by
純化方法
Recrystallise hydrocortisone from EtOH or isoPrOH. It is bitter tasting and has UV with max at 242 nm (log 4.20). Its solubility at 25o is: H2O (0.28%), EtOH (1.5%), MeOH (0.62%), Me2CO (0.93%), CHCl3 (0.16%), propylene glycol (1.3%) and Et2O (0.35%). It gives an intense green colour with conc H2SO4. [Wendler et al. J Am Chem Soc 72 5793 1950, Beilstein 8 IV 3422.]
ヒドロコルチゾン 上流と下流の製品情報
原材料
準備製品
6,9-Difluoropregn-4-ene-11,17,21-triol-3,20-dione17,21-diacetate
9-Bromo-11,17,21-trihydroxypregn-4-ene-3,20-dione17,21-diacetate
9-Bromo-11,17,21-trihydroxypregn-4-ene-3,20-dione 21-acetate
9-Fluoropregna-1,4-diene-11,17,21-triol-3,20-dione17,21-diacetate
6,9-Difluoro-11,16,17,21-tetrahydroxypregna-1,4-diene-3,20-dione 21-acetate
6-Fluoro-17,21-dihydroxypregna-4,9(11)-diene-3,20-dione 17,21-diacetate
21-アセチルオキシ-11α,17-ジヒドロキシプレグナ-4-エン-3,20-ジオン
9,11-Epoxy-6-fluoro-17,21-dihydroxypregn-4-ene-3,20-dione-17,21-diacetate
21-アセチルオキシ-6α,9-ジフルオロ-11β-ヒドロキシプレグナ-1,4,16-トリエン-3,20-ジオン
プレドニゾロン
9,11-Epoxypregn-4-ene-17,21-diol-3,20-dione 21-acetate
17,21-Diacetyloxy-9,11-epoxypregn-4-ene-3,20-dione
17α,21-ジアセトキシ-4,9(11)-プレグナジエン-3,20-ジオン
アネコルタブ酢酸エステル
プロピオン酸デプロドン
プレドニゾン
3,17,21-Trihydroxypregna-3,5,9(11)-trien-20-one 3,17,21-triacetate
酢酸 ヒドロコルチゾン
酪酸プロピオン酸ヒドロコルチゾン
17,21-ビス(アセチルオキシ)-6α,9-ジフルオロ-11β-ヒドロキシプレグナ-1,4-ジエン-3,20-ジオン
21-アセチルオキシ-9-フルオロ-11β-ヒドロキシプレグナ-1,4,16-トリエン-3,20-ジオン
Triamcinolone 21-acetate