아바카비르

그림문자(GHS)

• 그림문자(GHS)

  

• 신호 어

  Danger

• 유해·위험 문구

  H317：알레르기성 피부 반응을 일으킬 수 있음

  H334：흡입 시 알레르기성 반응, 천식 또는 호흡 곤란 등을 일으킬 수 있음

  H341：유전적인 결함을 일으킬 것으로 의심됨 (노출되어도 생식세포 유전독성을 일으키지 않는다는 결정적인 증거가 있는 노출경로가 있다면 노출경로 기재)

  H361：태아 또는 생식능력에 손상을 일으킬 것으로 의심됨

• 예방조치문구

  P201：사용 전 취급 설명서를 확보하시오.

  P202：모든 안전 조치 문구를 읽고 이해하기 전에는 취급하지 마시오.

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

  P272：작업장 밖으로 오염된 의복을 반출하지 마시오.

  P280：보호장갑/보호의/보안경/안면보호구를 착용하시오.

  P284：호흡 보호구를 착용하시오.

  P302+P352：피부에 묻으면 다량의 물로 씻으시오.

  P304+P340：흡입하면 신선한 공기가 있는 곳으로 옮기고 호흡하기 쉬운 자세로 안정을 취하시오.

  P308+P313：노출 또는 접촉이 우려되면 의학적인 조치· 조언를 구하시오.

  P333+P313：피부자극성 또는 홍반이 나타나면 의학적인 조치·조언를 구하시오.

  P405：밀봉하여 저장하시오.

아바카비르 화학적 특성, 용도, 생산

• 개요

  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.

• 용도

  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

• Indications

  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.

• Antimicrobial activity

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

• 원료

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

• 일반 설명

  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.

• Pharmaceutical Applications

  A synthetic analog of guanine formulated for oral use.

• Pharmacokinetics

  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.

• Clinical Use

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

• 부작용

  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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