アバカビル

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

  H317：アレルギー性皮膚反応を起こすおそれ

  H334：吸入するとアレルギー、喘息または、呼吸困難 を起こすおそれ

  H341：遺伝性疾患のおそれの疑い

  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。

  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。

  P272：汚染された作業衣は作業場から出さないこと。

  P280：保護手袋/保護衣/保護眼鏡/保護面を着用するこ と。

  P284：呼吸用保護具を着用すること。

  P302+P352：皮膚に付着した場合：多量の水と石鹸で洗うこと。

  P304+P340：吸入した場合：空気の新鮮な場所に移し、呼吸しやすい 姿勢で休息させること。

  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。

  P333+P313：皮膚刺激または発疹が生じた場合：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。

アバカビル 価格

アバカビル 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

• 効能

  抗ウイルス薬, 逆転写酵素阻害薬

• 説明

  The drug is extensively metabolized via stepwise phosphorylation to 5′-mono-, di-, and triphosphate. Abacavir is well absorbed (>75%) and penetrates the CNS. The drug can be taken without regard to meals. The drug does not show any clinically significant drug–drug interactions. Abacavir has been reported to produce life-threatening hypersensitivity reactions. The major use of abacavir appears to be in combination with other nucleoside RT inhibitors. A fixed-combination product has recently been approved by the U.S. FDA consisting of 300 mg of ABC, 150 mg of 3TC, and 300 mg of ZDV (Trizivar). The combination has been shown to be superior to other combinations in reducing viral load as well as to show improvement in CD4 cell count.

• 使用

  Abacavir is a commonly used nucleoside analogue with potent antiviral activity against HIV-1. - See more at: http://www.selleckchem.com/products/abacavir-sulfate.html#sthash.lApvcTNO.dpuf

• 適応症

  Abacavir (Ziagen) is a guanosine nucleoside analogue indicated for the therapy of HIV-1 infection in adults and children. It is used as part of a multidrug regimen and is available in a fixed-dose combination with zidovudine and lamivudine (Trizivir). It is also used for postexposure HIV infection prophylaxis.

• 抗菌性

  Abacavir has activity against HIV-1, HIV-2 and human T-cell lymphotrophic virus type-1 (HTLV-1).

• 獲得抵抗性

  Resistance is associated with specific changes in codons 184 with 65, 74 or 115 in the HIV reverse transcriptase codon region.

• 一般的な説明

  Abacavir is a nucleoside reverse transcriptase inhibitorNRTI that has been approved for use in combination therapiesfor the treatment of HIV and AIDS. Once in the tissues,it is metabolized by stepwise phosphorylation to themonophosphate, diphosphate, and triphosphate. Abacavir ishighly bioavailable (＞75%) and is effective by the oralroute. It penetrates the blood-brain barrier efficiently.Abacavir has been reported to produce life-threatening hypersensitivityreactions in some patients.

• 応用例（製薬）

  A synthetic analog of guanine formulated for oral use.

• 薬物動態学

  Oral absorption: 83%
  C_max 300 mg oral, twice daily: 3.0 ± 0.89 mg/L
  600 mg once daily: 4.26 mg/L
  Plasma half-life: 1.5 h
  Volume of distribution: 0.8 L/kg
  Plasma protein binding: c. 49%
  Absorption
  After oral administration abacavir sulfate undergoes rapid and extensive absorption unaffected by food.
  Distribution
  It penetrates well into the cerebrospinal fluid (CSF) and is an NRTI of choice if this characteristic is thought desirable. Good penetration into the male genital tract has been observed. The drug is secreted into human breast milk.
  Metabolism
  It is primarily metabolized in the liver, mainly by alcohol dehydrogenase and glucuronidation.
  Excretion
  Around 83% of the dose is eliminated in the urine, <2% as unchanged drug; the remainder is excreted in the feces. Dose adjustment is unnecessary in renal impairment. It can be used in moderate hepatic impairment, but is contraindicated if dysfunction is severe.

• 臨床応用

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

• 副作用

  Life-threatening hypersensitivity reactions occur in 5–8% of all individuals, necessitating discontinuation of the drug. Typically patients present within the first 6 weeks of starting treatment with fever, rash or other symptoms that worsen in severity with continued drug exposure. Hypersensitivity is associated with carriage of the major histocompatibility complex class I allele HLA-B57*01 and screening for this allele can significantly reduce the incidence of this effect.
  Current or recent (within the preceding 6 months) use of abacavir has been associated with a risk of myocardial infarction, but studies have yielded conflicting data.

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アバカビル スペクトルデータ(¹HNMR)

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