パロキセチン

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

  H302：飲み込むと有害

  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。

パロキセチン 化学特性,用途語,生産方法

• 用途

  パロキセチンは、脳内セロトニン神経系でセロトニンの再取り込みを阻害することで、脳内シナプス間隙に存在するセロトニン濃度が高まり、神経伝達能力が上がる。その結果、抗うつ作用及び抗不安作用を示すと考えられる。 また、ヒトP2X4受容体の強力な阻害作用（IC50=1.87μM）を有する。抗アロディニア作用を示し、神経因性疼痛の患者へ使用することが可能とみられる。

• 効能

  抗うつ薬, 選択的セロトニン再取り込み阻害薬

• 説明

  Paroxetine is a new highly selective serotonin reuptake inhibitor, mechanistically similar to fluoxetine, fluvoxamine and sertraline, introduced for the treatment of all types of depressive illnesses including depression associated with anxiety. It is reportedly non-sedating and non-stimulatory and compared to fluoxetine has a shorter duration of action (half-life of 24 hours versus 2 to 3 days). Paroxetine is also being investigated as a treatment for obesity, alcoholism and obsessive-compulsive disorders.

• 化学的特性

  White Solid

• 使用

  A istopically labelled selective serotonin reuptake inhibitor. Used as an antidepressant

• 生物学の機能

  Paroxetine (Paxil) has an elimination half-life of 21 hours and is also highly bound to plasma proteins, so it requires special attention when administered with drugs such as warfarin. Paroxetine is a potent inhibitor of the cytochrome P450 2D6 isoenzyme and can raise the plasma levels of drugs metabolized via this route. Of particular concern are drugs with a narrow therapeutic index, such as TCAs and the type 1C antiarrhythmics flecainide, propafenone, and encainide. Additionally, paroxetine itself is metabolized by this enzyme and inhibits its own metabolism, leading to nonlinear kinetics. Weight gain is higher with paroxetine than with the other SSRIs, and it tends to be more sedating, presumably because of its potential anticholinergic effects. Additionally, patients have had difficulty with abrupt discontinuation with this agent, reporting a flulike syndrome; this symptom can be avoided by tapering the medication.

• 一般的な説明

  In the structure of paroxetine (Paxil), an amino group, protonatedin vivo could H-bond with the–CH₂–O– unshared electrons.A β-arylamine–like structure with an extra aryl groupresults. The compound is a very highly selective SERT. Asexpected, it is an effective antidepressant and anxiolytic.

• 臨床応用

  In vitro binding studies suggest that paroxetine is a more selective and potent inhibitor of 5-HT reuptake than fluoxetine. The drug essentially has no effect on NE or dopamine reuptake, nor does it show affinity for other neuroreceptors. Its onset of action is 1 to 4 weeks.

パロキセチン 上流と下流の製品情報

パロキセチン 生産企業

Global(235)Suppliers

パロキセチン スペクトルデータ(¹HNMR)

61869-08-7, パロキセチン キーワード