betamethasone

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出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2017/04/28 21:40:36」(JST)

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英文文献

  • Comparison of efficacy of narrow band UVB therapies with UVB alone, in combination with calcipotriol, and with betamethasoneand calcipotriol in vitiligo.
  • Akdeniz N, Yavuz IH, Gunes Bilgili S, Ozaydın Yavuz G, Calka O.Author information Department of Dermatology, Atatürk University Faculty of Medicine , Erzurum , Turkey.AbstractObjective: The purpose of this study is to compare the efficacy of three therapies in the treatment of non-segmental vitiligo: a combination of topical calcipotriol, narrowband-ultraviolet B (NB-UVB), and betamethasone therapies; a combination of NB-UVB and topical calcipotriol; and NB-UVB alone. Material and methods: Forty-five patients with non-segmental vitiligo presenting to our Dermatology clinic were recruited to participate in the study. Patients were randomly divided into three groups. For each patient the size of the depigmented areas was assessed according to the rule of nines. The first group was treated with a combination of topical calcipotriol, NB-UVB, and betamethasone therapies. The second group was treated with a combination of NB-UVB and topical calcipotriol and third group was treated with NB-UVB alone. Since the patients' vitiligo lesions had similar phototypes, all patients were started with 0.1 j/cm(2), regardless of their skin phototype. The dose of NB-UVB was increased 10% in each session and no further increment was done after reaching 2.5 j/cm(2). Treatment effectiveness was evaluated according to the percentage improvement in repigmentation. The quality of life of the patients was measured by the Dermatology Life Quality Index (DLQI). Results: The patients were aged from 13 to 55 years (mean: 25.29). The duration of disease ranged from 3 months to 20 years. Family history was positive for vitiligo in 10 patients (22.2%). The percentage of recovery after treatment was 63.33% ± 7.55 in group 1, 60.67% ± 5.75 in group 2, and 46.67% ± 7.98 in group 3. There was no statistically significant difference between groups 1 and 2, and groups 2 and 3, but there was a statistically significant difference between groups 1 and 3 (p = 0.0048). Conclusions: In conclusion, NB-UVB-alone therapy and the combined therapies are effective treatment options in the treatment of vitiligo. Future studies with larger groups are warranted to confirm our results.
  • The Journal of dermatological treatment.J Dermatolog Treat.2014 Jun;25(3):196-9. doi: 10.3109/09546634.2013.777381. Epub 2013 May 6.
  • Objective: The purpose of this study is to compare the efficacy of three therapies in the treatment of non-segmental vitiligo: a combination of topical calcipotriol, narrowband-ultraviolet B (NB-UVB), and betamethasone therapies; a combination of NB-UVB and topical calcipotriol; and NB-UVB alone. Ma
  • PMID 23441902
  • 17β-carboxamide steroids - in vitro prediction of human skin permeability and retention using PAMPA technique.
  • Dobričić V1, Marković B2, Nikolic K2, Savić V3, Vladimirov S2, Cudina O2.Author information 1Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Belgrade, Vojvode Stepe 450, 11000 Belgrade, Serbia. Electronic address: vladimir@pharmacy.bg.ac.rs.2Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Belgrade, Vojvode Stepe 450, 11000 Belgrade, Serbia.3Department of Organic Chemistry, Faculty of Pharmacy, University of Belgrade, Vojvode Stepe 450, 11000 Belgrade, Serbia.AbstractIn this paper, twenty-two 17β-carboxamide steroids were synthesized from five corticosteroids (hydrocortisone, prednisolone, methylprednisolone, dexamethasone and betamethasone) in two steps. The first step was periodic acid oxydation of these corticosteroids to corresponding cortienic acids and the second step was amidation of thus obtained cortienic acids with esterified l-amino acids. These compounds are potential soft corticosteroids with local anti-inflammatory activity in the skin. Parallel artificial membrane permeability