トレプロスチニル

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

  H301：飲み込むと有毒

  H311：皮膚に接触すると有毒

  H331：吸入すると有毒

  H361：生殖能または胎児への悪影響のおそれの疑い

• 注意書き

  P201：使用前に取扱説明書を入手すること。

  P202：全ての安全注意を読み理解するまで取り扱わないこ 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。

  P280：保護手袋/保護衣/保護眼鏡/保護面を着用するこ と。

  P308+P313：暴露または暴露の懸念がある場合：医師の診断/手当てを 受けること。

  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。

トレプロスチニル 価格

トレプロスチニル 化学特性,用途語,生産方法

• 効能

  抗凝固薬, 血圧降下薬, 血管拡張薬, 血小板凝集抑制薬, プロスタグランジンI2受容体作動薬

• 商品名

  トレプロスト (持田製薬)

• 使用

  Synthetic analog of Prostacyclin (P839060). Antihypertensive. Treprostinil, marketed under the trade name Remodulin is a medication used to treat pulmonary arterial hypertension (PAH).

• 薬物動態学

  Treprostinil is rapidly absorbed from the subcutaneous site of infusion, with an almost 100% bioavailability and a mean half-life of 85 minutes (34 minutes for the IV infusion). The IV solution must be diluted with normal saline or sterile water before starting the infusion. Unlike epoprostenol, treprostinil is stable at room temperature for up to 5 years, with vasodilation action lasting from 4 to 6 hours, compared with the short, 2- to 3-minute action for epoprostenol. Because of its long life in the body, it can be administered under the skin with a microinfusion subcutaneous infusion pump rather than into the bloodstream and, thus, without hospitalization, as contrasted with the central IV infusion of epoprostenol.

• 臨床応用

  Treprostinil is a synthetic, stable form of prostacyclin for the treatment for advanced pulmonary hypertension with NYHA class III or IV symptoms as well as for late-stage peripheral vascular disease (PVD). Its sodium salt injectable form is administered either as a continuous subcutaneous infusion directly into the skin or, if the subcutaneous infusion is not tolerated, as a continuous IV infusion without an implanted catheter.

• 副作用

  Side effects include jaw pain, headaches, nausea, diarrhea, flushing, and localized pain at the delivery site under the skin. This pain has been reported as slight to severe irritation. Patients using the drug seem to ex-perience improvement in their condition, including decreased fatigue, decreased shortness of breath, and decreased pulmonary artery pressures, as well as overall improvement in quality of life.

• 合成

  A 250-mL, round-bottom flask with a magnetic stirrer was charged with treprostinil diethanolamine salt (4 g) and water (40 mL). The mixture was stirred to obtain a clear solution. Ethyl acetate (100 mL) was added to the clear solution. While stirring, 3M HCl (3.2 mL) was added slowly until pH=1 was attained. The mixture was stirred for 10 minutes, and the organic layer was separated. The aqueous layer was extracted with ethyl acetate (2×100 mL). The combined organic layers were washed with water (2×100 mL) and brine (1×50 mL) and dried over anhydrous Na2SO4. The ethyl acetate solution of treprostinil was filtered, and the filtrate was concentrated under a vacuum at 50° C. to give an off-white solid. The crude treprostinil was recrystallized from 50% ethanol in water (70 mL). The pure treprostinil was collected in a Buchner funnel by filtration, and the cake was washed with a cold 20% ethanolic solution in water. The cake of treprostinil was air-dried overnight and further dried in a vacuum oven at 50° C under high vacuum to afford 2.9 g of treprostinil (Yield 91.4%).

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81846-19-7, トレプロスチニル キーワード