チボロン

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

  H319：強い眼刺激

• 注意書き

  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。

  P280：保護手袋/保護衣/保護眼鏡/保護面を着用するこ 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。

  P337+P313：眼の刺激が続く場合：医師の診断/手当てを受けること。

チボロン 価格

MSDS Information

• 17-Hydroxy-7alpha-methyl-19-norpregn-5(10)-en-20-yn-3-one

チボロン 化学特性,用途語,生産方法

• 効能

  卵胞ホルモン補充薬, エストロゲン受容体作動薬

• 説明

  Tibolone is a synthetic steroid with weak progestational and estrogenic properties, reportedly useful in controlling symptoms resulting from natural or surgical menopause. It has thus far shown no significant antithrombotic effect in post-menopausal patients.

• 化学的特性

  White Solid

• 使用

  A synthetic steroid with weak estrogenic, androgenic and progestogenic activity. A pharamceutical used in the treatment of menopausal syndrome

• 定義

  ChEBI: Estran-3-one with a double bond between positions 5 and 10, and bearing both an ethynyl group and a hydroxy group at position 17 (R-configuration). A synthetic steroid hormone drug which acts as an agonist at all five type I steroid hormon receptors, it is used in the prevention of postmenopausal osteoporosis and for treatment of endometriosis.

• 薬物動態学

  Raloxifene is rapidly absorbed following oral administration, with an estimated 60% absorption, but it has a very low bioavailability (2%), associated with extensive phase II metabolism. The metabolites are excreted via the bile, with potential enterohepatic recycling that could account for the interaction with cholestyramine. Supportive of the enterohepatic recycling is the half-life of 28 hours. Metabolism of raloxifene occurs to a great extent in the intestine and consists of glucuronide conjugation catalyzed by uridine diphosphate glucuronosyltransferase (UGT).

• 臨床応用

  Tibolone is a synthetic steroid that has been shown to increase bone mineral density similar to alendronate. The U.S. FDA approval is pending; overseas, this agent is used for the treatment of menopausal symptoms as well as the prevention of osteoporosis. It is considered to be a viable alternative to conjugated equine estrogen plus micronized progesterone.

• 副作用

  The most common reason for patient withdrawal from clinical trials was vaginal bleeding (also a common side effect when estrogen therapy is used).

• 合成

  The 1,4-diene intermediate was obtained by Birch reduction (lithium metal/liquid ammonia); subsequently, it was hydrolyzed under acidic conditions and protected by ketalization of the 3-keto group (e.g., to prepare a 3,3-dimethoxy derivative); then, the 17-hydroxyl group was oxidized to a ketone and a 17α-ethynyl group was introduced by nucleophilic addition of acetylene; finally, the 3-protecting group was removed by hydrolysis under mild acidic conditions to obtain Tibolone.

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