プレドニゾロン 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
エタノール,メタノールに可溶、アセトン,ジオキサンに微溶、クロロホルム,酢酸エチル,水に難溶。エタノール(1g/約30ml), アセトン(1g/50ml), クロロホルム(1g/180ml)に溶ける。エタノールにやや溶けやすく、アセトンにやや溶けにくく、水に極めて溶けにくい。
解説
プレドニゾロン,白色の結晶性粉末．分解点235 ℃．[α]D20"＋103°(ジオキサン)．メタノール，エタノールに易溶，アセトン，ジオキサンに微溶．酢酸エチル，水に難溶．副じん皮質ホルモン作用，とくに糖質コルチコイド作用が強く，リウマチ性関節炎，気管支ぜん息，皮膚炎などの治療に用いられる．
森北出版「化学辞典（第2版）
用途
副腎皮質ホルモン剤です。糖
質コルチコイドに二重結合を導入し、糖質コ
ルチコイド作用を強めています。鉱質コルチ
コイド作用を弱めた性質を有しています。
用途
副腎皮質ホルモン剤です。糖
質コルチコイドに二重結合を導入し、糖質コ
ルチコイド作用を強めています。鉱質コルチ
コイド作用を弱めた性質を有しています。
用途
プレドニゾロン試験用標準品。
用途
生理作用研究用。
効能
抗炎症薬, 抗リウマチ薬, グルココルチコイド受容体作動薬
製造
プレドニゾロン,デヒドロコルチゾンともいう．ヒドロコルチゾンの微生物酸化で，脱水素を行って得られる合成ステロイド．
毒性
LD50 ＞ 3500 mg/kg(マウス，皮下)．
商品名
プレドニゾロン (キョーリンリメディオ); プレドニゾロン (キョーリンリメディオ); プレドニゾロン (キョーリンリメディオ); プレドニゾロン (ニプロ); プレドニゾロン (マイラン製薬); プレドニゾロン (帝國製薬); プレドニゾロン (旭化成ファーマ); プレドニゾロン (東和薬品); プレドニゾロン (武田テバ薬品); プレドニゾロン (辰巳化学); プレドニゾロン (陽進堂); プレドニゾロン (陽進堂); プレドニン (塩野義製薬)
説明
Prednisolone is the active metabolite of the synthetic corticosteroid prednisone , which is used in the suppression of inflammation and autoimmunity, as well as in other conditions. It alters gene expression through both the glucocorticoid and mineralocorticoid receptors.
化学的特性
Crystalline Solid. soluble in organic solvents such as ethanol, DMSO, and dimethyl formamide, which should be purged with an inert gas. The solubility of prednisone in these solvents is approximately 3, 30, and 25 mg/ml, respectively.
使用
Prednisolone is used for the same indications as all corticosteroids: rheumatism, polyarthritis,
bronchial asthma, neurodermatitis, and eczema.
定義
ChEBI: Prednisolone is a glucocorticoid that is prednisone in which the oxo group at position 11 has been reduced to the corresponding beta-hydroxy group. It is a drug metabolite of prednisone. It has a role as an adrenergic agent, an anti-inflammatory drug, an antineoplastic agent, an immunosuppressive agent, a drug metabolite, an environmental contaminant and a xenobiotic. It is a glucocorticoid, an 11beta-hydroxy steroid, a 21-hydroxy steroid, a 17alpha-hydroxy steroid, a 20-oxo steroid, a 3-oxo-Delta(1),Delta(4)-steroid, a primary alpha-hydroxy ketone, a tertiary alpha-hydroxy ketone and a C21-steroid. It is functionally related to a Delta(1)-progesterone.
主な応用
Prednisolone is a synthetic corticosteroid with metabolically interconvertible with prednisone. It mediates its effect by acting on neurokinin 1 receptor. It is used to treat many conditions that cause inflammation, including inflammatory bowel disease (IBD).
一般的な説明
Prednisolone,Δ
1-hydrocortisone,11β,17,21-trihydroxypregna-1,4-diene-3,20-dione, hasless salt-retention activity than hydrocortisone, but some patients have more frequently experiencedcomplications such as gastric irritation and peptic ulcers.Because of low MC activity, it cannot be used alone for adrenalinsufficiency. Prednisolone is available in varioussalts and esters to maximize its therapeutic utility:
Prednisolone acetate, USP (21-acetate)
Prednisolone sodium phosphate, USP (21-sodiumphosphate)
Prednisolone sodium succinate, USP (21-sodiumsuccinate)
Prednisolone tebutate, USP (21-tebutate).
危険性
Causes sodium retention; may have side
effects similar to cortisone.
作用機序
Prednisolone is hydrocortisone to which has been added a ?1
double bond. This places two
double bonds in ring A, which flattens it and increases glucocorticoid action at the expense of
mineralocorticoid activity. Prednisolone has fourfold the glucocorticoid activity of hydrocortisone
while having approximately half its mineralocorticoid activity. In addition, prednisolone has an
increased duration of action compared to hydrocortisone, because the extra double bond in ring A
retards its metabolic reduction.
臨床応用
Prednisolone can be used to treat severe asthmatic attacks that do not respond to conventional
treatment, and it is available as the free alcohol for oral administration. The C-21 sodium
phosphate (Hydeltrasol) ester is available for parenteral use.
副作用
A prodrug of prednisolone is prednisone. It is the 11-keto analogue of prednisolone and must be converted in vivo to the active 11β-hydroxy compound, which is necessary to hydrogen bond to Asn-564 in the glucocorticoid receptor. Prednisone should not be used in patients with hepatic dysfunction, because their ability to reduce the 11-keto group with 11β-hydroxysteroid dehydrogenase to the active metabolite may be impaired.
Prednisolone is well tolerated by most people and can start to work very quickly. Side effects can be dependent on the dose and duration of treatment. Short courses of treatment often have fewer side effects than long term use. A Severe allergic reaction is a very rare side effect of prednisolone.
安全性プロファイル
A poison by
intravenous and subcutaneous routes.
Moderately toxic by ingestion and
intraperitoneal routes. Human teratogenic
effects by an unspecified route:
developmental abnormalities of the central
nervous system; effects on embryo or fetus:
fetal death, extra embryonic structures.
Human reproductive effects by an
unspecified route: stdlbirth. An experimental
teratogen. Experimental reproductive
effects. Human mutation data reported.
When heated to decomposition it emits
acrid smoke and irritating fumes.
プレドニゾロン 上流と下流の製品情報
原材料
準備製品