リバスチグミン

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

  H300：飲み込むと生命に危険

  H411：長期的影響により水生生物に毒性

• 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。

  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。

  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。

  P391：漏出物を回収すること。

  P405：施錠して保管すること。

リバスチグミン 価格

リバスチグミン 化学特性,用途語,生産方法

• 外観

  無色～褐色、澄明の液体

• 溶解性

  エタノールに可溶(10mg/ml：ほとんど澄明以内)

• 用途

  強力なコリンエステラーゼ及 びブチリルコリンエステラーゼの阻害剤で す。

• 効能

  認知症治療薬, アセチルコリンエステラーゼ阻害薬

• 商品名

  イクセロン (ノバルティスファーマ); リバスタッチ (小野薬品工業)

• 使用上の注意

  不活性ガス封入

• 来歴

  Rivastigmine was discovered by Marta Weinstock-Rosin of the Department of Pharmacology at the Hebrew University of Jerusalem and sold to Novartis by Yissum for commercial development. Rivastigmine, sold under the brand name Exelon among others, is an acetylcholinesterase inhibitor used for the treatment of dementia associated with Alzheimer's disease and with Parkinson's disease.

• 使用

  Antidepressant

• 定義

  ChEBI: A carbamate ester obtained by formal condensation of the carboxy group of ethyl(methyl)carbamic acid with the phenolic OH group of 3-[(1S)-1-(dimethylamino)ethyl]phenol. A reversible cholinesterase inhibitor.

• 一般的な説明

  Rivastigmine (Exelon, EA 713) is apseudoirreversible noncompetitive carbamate inhibitor ofAChE. Although the half-life is approximately 2 hours,the inhibitory properties of this agent last for 10 hours becauseof the slow dissociation of the drug from the enzyme.The Food and Drug Administration (FDA) approved its usein mild-to-moderate Alzheimer disease in April 2000. InJuly 2007, rivastigmine was granted approval for use inmanaging mild-to-moderate dementia associated withParkinson disease.

• 薬物動態学

  Rivastigmine is a centrally selective, arylcarbamate AChEI that was approved in 2000 for oral administration in the treatment of AD. It has an elimination half-life of 1.4 to 1.7 hours but is able to inhibit AChE for up to 10 hours. Because of the slow dissociation of the carbamylated enzyme, it has been referred to as a pseudo-irreversible AChEI. Like donepezil, rivastigmine exhibits a low level of hepatotoxicity. It is rapidly and extensively hydrolyzed in the CNS by cholinesterase with minimal involvement of CYP450. The phenolic metabolite is excreted primarily via the kidneys.

• 代謝

  Rivastigmine is the tertiary amines that are rapidly absorbed from the gastrointestinal tract, as are tacrine, donepezil, and galanthamine, whereas quaternary ammonium compounds are poorly absorbed after oral administration. Nevertheless, quaternary ammonium compounds like neostigmine and pyridostigmine are orally active if larger doses are employed. Only the quaternary ammonium inhibitors do not readily enter the CNS. Because of their high lipid solubility and low molecular weight, most of the organophosphates are absorbed by all routes of administration; even percutaneous exposure can result in the absorption of sufficient drug to permit the accumulation of toxic levels of these compounds.

リバスチグミン 上流と下流の製品情報

リバスチグミン 生産企業

Global(353)Suppliers

リバスチグミン スペクトルデータ(¹HNMR)

123441-03-2, リバスチグミン キーワード