assay (PAMPA) was applied in order to predict permeability and retention of these compounds in human skin. Comparison of permeability and retention parameters between 17β-carboxamide steroids and corresponding corticosteroids was performed. Compounds with significantly higher retention were identified and the derivative that does not have significantly higher permeability was underlined. Molecular structures of all compounds were optimized by use of Gaussian semiempirical/PM3 method. Geometrical, thermodynamic, physicochemical and electronical molecular parameters of the optimized structures were calculated and quantitative structure-property relationship (QSPR) analysis was performed in order to explain permeability and retention of these compounds. ANN-, PLS- and MLR-QSPR models were created. Quality of these models was evaluated by commonly used statistical parameters and the most reliable models were selected. Analyzing descriptors in the selected models, main molecular properties that influence permeability and retention in the PAMPA artificial membrane were identified. Based on these data, further structural modifications could be applied in order to increase retention without significant increase of permeability, which can positively affect potential local anti-inflammatory activity of these compounds. Selected QSPR models could be used as in silico tool for predicting human skin permeability and retention of novel 17β-carboxamide steroids without performing PAMPA experiments.
  • European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences.Eur J Pharm Sci.2014 Feb 14;52:95-108. doi: 10.1016/j.ejps.2013.10.017. Epub 2013 Nov 12.
  • In this paper, twenty-two 17β-carboxamide steroids were synthesized from five corticosteroids (hydrocortisone, prednisolone, methylprednisolone, dexamethasone and betamethasone) in two steps. The first step was periodic acid oxydation of these corticosteroids to corresponding cortienic acids and th
  • PMID 24239478
  • Efficacy and maintenance strategies of two-compound formulation calcipotriol and betamethasone dipropionate gel (Xamiol® gel) in the treatment of scalp psoriasis: results from a study in 885 patients.
  • Saraceno R, Camplone G, D'Agostino M, De Simone C, Di Cesare A, Filosa G, Frascione P, Gabellini M, Lunghi F, Mazzotta A, Peris K, Scotto Di Luzio G, Calvieri S, Simonacci M, Chimenti S.Author information U.O.C. Dermatologia, University of Rome 'Tor Vergata' - PTV, Viale Oxford, 81, 00133 Rome , Italy.AbstractBackground: Previous studies showed the efficacy of a formulation containing calcipotriol and betamethasone dipropionate for the treatment of psoriasis. Objective: To investigate maintenance strategies of a formulation containing calcipotriol (50 µg/g) and betamethasone dipropionate (0.5 mg/g) for the treatment of scalp psoriasis. Materials and methods: Nine-hundred and four patients were screened and randomised on a 1:1 basis in two groups: maintenance of two applications per week (group A) versus on-demand therapy (group B). Clinical evaluation was performed at weeks 0, 2, 4, 8 and 12. Results: Eight-hundred and eighty-five patients were randomised: 441 in group A and 444 in group B. From week 2, both groups showed a significant clinical improvement compared with baseline; at weeks 8 and 12, group A demonstrated a higher clinical response compared with group B (p < 0.05). This difference was statistically significant (OR 0.47, 95% CI 0.37, 0.60). Conclusions: The maintenance of twice-weekly application versus on-demand treatment of calcipotriol/betamethasone dipropionate gel is more effective and is associated with a lower rate of relapse.
  • The Journal of dermatological treatment.J Dermatolog Treat.2014 Feb;25(1):30-3. doi: 10.3109/09546634.2013.800182. Epub 2013 May 23.
  • Background: Previous studies showed the efficacy of a formulation containing calcipotriol and betamethasone dipropionate for the treatment of psoriasis. Objective: To investigate maintenance strategies of a formulation containing calcipotriol (50 µg/g) and betamethasone dipropionate (0.5 mg/g) for
  • PMID 23621170

