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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

• 注意書き

  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。

  P501：内容物/容器を．．．に廃棄すること。

ネルフィナビル, FREE BASE 化学特性,用途語,生産方法

• 効能

  抗ウイルス薬, HIVプロテアーゼ阻害薬

• 使用

  Antiviral.

• 定義

  ChEBI: An aryl sulfide that is used (as its mesylate salt) for treatment of HIV and also exhibits some anticancer properties.

• 適応症

  Nelfinavir (Viracept) is probably the most commonly used protease inhibitor because of its low incidence of serious adverse effects. Its most common side effects are diarrhea and flatulence; these may resolve with continued use. In addition to the drugs contraindicated for use with all protease inhibitors, amiodarone, rifampin, and quinidine are contraindicated in patients taking nelfinavir.

• 抗菌性

  Nelfinavir inhibits HIV-1 and HIV-2 proteases. Bioavailability is affected to only a limited degree by combination with lowdose ritonavir.

• 獲得抵抗性

  Resistance is most frequently selected through a D30N mutation in the HIV protease. An L90M mutation also confers resistance.

• 応用例（製薬）

  A synthetic chemical formulated as the mesylate for oral administration.

• 薬物動態学

  Oral absorption: c. 70–80% (with food)
  C_max 750 mg thrice daily: c. 3–4 mg/L
  1250 mg twice daily: c. 4 mg/L
  C_min 750 mg thrice daily: c. 1–3 mg/L
  1250 mg twice daily: c. 0.7–2.2 mg/L
  Plasma half-life: c. 3.5 h
  Volume of distribution: c. 2–7 L/kg
  Plasma protein binding: >98%
  Absorption and distribution
  Food improves the bioavailability and the drug should be administered with a light meal. The semen:plasma ratio is 0.07. It is distributed into breast milk.
  Metabolism and excretion
  One major and several minor oxidative metabolites are found in plasma. Most of an oral dose is recovered in feces as unchanged drug (22%) and metabolites (78%). The remainder is recovered in urine, mainly unchanged.
  An increase in the area under the time–concentration curve (AUC) has been observed in patients with hepatic impairment, but specific dose recommendations have not been made.

• 臨床応用

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

• 副作用

  The most common adverse effect is diarrhea of mild to moderate severity. Other side effects include nausea, fatigue, vomiting and headache. It is associated with less dyslipidemia in comparison with ritonavir-boosted protease inhibitors.

• 代謝

  Following oral administration, nelfinavir peak levels in plasma ranged from 0.34 mg/mL (10 mg/kg in the dog) to 1.7 mg/mL (50 mg/kg in the rat). In the dog, nelfinavir was slowly absorbed, and bioavailability was 47%. The drug appeared to be metabolized in the liver, and the major excretory route was in feces.

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