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Phosphonoformic acid trisodium salt hexahydrate

Phosphonoformic acid trisodium salt hexahydrate 구조식 이미지
카스 번호:
34156-56-4
상품명:
Phosphonoformic acid trisodium salt hexahydrate
동의어(영문):
FOSCARNET;PFA Hydrate;Gefin Hydrate;EHB 776 Hydrate;A 29622 Hydrate;Foscavir Hydrate;FORSCARNETSODIUM;Triapten Hexahydrate;Foscarnet Sodium(PFA);Foscarnet Sodium (50 mg)
CBNumber:
CB3714429
분자식:
CH12Na3O11P
포뮬러 무게:
300.04
MOL 파일:
34156-56-4.mol

Phosphonoformic acid trisodium salt hexahydrate 속성

저장 조건
2-8°C
용해도
H2O: 0.1 g/mL hot, clear, colorless
물리적 상태
neat
수용성
Soluble in water.
InChIKey
ILRVASBWNRYBFD-UHFFFAOYSA-K
CAS 데이터베이스
34156-56-4(CAS DataBase Reference)
안전
  • 위험 및 안전 성명
  • 위험 및 사전주의 사항 (GHS)
위험품 표기 Xi
위험 카페고리 넘버 36/37/38
안전지침서 26-36
WGK 독일 3
RTECS 번호 SY8300000
HS 번호 29319090
그림문자(GHS):
신호 어: Warning
유해·위험 문구:
암호 유해·위험 문구 위험 등급 범주 신호 어 그림 문자 P- 코드
H315 피부에 자극을 일으킴 피부부식성 또는 자극성물질 구분 2 경고 P264, P280, P302+P352, P321,P332+P313, P362
H319 눈에 심한 자극을 일으킴 심한 눈 손상 또는 자극성 물질 구분 2A 경고 P264, P280, P305+P351+P338,P337+P313P
H335 호흡 자극성을 일으킬 수 있음 특정 표적장기 독성 - 1회 노출;호흡기계 자극 구분 3 경고
예방조치문구:
P261 분진·흄·가스·미스트·증기·...·스프레이의 흡입을 피하시오.
P304+P340 흡입하면 신선한 공기가 있는 곳으로 옮기고 호흡하기 쉬운 자세로 안정을 취하시오.
P305+P351+P338 눈에 묻으면 몇 분간 물로 조심해서 씻으시오. 가능하면 콘택트렌즈를 제거하시오. 계속 씻으시오.
P405 밀봉하여 저장하시오.

Phosphonoformic acid trisodium salt hexahydrate C화학적 특성, 용도, 생산

화학적 성질

Phosphonoformic acid trisodium salt hexahydrate is white or almost white, crystalline powder.

용도

Foscarnet inhibits viral DNA polymerase and reverse transcriptase. Foscarnet is used as an antiviral.

용도

Type II Pi transporter inhibitor.

정의

ChEBI: The hexahydrate form of trisodium phosphonoformate. It is used as an antiviral agent in the treatment of cytomegalovirus retinitis (CMV retinitis, an inflamation of the retina that can lead to blindness) and as an alternative to ganciclovir for AIDS patien s who require concurrent antiretroviral therapy but are unable to tolerate ganciclovir due to haematological toxicity.

원료

Phosphonoformic acid trisodium salt hexahydrate can be generated in vitro, and CMV strains resistant to both ganciclovir and foscarnet have occasionally been recovered from humans.

Pharmaceutical Applications

Phosphonoformic acid trisodium salt hexahydrate is a synthetic non-nucleoside pyrophosphate analog formulated as the trisodium hexahydrate for intravenous use. The solubility in water at pH 7 is only about 5% (w/w).

Pharmacokinetics

Oral absorption: c. 17%
Cmax 60 mg/kg intravenous 8-hourly: 557 μmol/L
Plasma half-life: 3.3–6.8 h
Volume of distribution: 0.52–0.74 L/kg
Plasma protein binding: 14–17%
Absorption and distribution
Oral bioavailability is poor. A wide range of plasma concentrations was noted (75–500 μmol/L) during 3–21 days of continuous intravenous infusion of 0.14–0.19 mg/kg per min. During continuous intravenous therapy the concentrations reached a plateau on day 3. Considerable differences in steady-state plasma concentrations exist between individuals. Drug penetrates the CSF; the mean concentration is about 40–60% of the mean plasma concentration, depending upon dose.
Metabolism and excretion
Elimination appears to be triphasic, with two initially short half-lives of 0.5–1.4 h and 3.3–6.8 h, followed by a long terminal phase of 88 h. About 88% of the cumulative intravenous dose is recovered unchanged in the urine within a week of stopping an infusion, indicating that the drug is not significantly metabolized. Non-renal clearance accounts for 14–18% of total clearance and may relate to uptake into bone. Plasma clearance decreases markedly with decreased renal function and the elimination half-life may be increased by up to 10-fold. Conventional dialysis eliminates about 25% of a dose while high-flux dialysis can remove nearly 60%.

Clinical Use

Treatment of CMV retinitis in patients for whom ganciclovir is contraindicated, inappropriate or ineffective
It is also potentially of value in the treatment of aciclovir-resistant HSV infection.

부작용

Treatment is more frequently limited by toxicity than with ganciclovir. Renal toxicity is most common. A two- to three-fold increase in serum creatinine levels occurs in 20–60% (mean 45%) of patients given 130–230 mg/kg per day as a continuous intravenous infusion. Renal impairment usually develops within the first few weeks of treatment and is generally reversible within several weeks of discontinuing therapy. Foscarnet chelates metal ions, and serum electrolyte abnormalities – predominantly hypocalcemia, hypomagnesemia, hypokalemia and hypophosphatemia – occur in about 30, 15, 16 and 8% of patients, respectively. Convulsions occur in 10–15%. Other side effects include anemia (25–50%), penile or vulval ulceration (3–9%), nausea and vomiting (20–30%), local irritation and thrombophlebitis at the infusion site, abdominal pain and occasional pancreatitis, headache (c. 25%), dizziness, involuntary muscle contractions, tremor, hypoesthesia, ataxia, neuropathy, anxiety, nervousness, depression and confusion, and skin rash. Nephrogenic diabetes insipidus has been reported.
Foscarnet is contraindicated in pregnancy. Topical application does not result in dermal toxicity similar to that produced by phosphonacetic acid.

Phosphonoformic acid trisodium salt hexahydrate 준비 용품 및 원자재

원자재

준비 용품


Phosphonoformic acid trisodium salt hexahydrate 공급 업체

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