ドネペジル

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

  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。

  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。

ドネペジル 化学特性,用途語,生産方法

• 用途

  中枢性可逆的アセチルコリンエステラーゼ（AChE）阻害薬アルツハイマー型認知症治療薬。中枢性可逆的アセチルコリンエステラーゼ（AChE）阻害薬として実用化された。認知症状の改善作用をもつ。

• 効能

  認知症治療薬, アセチルコリンエステラーゼ阻害薬

• 説明

  Donepezil is another “nonclassic,” centrally acting, reversible, noncompetitive AChEI that was approved in 1997 for treatment of mild-to-moderate AD and dementia. Its selectivity for AChE is 570- to 1,250-fold that for butyrylcholinesterase, and it also exhibits greater affinity for brain AChE than for AChE in the periphery.

• 使用

  Acetylcholine is a neurotransmitter involved in neural signaling throughout the body. Donepezil is a reversible acetylcholinesterase inhibitor that readily crosses the blood-brain barrier to reduce the breakdown of acetylcholine. It has a half-life in circulation of about 70 hours. As acetylcholine modulates plasticity, excitability, and arousal in the central nervous system, donepezil is commonly used in the treatment of Alzheimer’s disease to improve cognition, memory, and behavior. In this way, it is intended to prevent or reverse dementia. Studies on these effects have been equivocal, indicating that more research into the therapeutic potential of donepezil is warranted.[Cayman Chemical]

• 定義

  ChEBI: Donepezil is a centrally acting reversible acetyl cholinesterase inhibitor. Its main therapeutic use is in the treatment of Alzheimer's disease where it is used to increase cortical acetylcholine.

• 一般的な説明

  Donepezil, (±)-2,3-dihydro-5,6-dimethoxy-2-[[1-(phenylmethyl)-4-piperidinyl]methyl]-1H-inden-1-one (Aricept), commonly referred to in the literature asE2020, is a reversible inhibitor of AChE. It is indicated forthe treatment of symptoms of mild-to-moderate Alzheimerdisease. Donepezil is approximately 96% bound to plasmaproteins, with an elimination half-life of 70 hours. It is metabolizedprincipally by the 2D6 and 3A4 isozymes of theP450 system.

• 代謝

  When compared to tacrine, donepezil exhibits greater CNS AChE selectivity, longer elimination half-life (70–104 hours in subjects older than 55 years) and little or no potential for hepatotoxicity. Donepezil is metabolized by CYP2D6 and CYP3A4 via demethylation, debenzylation, hydroxylation, oxidation to the cis-N-oxide, and glucuronidation. The 6-O-desmethyl metabolite accounts for 11% of a dose, and it exhibits AChE inhibitory activity comparable to that of the parent compound.

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