AMPRENAVIR

그림문자(GHS)

• 그림문자(GHS)

  

• 신호 어

  Warning

• 유해·위험 문구

  H302：삼키면 유해함

  H315：피부에 자극을 일으킴

  H319：눈에 심한 자극을 일으킴

  H332：흡입하면 유해함

  H335：호흡 자극성을 일으킬 수 있음

• 예방조치문구

  P261：분진·흄·가스·미스트·증기·...·스프레이의 흡입을 피하시오.

  P280：보호장갑/보호의/보안경/안면보호구를 착용하시오.

  P305+P351+P338：눈에 묻으면 몇 분간 물로 조심해서 씻으시오. 가능하면 콘택트렌즈를 제거하시오. 계속 씻으시오.

AMPRENAVIR 화학적 특성, 용도, 생산

• 개요

  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.

• 화학적 성질

  Off-White to Pale Yellow

• 용도

  A selective HIV protease inhibitor. An analogue of Ritonavir

• Indications

  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).

• 원료

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

• 일반 설명

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

• Pharmaceutical Applications

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

• Pharmacokinetics

  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.

• Clinical Use

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

• 부작용

  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.

AMPRENAVIR 준비 용품 및 원자재

AMPRENAVIR 공급 업체

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