フルボキサミン

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

  H302：飲み込むと有害

  H319：強い眼刺激

  H331：吸入すると有毒

  H335：呼吸器への刺激のおそれ

  H410：長期的影響により水生生物に非常に強い毒性

• 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。

  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。

  P271：屋外または換気の良い場所でのみ使用すること。

  P273：環境への放出を避けること。

  P280：保護手袋/保護衣/保護眼鏡/保護面を着用するこ と。

  P301+P312：飲み込んだ場合：気分が悪い時は医師に連絡する こと。

  P304+P340：吸入した場合：空気の新鮮な場所に移し、呼吸しやすい 姿勢で休息させること。

  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。

  P311：医師に連絡すること。

  P321：特別な処置が必要である（このラベルの．．． を見よ）。

  P330：口をすすぐこと。

  P391：漏出物を回収すること。

  P403+P233：換気の良い場所で保管すること。容器を密閉 しておくこと。

  P405：施錠して保管すること。

  P501：内容物/容器を．．．に廃棄すること。

フルボキサミン 価格

フルボキサミン 化学特性,用途語,生産方法

• 用途

  選択的セロトニン再取込み阻害薬（SSRI）うつ病やうつ状態の治療に用いられ，選択的セロトニン再取込み阻害薬（SSRI）に分類される。受容体遮断作用による副作用が少なく，半減期も長いことから，うつ病治療の第一選択薬となっている 。

• 効能

  抗うつ薬, 選択的セロトニン再取り込み阻害薬

• 化学的特性

  Colourless Oil

• 来歴

  The development of Fluvoxamine began in the 1970s, led by a research team at the Belgian pharmaceutical company Solvay. As the first successfully commercialized selective serotonin reuptake inhibitor (SSRI), fluvoxamine was designed and synthesized to exert its antidepressant effect by highly selectively inhibiting the presynaptic serotonin transporter, while exhibiting a higher safety profile compared to tricyclic antidepressants. This compound received its first clinical approval and market launch in Switzerland in 1983, marking the beginning of the SSRI era. Leading researchers in psychopharmacology, including C. M. van Hout, systematically elucidated the pharmacological properties and clinical efficacy of fluvoxamine. With the expansion of its clinical applications, fluvoxamine has also established a therapeutic role in indications such as obsessive-compulsive disorder, and during the COVID-19 pandemic, its re-evaluation as a potential immunomodulator sparked renewed research interest, reflecting its evolution from a classic antidepressant to a multi-purpose psychopharmacological drug.

• 一般的な説明

  The E-isomer of fluvoxamine (Luvox) can fold after protonation to the β-arylamine–like grouping. Here,the “extra” hydrophobic group is aliphatic.

• 危険性

  A poison.

• 作用機序

  Fluvoxamine is a highly selective inhibitor of 5-HT reuptake at the presynaptic membrane. Potency data from in vitro affinity studies suggest that fluvoxamine is less potent than the other SSRIs (e.g., paroxetine, sertraline, and citalopram). Its mechanism of action is similar to that of the other SSRIs. Fluvoxamine appears to have little or no effect on the reuptake of NE or dopamine. In vitro studies have demonstrated that fluvoxamine possesses virtually no affinity for other neuroreceptors. Its onset of action is similar to the other SSRIs (2–4 weeks).

• 薬物動態学

  Fluvoxamine is well absorbed, with a bioavailability of approximately 50%, probably because of first-pass metabolism. At steady-state doses, fluvoxamine demonstrates nonlinear pharmacokinetics over a dosage range of 100 to 300 mg/day, which results in higher plasma concentrations at higher doses than would be predicted by lower-dose kinetics (single dose, 15 hours; multiple dosing, 22 hours). Food does not significantly affect oral bioavailability. The mean apparent volume of distribution for fluvoxamine reflects its lipophilic nature, extensive tissue distribution, and protein binding. Fluvoxamine is distributed into breast milk. Fluvoxamine is preferentially metabolized by CYP2D6 in the liver by O-demethylation to its alcohol metabolite, which subsequently is oxidized to a carboxylic acid. Oxidative deamination and nine other metabolites have been identified, none of which shows significant pharmacological activity.

• 臨床応用

  Fluvoxamine is approved for use in obsessive-compulsive disorders.

• 副作用

  The adverse effects for fluvoxamine include symptoms of drowsiness, nausea or vomiting, abdominal pain, tremors, sinus bradycardia, and mild anticholinergic symptoms. Toxic doses could produce seizures and severe bradycardia.

• 薬物相互作用

  In vitro studies have shown fluvoxamine to be a potent inhibitor of CYP1A2, to inhibit CYP3A4 and CYP2C19, and to weakly inhibit CYP2D6. The bioavailability of fluvoxamine is significantly decreased in smokers compared with nonsmokers, possibly because of induction of CYP1A metabolism of fluvoxamine. Therefore, interactions with drugs that inhibit CYP1A2 also should be considered (e.g., theophylline and caffeine).

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