和文文献

  • IS-AC-3-6 Low-dose betamethasone infusions elicit partial lung maturation in a sheep model of pregnancy(Group 3 Perinatology 1,International Session Award Candidate)
  • Inflammatory Pseudotumor of the Brain Parenchyma with IgG4 Hypergammaglobulinemia
  • Betamethasone, but Not Tacrolimus, Suppresses the Development of Th2 Cells Mediated by Langerhans Cell-Like Dendritic Cells

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★リンクテーブル★
リンク元糖質コルチコイド」「ベタメタゾン」「betamethasone dipropionate」「betamethasone butyrate propionate
拡張検索betamethasone sodium phosphate」「betamethasone 17-valerate」「betamethasone acetate

糖質コルチコイド」

  [★]

glucocorticoid (Z), glucocorticoids
グルココルチコイド
副腎皮質副腎皮質ホルモン
  • 以下、内的に合成される糖質コルチコイドについて述べる

種類

分類

性状

  • ステロイド

産生組織

標的組織

生理作用

1. エネルギー代謝

糖新生においてグルコースの前駆体となるアミノ酸を肝臓に供給すべく動員する作用 (SP.894)

a. 糖代謝作用

糖新生の亢進
血糖上昇
肝細胞以外のグルコースの取り込みを抑制 (SP.894) ← 末梢でインスリンの作用に拮抗
グルコース-6-ホスファターゼの活性亢進 (SP.894)
グリコーゲンの合成亢進
血糖値の上昇に伴い、肝臓などでグルコースからグリコーゲンが作られる (SP.894)

b. タンパク質代謝作用

肝臓での糖新生の基質を末梢から供給する作用
肝細胞以外でのアミノ酸取り込み阻害 (SP.894)
特定のアミノ酸合成を阻害 (SP.894)
生理的範囲:(肝臓)同化作用が起こる、(肝臓以外)異化作用が起こる
ステロイド大量投与時:ほとんど異化作用が起こる→副作用につながる

c. 脂質代謝作用

  • 脂肪細胞に対して、インスリンの拮抗作用を持つが、一方で糖質コルチコイドにより血糖値が上昇する
  • 脂肪分解↑→血糖値↑ …(1)
脂肪細胞に対してグルコースの取り込みを抑制し、中性脂肪の生合成を抑制し、さらに大量の遊離脂肪酸とグリセロールを放出させる。肝臓でグリセロールからグルコースが合成される。 (SP.894)
  • 血糖値↑→脂肪合成↑ …(2)
血糖値の上昇によりインスリンが分泌され、脂肪細胞で脂肪の合成が促進される (SP.894)
  • (1)、(2)のいずれの反応が起こるかは体の部位によって異なり、脂肪分布の変化が生じる。
中心性肥満、満月様顔貌、バッファローハンプ

2. 電解質代謝作用

糖質コルチコイドの電解質コルチコイド様作用。
Na+再吸収↑、K+排泄↑
コルチゾールの電解質作用はアルドステロンの約1/400
コルチゾールの量    はアルドステロンの約 200倍
ゆえに、電解質コルチコイドの1/2の作用力を持つ

3. 水代謝作用

GFR↑、ADHに拮抗、細胞内への水移動の抑制→水利尿作用を有する。  尿崩症 + 副腎不全 → 多尿がいくらか改善されると考えて良いと思われる。仮面尿崩症

4. 骨・軟骨に対する作用

  • a. ビタミンDと拮抗して腸管からのCa吸収阻害 (SP.894)
  • b. 腎尿細管におけるCa再吸収阻害 (SP.894)
  • c. 骨芽細胞の分化・増殖を抑制 (SP.894)
糖質コルチコイドの大量投与→軟骨↓骨成長↓(活性型ビタミンD3に拮抗・尿細管Ca再吸収↓→PTH↑、骨芽細胞の分化抑制、タンパク質の異化作用↑)→骨粗鬆症、骨壊死 or 骨端線閉鎖を促進(←?要調査)
b.の機序で尿に排泄されるカルシウムが増加  →  高カルシウム尿症 → 尿路結石

5. 抗炎症作用

  • 胸腺やリンパ組織を萎縮させる → 炎症反応や免疫反応を抑制
リンパ球数の減少、白血球の遊走抑制、抗体産生低下、ヒスタミン放出抑制(局所の毛細血管拡張抑制) (SP.894)
末梢好中球数は増加する(YN.F-78) → 白血球増多症

