ブデソニド

危険有害性情報のコード(GHS)

• 絵表示(GHS)

  

• 注意喚起語

  Danger

• 危険有害性情報

  H312：皮膚に接触すると有害

  H317：アレルギー性皮膚反応を起こすおそれ

  H332：吸入すると有害

  H334：吸入するとアレルギー、喘息または、呼吸困難 を起こすおそれ

  H361：生殖能または胎児への悪影響のおそれの疑い

• 注意書き

  P201：使用前に取扱説明書を入手すること。

  P202：全ての安全注意を読み理解するまで取り扱わないこ と。

  P261：粉じん/煙/ガス/ミスト/蒸気/スプレーの吸入を避ける こと。

  P271：屋外または換気の良い場所でのみ使用すること。

  P272：汚染された作業衣は作業場から出さないこと。

  P280：保護手袋/保護衣/保護眼鏡/保護面を着用するこ と。

  P281：指定された個人用保護具を使用すること。

  P285：換気が十分でない場合には、呼吸用保護具を着用する こと。

  P302+P352：皮膚に付着した場合：多量の水と石鹸で洗うこと。

  P304+P340：吸入した場合：空気の新鮮な場所に移し、呼吸しやすい 姿勢で休息させること。

  P304+P341：吸入した場合：呼吸が困難な場合には、空気の新鮮な場 所に移し、呼吸しやすい姿勢で休息させること。

  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。

  P312：気分が悪い時は医師に連絡すること。

  P321：特別な処置が必要である（このラベルの．．． を見よ）。

  P322：特別な処置が必要である（このラベルの．．． を見よ）。

  P333+P313：皮膚刺激または発疹が生じた場合：医師の診断/手当てを 受けること。

  P342+P311：呼吸に関する症状が出た場合：医師に連絡すること。

  P363：汚染された衣類を再使用す場合には洗濯をすること。

  P405：施錠して保管すること。

  P501：内容物/容器を．．．に廃棄すること。

ブデソニド 価格

MSDS Information

• 16a(R),17-(Butylidenebis(oxy))-11b,21-dihydroxypregna-1,4-diene-3,20-dione

ブデソニド 化学特性,用途語,生産方法

• 用途

  吸入ステロイド薬気道の炎症を抑制し，喘息症状を改善する

• 効能

  喘息治療薬, 抗炎症薬, グルココルチコイド受容体作動薬

• 商品名

  ゼンタコート (ゼリア新薬工業); パルミコート (アストラゼネカ); パルミコート (アストラゼネカ); レクタブル (EAファーマ); レクタブル (EAファーマ)

• 説明

  Budesonide is composed of a 1:1 mixture of epimers of the 16,17-butylacetal, creating a chiral center. The 22R-epimer binds to the GR with higher affinity than does the 22S-epimer (Table 33.5). The butyl acetal chain provided the highest potency for the homologous acetal chains. Its rate of topical uptake into epithelial tissue is more than 100 times faster than that for hydrocortisone and dexamethasone. Approximately 85% of the IV administered dose of budesonide undergoes extensive first-pass hepatic metabolism by CYP3A4 to its primary metabolites, 6β-hydroxybudesonide and 16α-hydroxyprednisolone, which have approximately 1/100 the potency of budesonide. This is an important inactivation step in limiting budesonide's systemic effect on adrenal suppression.

• 化学的特性

  White Solid

• 使用

  Budesonide is a glucocorticoid steroid that activates the glucorcorticoid receptor with an EC50 value of 12.4 nM. Like other glucocorticoids, budesonide reduces inflammation and has utility in inflammatory diseases, like asthma and inflammatory bowel disease. Also like other glucocorticoids, budesonide may be abused by athletes.[Cayman Chemical]

• 定義

  ChEBI: A glucocorticoid steroid having a highly oxygenated pregna-1,4-diene structure. It is used mainly in the treatment of asthma and non-infectious rhinitis and for treatment and prevention of nasal polyposis.

• 適応症

  Budesonide is a synthetic corticosteroid having a potent glucocorticoid and weak mineralocorticoid activity. In standard in vitro and animal models, budesonide has an approximately 200-fold higher affinity for the glucocorticoid receptor and a 1000-fold higher topical antiinflammatory potency than cortisol.

• 一般的な説明

  Budesonide (Pulmicort Turbohaler,Rhinocort) is extensively metabolized in the liver, with 85%to 95% of the orally absorbed drug metabolized by the firstpasseffect. The major metabolites are 6β-hydroxybudesonideand 16α-hydroxyprednisolone, both with less than1% of the activity of the parent compound. Metabolism involvesthe CYP3A4 enzyme, so coadministration of budesonidewith a known CYP3A4 inhibitor should be monitoredcarefully.

• 生物活性

  Synthetic anti-inflammatory glucocorticoid that displays chemopreventive activity. Prevents formation of lung adenomas and adenocarcinomas in mice following inhalation or oral administration. Reverses DNA hypomethylation and modulates expression of cancer related genes.

• 作用機序

  Budesonide is an acetal formed between the 16α,17α-dihydroxyl groups and butanal. It is a nonhalogenated glucocorticoid with a 16,17-acetal that decreases the mineralocorticoid activity. In receptor affinity studies, the R-epimer was twofold more active than the S-epimer. Because the C-21 hydroxy is free, budesonide is not a prodrug and is active as administered. Only 34% of the metered dose of inhaled budesonide reaches the lung.

• 薬理学

  While budesonide is well absorbed from the GI tract, its oral bioavailability is low (about 10%), primarily because of extensive first-pass metabolism in the liver. Two major metabolites (16α-hydroxyprednisolone and 6β- hydroxybudesonide) are formed via the cytochrome P450 3A enzyme. In vitro studies on the binding of the two primary metabolites to the corticosteroid receptor indicate that their affinity for the receptor is less than 1% of that of the parent compound. It is hoped that use of this drug will avoid the long-term adverse reactions seen with systemically active corticosteroids.

• 臨床応用

  Recently, budesonide (Entecort EC) has been approved for the treatment of mildly to moderately active Crohn’s disease involving the ileum and/or ascending colon.

• 代謝

  Budesonide was metabolized three- to sixfold more rapidly than triamcinolone acetonide. The pharmacokinetics of budesonide after inhalation, oral, and IV administration displayed a mean plasma half-life of 2.8 hours and a systemic bioavailability of approximately 10% after oral administration (Table 33.5) (101). Pulmonary bioavailability is less than 40% after inhalation (70–75% after correction for the amounts of budesonide deposited in the inhalation device and oral cavity). No oxidative metabolism was observed in the lung. When given by inhalation, 32% of the dose is excreted in the urine as metabolites, 15% in the feces, and 41% of the dose remained in the mouthpiece of the inhaler. Following intranasal administration, very little of intranasal budesonide is absorbed from the nasal mucosa. Much of the intranasal dose (~60%) was swallowed, however, and remained in the GI tract to be excreted unchanged in the feces, whereas that fraction of the intranasal dose that was absorbed was extensively metabolized.

ブデソニド 上流と下流の製品情報

ブデソニド 生産企業

Global(632)Suppliers

ブデソニド スペクトルデータ(MS)

51333-22-3, ブデソニド キーワード