テルビナフィン塩酸塩

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

  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。

  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。

  P302+P352：皮膚に付着した場合：多量の水と石鹸で洗うこと。

  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。

テルビナフィン塩酸塩 価格

テルビナフィン塩酸塩 化学特性,用途語,生産方法

• 外観

  白色～ほとんど白色粉末～結晶

• 用途

  スクアレンエポキシダーゼの 選択的阻害作用を示します。

• 用途

  スクアレンエポキシダーゼ選 択的阻害作用を示します。

• 効能

  抗真菌薬, エルゴステロール合成阻害薬

• 商品名

  テルビナフィン (岩城製薬); テルビナフィン塩酸塩 (岩城製薬); ラミシール (サンファーマ); ラミシール (サンファーマ); ラミシール (サンファーマ); ラミシール (サンファーマ)

• 説明

  Terbinafine hydrochloride is the first orally active allylamine antifungal with 30-fold greater antifungal activity than naftifine. The compound is indicated for the treatment of ringworm and fungal nail infections. Terbinatine hydrochloride acts on a single fungal enzyme, squalene epoxidase, interfering with the biosynthesis of ergosterols in cell membranes. Unlike other antifungal agents, it does not inhibit cytochrome P450 enzymes.

• 化学的特性

  Terbinafine hydrochloride is an off-white crystalline material that is soluble in polar organic solventssuch as methanol, ethanol, and methylene chloride but isonly slightly soluble in water. The highly lipophilic freebase is insoluble in water.

• 定義

  ChEBI: A hydrochloride obtained by reaction of terbinafine with one molar equivalent of hydrogen chloride.

• 適応症

  Terbinafine Hydrochloride is a synthetic allylamine antifungal agent, structurally related to naftifine. It inhibits fungal sterol biosynthesis by inhibiting the enzyme squalene 2,3-epoxidase. The deficiency of ergosterol and concomitant accumulation of squalene within the fungal cell results in cell death. It can be fungicidal or fungistatic, depending on the concentration used, and is effective against dermatophytes, Aspergillus, blastomycosis, and histoplasmosis. It is only minimally effective against Candida.

• 一般的な説明

  Terbinafine Hydrochloride is a synthetic allylamine derivative structurally related to naftifine, antifungal Terbinafine Hydrochloride blocks ergosterol biosynthesis by inhibition of squalene epoxidase, part of the sterol synthesis pathway for the fungal cell membrane.

• 生物活性

  Terbinafine is a broad-spectrum antifungal agent that has activity against T. rubrum, T. metagrophytes, T. verrucosum, E. floccosum, M. canis, A. fumigatus, and S. schenckii (MIC50s = 0.003-0.8 μg/ml). It selectively inhibits C. albicans squalene epoxidase over rat liver epoxidase (IC50s = 0.03 and 77 μM, respectively). Terbinafine (90-120 μM) induces cell cycle arrest at the G0/G1 phase in COLO 205 tumor cells and human umbilical vein endothelial cells (HUVECs). Formulations containing terbinafine have been used in the treatment of nail and skin fungal infections.

• Biochem/physiol Actions

  Mode of Action: Inhibits squalene epoxidase, preventing biosynthesis of ergosterol.
  Antimicrobial spectrum: Antifungal and antimycotic. Fungicidal against dermatopytes and some yeasts; fungistatic against Candida albicans.

• 副作用

  Adverse reactions include lens and retinal disturbances (red/green visual perception), metallic taste disturbance that may last up to 4 weeks after medication discontinuation, hepatoxicity, and pancytopenia. Five percent of patients will experience delayed gastric emptying with symptoms of nausea, fullness, and/or dyspepsia. Terbinafine does not appear to have any effect on the cytochrome P-450 systems (Check baseline CBC and LFTs; repeat if taken for >6 weeks).

• 合成

  Terbinafine is produced from olefin metathesis of 1,3-dichloropropene and neohexene followed by reaction with N-methyl-1-naphthalenemethanamine.

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