メチルナルトレキソン臭化物

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

  H301：飲み込むと有毒

  H400：水生生物に強い毒性

• 注意書き

  P273：環境への放出を避けること。

  P301+P310：飲み込んだ場合：直ちに医師に連絡すること。

メチルナルトレキソン臭化物 価格

メチルナルトレキソン臭化物 化学特性,用途語,生産方法

• 効能

  便秘治療薬, オピオイド受容体拮抗薬

• 説明

  The widespread efficacy of opioids in treating patients with moderate to severe acute and chronic pain is often accompanied by untoward side effects. In particular, opioid-induced bowel dysfunction is one of the more common and debilitating consequences afflicting up to 50% of patients. To counteract the peripherally-mediated adverse effects, opioid antagonists such as naloxone, naltrexone, and nalmephene are sometimes prescribed. The latest market entry exploits a strategic modification of naltrexone to lower its lipid solubility and increase its polarity: quaternization of the amine of naltrexone by methylation (methyl bromide) prevents crossing of the blood–brain barrier thereby creating an effective peripheral antagonist. Despite a loss of potency upon methylation, methylnaltrexone antagonizes opioid binding at m-opioid receptors with an IC₅₀ of 70 nM. Its affinity for k-opioid receptors is approximately eightfold less (IC₅₀＝ 575 nM) with no significant binding to d-opioid, orphanin, or non-opioid receptors. Methylnaltrexone bromide has been approved for the treatment of opioid-induced constipation in patients with advanced illness receiving palliative care.Regarding metabolism, methylnaltrexone bromide is eliminated primarily as intact drug (85% based on administered radioactivity) by slightly more renal than hepatic clearance.
  The most common adverse events were abdominal pain and flatulence followed by nausea, dizziness, and diarrhea.

• 化学的特性

  Pale Pink Solid

• 使用

  A metabolite of Naltrexone (N285750). Methylnaltrexone (MNTX), a selective μ-opioid receptor antagonist, functions as a peripherally acting receptor antagonist in tissues of the gastrointestinal tract.

• 一般的な説明

  Methylnaltrexone does not cross blood brain barrier and does not affect the opioid effects in the brain, such as analgesia. It is used to treat opioid-induced constipation (OIC).

メチルナルトレキソン臭化物 生産企業

Global(74)Suppliers

73232-52-7, メチルナルトレキソン臭化物 キーワード