メチラポン

危険有害性情報のコード(GHS)

• 絵表示(GHS)

  

• 注意喚起語

  Warning

• 危険有害性情報

  H302：飲み込むと有害

  H315：皮膚刺激

  H319：強い眼刺激

  H335：呼吸器への刺激のおそれ

• 注意書き

  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。

  P264：取扱い後は皮膚をよく洗うこと。

  P264：取扱い後は手や顔をよく洗うこと。

  P270：この製品を使用する時に、飲食または喫煙をしないこ と。

  P301+P312：飲み込んだ場合：気分が悪い時は医師に連絡する 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。

  P305+P351+P338：眼に入った場合：水で数分間注意深く洗うこと。次にコ ンタクトレンズを着用していて容易に外せる場合は外す こと。その後も洗浄を続けること。

メチラポン 価格

メチラポン 化学特性,用途語,生産方法

• 効能

  診断補助薬 (下垂体機能判定)

• 商品名

  メトピロン (セオリアファーマ)

• 使用

  Metyrapone acts as a glucocorticoid synthesis inhibitor, maintaining stress-hormone levels.

• 生物活性

  Cytochrome P450 inhibitor. Blocks glucocorticoid synthesis via inhibition of steroid 11- β hydroxylase (CYP11B1) activity (IC 50 = 7.83 μ M). Also inhibits CYP3A4 and cytochrome P450-mediated ω / ω -1 hydroxylase activity.

• 作用機序

  Metyrapone (Metopirone) produces its primary pharmacological effect by inhibiting 11-β-hydroxylase, thereby causing diminished production and release of cortisol. The resulting reduction in the negative feedback of cortisol on the hypothalamus and pituitary causes an increase in corticotrophin release and in the secretion of precursor 11-deoxysteroids.

• 臨床応用

  Metyrapone is used in the differential diagnosis of both adrenocortical insufficiency and Cushing’s syndrome (hypercortisolism). The drug tests the functional competence of the hypothalamic–pituitary axis when the adrenals are able to respond to corticotrophin; that is, when primary adrenal insufficiency has been ruled out.
  After metyrapone administration, a patient with a disease of pituitary origin cannot achieve a compensatory increase in the urinary excretion of 17-hydroxycorticosteroids or 11-deoxysteroids. Moreover, if pituitary corticotrophin is suppressed by an autonomously secreting adrenal carcinoma, there will be no increase in response to metyrapone. On the other hand, if pituitary corticotrophin secretion is maintained, as occurs in adrenal hyperplasia, the inhibition of corticoid synthesis produced by metyrapone will stimulate corticotrophin secretion and the release of metabolites of precursor urinary steroids, which can be measured as 17-hydroxycorticosteroids. Metyrapone is now used less frequently in the differential diagnosis of Cushing’s syndrome because of the ability to measure plasma corticotrophin directly.
  The steroid-inhibiting properties of metyrapone have also been used in the treatment of Cushing’s syndrome, and it remains one of the more effective drugs used to treat this syndrome. However, the compensatory rise in corticotrophin levels in response to falling cortisol levels tends to maintain adrenal activity.This requires that glucocorticoids be administered concomitantly to suppress hypothalamic–pituitary activity. Although metyrapone interferes with 11β- and 18- hydroxylation reactions and thereby inhibits aldosterone synthesis, it may not cause mineralocorticoid deficiency because of the compensatory increased production of 11-desoxycorticosterone.

• 副作用

  Side effects associated with the use of metyrapone include gastrointestinal distress, dizziness, headache, sedation, and allergic rash. The drug should not be used in cases of adrenocortical insufficiency or when hypersensitivity reactions can be expected. When administered to pregnant women during the second or third trimesters, the drug may impair steroid biosynthesis in the fetus. Because metyrapone is relatively nontoxic, it is used in combination therapy with the more toxic aminoglutethimide to reduce its dosage.

メチラポン 上流と下流の製品情報

メチラポン 生産企業

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メチラポン スペクトルデータ(¹HNMR、IR1、IR2、MS、Raman)

54-36-4, メチラポン キーワード