넬피나비어

넬피나비어
넬피나비어 구조식 이미지
카스 번호:
159989-64-7
한글명:
넬피나비어
동의어(한글):
넬피나비어
상품명:
NELFINAVIR
동의어(영문):
AG 1341;nefinavir;NELFINAVIR;NELFINAVIR-12;Nelfinavir D5;8a-beta))-a-bet;NELFINAVIR iMpurity;NELFINAVIR USP/EP/BP;Nelfinavir (AG-1341);Nelfinavir Regeoisomer
CBNumber:
CB8213806
분자식:
C32H45N3O4S
포뮬러 무게:
567.78
MOL 파일:
159989-64-7.mol

넬피나비어 속성

녹는점
185-186 °C
끓는 점
786.8±60.0 °C(Predicted)
알파
D -119.23° (c = 0.26 in methanol)
밀도
1.22±0.1 g/cm3(Predicted)
저장 조건
under inert gas (nitrogen or Argon) at 2–8 °C
용해도
≥ 20.45mg/mL in Ethanol
물리적 상태
가루
산도 계수 (pKa)
pKa1 6.0; pKa2 11.06(at 25℃)
수용성
7g/L(온도는 명시되지 않음)
안전
  • 위험 및 안전 성명
  • 위험 및 사전주의 사항 (GHS)
독성 rat,LD,oral,> 5gm/kg (5000mg/kg),Toxicologist. Vol. 42, Pg. 55, 1998.
그림문자(GHS): GHS hazard pictograms
신호 어: Warning
유해·위험 문구:
암호 유해·위험 문구 위험 등급 범주 신호 어 그림 문자 P- 코드
H302 삼키면 유해함 급성 독성 물질 - 경구 구분 4 경고 GHS hazard pictograms P264, P270, P301+P312, P330, P501
예방조치문구:
P264 취급 후에는 손을 철저히 씻으시오.
P264 취급 후에는 손을 철저히 씻으시오.
P270 이 제품을 사용할 때에는 먹거나, 마시거나 흡연하지 마시오.

넬피나비어 C화학적 특성, 용도, 생산

용도

Antiviral.

정의

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

Indications

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.

Antimicrobial activity

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

원료

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

Pharmaceutical Applications

A synthetic chemical formulated as the mesylate for oral administration.

Pharmacokinetics

Oral absorption: c. 70–80% (with food)
Cmax 750 mg thrice daily: c. 3–4 mg/L
1250 mg twice daily: c. 4 mg/L
Cmin 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.

Clinical Use

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

부작용

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.

신진 대사

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.

넬피나비어 준비 용품 및 원자재

원자재

준비 용품


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