アムプレナビル

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

  H302：飲み込むと有害

  H315：皮膚刺激

  H319：強い眼刺激

  H332：吸入すると有害

  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。

  P280：保護手袋/保護衣/保護眼鏡/保護面を着用するこ 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。

アムプレナビル 価格

アムプレナビル 化学特性,用途語,生産方法

• 外観

  白色～うすい褐色, 結晶性粉末～粉末

• 溶解性

  エタノール及びアセトンに溶け、水にほとんど溶けない。

• 効能

  抗ウイルス薬, HIVプロテアーゼ阻害薬

• 使用上の注意

  不活性ガス封入

• 説明

  Amprenavir was launched as Agenerase in the US for the treatment of AIDS patients in combination with approved agent antiretroviral nucleoside analogs. It is the fifth non-peptidic inhibitor of HIV-1 protease to be marketed in this indication after the last approved Neflinavir. Amprenavir, designed via a structure-based process, is the smallest molecule in the 《navir》 class and exhibits a reduced peptidic character. An improved process for preparation comprising four steps from a (1S, 2R)-2-hydroxy-3-aminopropylcarbamate has been developed. Amprenavir is a potent inhibitor of HIV-1 aspartyl protease (Ki = 0.6nM), an enzyme required by the virus to cleave pro-form polyproteins to structural proteins during the last stage in the replication process. The compound displays good oral bioavailability in humans and penetrates the CNS, which is an important advantage in long-term treatment. Its plasma half-life is approximately 10h. Treatment with Amprenavir in combination with nucleoside analog reverse transcriptase inhibitors considerably decreases viral load and restores CD4+ T-cell counts in patients with HIV infection.

• 化学的特性

  Off-White to Pale Yellow

• 使用

  A selective HIV protease inhibitor. An analogue of Ritonavir

• 適応症

  Amprenavir (Agenerase) is administered twice daily, providing the patient with an advantage over other protease inhibitors that must be taken more frequently (e.g., indinavir, saquinavir). Common side effects of am-prenavir include nausea, vomiting, diarrhea, and perioral paraesthesias. Rash occurs in approximately 20 to 30% of patients and can be mild or severe (Stevens- Johnson syndrome).

• 獲得抵抗性

  Mutations at position 50, 76 and 84 of the protease enzyme gene are associated with significantly reduced susceptibility.

• 一般的な説明

  Amprenavir is a second-generation drug derived from hydroxyethylamine sulfonamide.

• 応用例（製薬）

  A synthetic compound formulated as the calcium salt of the oral prodrug fosamprenavir.

• 薬物動態学

  Oral absorption: Not known/available
  C_max 700 mg + ritonavir 100 mg:c. 6.08 mg/L
  twice daily
  C_min 700 mg + ritonavir 100 mg:c. 2.12 mg/L
  twice daily
  Plasma half-life: c. 7.7 h
  Volume of distribution: c. 430 L
  Plasma protein binding: c. 90%
  Absorption
  Fosamprenavir is rapidly and almost completely hydrolyzed to amprenavir and inorganic phosphate by cellular phosphatases in the gut epithelium as it is absorbed. Absolute bioavailability has not been established. It can be taken without regard to food.
  Distribution
  It penetrates moderately well into the CNS. The semen:plasma ratio is negligible. It is not known if it is distributed into breast milk.
  Metabolism and excretion
  It is extensively metabolized by the cytochrome P₄₅₀ (CYP) 3A4 enzyme system. Two major metabolites have been identified that appear to result from the oxidation of the tetrahydrofuran and aniline moieties. Around 14% of a dose is eliminated in the urine and 75% in feces, <3% as unchanged drug. Metabolites account for >90% of administered drug found in fecal samples. It should be used with caution and at reduced doses in adults with mild or moderate hepatic impairment; it is contraindicated in patients with severe hepatic impairment.

• 臨床応用

  Treatment of HIV infection (in combination with other antiretroviral drugs)

• 副作用

  The most common adverse events in patients receiving boosted fosamprenavir were diarrhea, nausea, headache, fatigue, vomiting and rash. Ritonavir-boosted fosamprenavir is associated with a dyslipidemia profile characteristic of those treated with other protease inhibitors boosted with 200 mg of ritonavir.

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アムプレナビル スペクトルデータ(¹HNMR)

161814-49-9, アムプレナビル キーワード