SPC.330

  • a) 核内受容体を介してlipocortinを発現させ、これがphospholipase A2を阻害する。これにより、アラキドン酸の産生が抑制され、炎症を促進するロイコトリエンの産生も抑制される。
  • b) 末梢血Tリンパ球、単球、好酸球、好塩基球:骨髄からの放出減少と再分配(?)のため末梢血中では減少する。
  • c) 末梢血好中球:炎症部位への集合が抑制され(血管外への遊走が抑制される(GOO.1600))、末梢血中では増加する。
  • d) Bリンパ球はヘルパーT細胞が抑制されるために抗体産生能が減少する。
  • e) リンパ球などの細胞表面の立体構造を換えて抗体や補体の結合を抑制する。
  • f) 毛細血管(毛細管)の収縮により、血管の透過性は低下する。

6. 循環器

  • カテコールアミン・アンジオテンシンIIによる血管収縮作用の許容作用 → 糖質コルチコイドなしではその作用を十分に及ぼし得ない
欠乏症では血管のカテコールアミン・アンジオテンシンIIに対する感受性低下

7. 中枢神経系

  • 認知機能や情動を修飾 (SP.895)

8. 成長発達

  • 胎児期の消化酵素・リン脂質(肺胞表面の張力に関与)の合成に関与 (SP.895)
  • 小児期で骨や熱強訴域に直接作用して身長の伸びを抑制する (SP.895)

作用機序

免疫抑制(GOO. 657,674,1600)

糖質コルチコイドはリポコルチンを産生→リポコルチンはホスホリパーゼA2の活性を修飾→アラキドン酸産生↓

分泌調節

  • 1. 概日リズム
  • 2. フィードバック制御
    • 糖質コルチコイドがACTHCRHを抑制
  • 3. ストレス反応

臨床関連


  • 合成ステロイドホルモン

副作用

副腎皮質ホルモン剤
Table 59–2 Relative Potencies and Equivalent Doses of Representative Corticosteroids
COMPOUND ANTIINFLAMMATORY POTENCY Na+-RETAINING POTENCY DURATION OF ACTION* EQUIVALENT DOSE, MG
cortisol 1 1 S 20
cortisone 0.8 0.8 S 25
fludrocortisone 10 125 I
prednisone 4 0.8 I 5
prednisolone 4 0.8 I 5
6α-methylprednisolone 5 0.5 I 4
triamcinolone 5 0 I 4
betamethasone 25 0 L 0.75
dexamethasone 25 0 L 0.75


-グルココルチコイド
-グルココルチコイド
-glucocorticoid


ベタメタゾン」

  [★]

betamethasone
ベタメサゾン
ベタメタゾンリン酸エステルナトリウムリン酸ベタメタゾンナトリウム betamethasone sodium phosphate
酢酸ベタメタゾン betamethasone acetate
吉草酸ベタメタゾン betamethasone valerateベタメタゾン吉草酸エステル
ベタメタゾンジプロピオン酸エステルジプロピオン酸ベタメタゾン betamethasone dipropionate
ベタメタゾン酪酸エステルプロピオン酸エステル
リンデロン RinderonアンテベートCelestone
アンテベートアンフラベートエンペラシンケリグロールサクコルチンサレックスサンベタゾンステロネマセレスタミンダイプロセルディーピーポロンデキサンVGデルモゾールDPデルモゾールGデルモゾールトクダームトチプロベタゾンノルコットハイコートヒスタブロックヒズボットフロダームプラデスミンベクトミランベタセレミン、ベトネベートN、ベトネベート、ベトノバールG、ベルベゾロンFベルベゾロンリダスロンリネステロンリノロサールリンデロン-DPリンデロン-VGリンデロン-VリンデロンリンベタPFルリクールVGリンデロンA
鎮痛,鎮痒,収歛,消炎剤




betamethasone dipropionate」

  [★]

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betamethasone butyrate propionate」

  [★]

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betamethasone sodium phosphate」

  [★]

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betamethasone 17-valerate」

  [★]

17-吉草酸ベタメタゾン吉草酸ベタメタゾン

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betamethasone acetate」

  [★]

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