엠트리시타빈

그림문자(GHS)

• 그림문자(GHS)

  

• 신호 어

  Warning

• 유해·위험 문구

  H302：삼키면 유해함

  H315：피부에 자극을 일으킴

  H319：눈에 심한 자극을 일으킴

  H335：호흡 자극성을 일으킬 수 있음

• 예방조치문구

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

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

엠트리시타빈 화학적 특성, 용도, 생산

• 화학적 성질

  White to Off-White Crystalline Solid

• 용도

  Labeled Emtricitabine, intended for use as an internal standard for the quantification of Emtricitabine by GC- or LC-mass spectrometry.

• 정의

  ChEBI: An organofluorine compound that is 5-fluorocytosine substituted at the 1 position by a 2-(hydroxymethyl)-1,3-oxathiolan-5-yl group (2R,5S configuration). It is used in combination therapy for the treatment of HIV-1 infect on.

• 원료

  Resistance is associated with a substitution in the HIV-1 reverse transcriptase gene at codon 184 (M184V/I). Emtricitabineresistant isolates are cross-resistant to lamivudine. HIV-1 isolates with the K65R substitution in the reverse transcriptase coding region have reduced susceptibility.

• 일반 설명

  Emtricitabine is an orally active NRTI whose pharmacokineticsare favorable for once-daily administration.

• Pharmaceutical Applications

  A synthetic nucleoside analog of cytosine, formulated for oral use.

• Pharmacokinetics

  Oral absorption: capsules 93%
  C_max 200 mg oral once daily: 1.8 ± 0.7 mg/L
  Plasma half-life: c. 10 h
  Volume of distribution: 1.4 ± 0.3 L/kg
  Plasma protein binding: <4%
  Absorption and distribution
  It is rapidly and extensively absorbed. There is moderate CNS penetration. The estimated semen:plasma ratio is approximately 4. There are presently no data on levels in breast milk.
  Metabolism and excretion
  It does not inhibit human cytochrome P₄₅₀ enzymes. About 80% is excreted in the urine, the rest in feces. Renal clearance is greater than the estimated creatinine clearance, suggesting elimination by both glomerular filtration and active tubular secretion. There may be competition for elimination with other compounds that are renally excreted. Exposure is significantly increased in renal insufficiency, but dose reductions are not generally recommended. It is unlikely that a dose adjustment would be required in the presence of hepatic impairment.

• Clinical Use

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

• 부작용

  At least 10% of patients suffer headache, diarrhea, nausea, fatigue, dizziness, depression, insomnia, abnormal dreams, rash, abdominal pain, asthenia, increased cough and rhinitis. Skin hyperpigmentation is common (≥10%) in pediatric patients. Emtricitabine competes with lamivudine for the enzymes involved in intracellular phosphorylation; their co- administration is contraindicated.

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