ミフェプリストン

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

  H360：生殖能または胎児への悪影響のおそれ

• 注意書き

  P201：使用前に取扱説明書を入手すること。

  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。

ミフェプリストン 価格

MSDS Information

• 11b-[p-(Dimethylamino)phenyl]-17b-hydroxy-17-(1-propynyl)estra-4,9-dien-3-one

ミフェプリストン 化学特性,用途語,生産方法

• 外観

  白色～うすい黄色～緑色粉末～結晶

• 用途

  ミフェプリストン (mifepristone) は、抗グルココルチコイド作用と抗アンドロゲン作用も持つ薬物。通常、ミソプロストールとの併用により使用される。妊娠7週（49日；受精からは5週間相当）以内の初期であれば胎児は膣から血塊となって排出され中絶される。

• 効能

  妊娠中絶薬, 避妊薬, プロゲステロン受容体拮抗薬

• 説明

  Mifepristone is an orally-active progesterone and glucocorticoid receptor antagonist indicated for use as a post-coital contraceptive. In addition to being an abortifacient, mifepristone is reported to be effective in the treatment of ocular hypertension; its potential therapeutic effect in hormone-dependent tumors is currently under investigation.

• 化学的特性

  Pale Yellow Solid

• 来歴

  Mifepristone (brand name: Mifeprex) is an abortion drug approved by the FDA in 2000 for the medical termination of pregnancy, up to 7 weeks of gestation, an extension extended to 10 weeks in 2016. A generic version of Mifeprex, mifepristone tablets (200 mg), was approved in 2019. The drug has been in use for 25 years. However, following a study by the Center for Ethics and Public Policy (EPPC) showing that nearly 11% of women using the drug experience serious adverse events, the FDA is reviewing the safety of mifepristone.

• 使用

  Mifepristone is a progesterone receptor antagonist with partial agonist activity. Abortifacient.

• 適応症

  Mifepristone is a progesterone receptor antagonist that has a high affinity for glucocorticoid receptors and little agonist effect.This drug has recently been approved for use in the United States for the treatment of hypercortisolism. At high doses, mifepristone blocks negative feedback of the hypothalamic–pituitary axis, thereby increasing endogenous corticotrophin and cortisol levels. Because mifepristone exerts its effects at the receptor level and not by altering glucocorticoid production, elevated serum cortisol and corticotrophin levels may not accurately reflect the effectiveness of the therapeutic regimen. Mifepristone does not inhibit cortisol binding to the mineralocorticoid receptor, so that the resulting corticotrophin disinhibition may cause potassium depletion. Thus, administration of a mineralocorticoid receptor antagonist such as spironolactone may be indicated with mifepristone. Hypoadrenalism, nausea, and drowsiness have been reported during prolonged administration of mifepristone.

• 世界保健機関（WHO）

  Mifepristone, an antiprogesterone used in combination with a prostaglandin for the termination of early pregnancy, was introduced in 1990. Use of the combination has been associated with episodes of coronary spasm that are attributed to administration of the prostaglandin and which have resulted in several cases of cardiac infarction and ventricular fibrillation. At least one of these incidents has been fatal.

• 生物活性

  Selective antagonist at progesterone (PR) and glucocorticoid (GR) receptors in vitro and in vivo . Is a silent antagonist at PR and has a higher affinity than progesterone. Has higher affinity for GR than dexamethasone.

• 薬物動態学

  Following oral administration, mifepristone is rapidly absorbed, with a peak plasmaconcentration in approximately 90 minutes , an oral bioavailability of approximately 70%, and a term inal elimination half-life of 18 hours. It is 98% protein bound, primarily to album in and α1-acid glycoprotein. Mifepristone is metabolized primarily via CYP3A4 pathways involving mono- and di-N-demethylation and terminal hydroxylation of the 17-propynyl chain. The fact that approximately 83% of the drug is recovered in the feces and 9% in the urine suggests a biliary route of elimination. Mifepristone also demonstrates antiglucocorticoid activity.

• 臨床応用

  An antiprogestin is a substance that competes with progesterone for its receptor and, ultimately, prevents progesterone from binding to and activating its receptor. Because progesterone is integral to the continuation of an early pregnancy, it is expected that antipro-gestins will interfere with pregnancy maintenance. In 1982, the first antiproges tin, mifepristone (RU 486), was reported. Mifepristone was shown to interrupt early stages of implantation and pregnancy in humans.

• 参考文献

  https://pubchem.ncbi.nlm.nih.gov/compound/mifepristone#section=Top
  https://www.drugbank.ca/drugs/DB00834
  https://www.drugs.com/cdi/mifepristone-tablets.html

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