설파독신

한글명:설파독신

카스 번호2447-57-6

상품명:Sulfadoxine

CBNumberCB8171942

분자식C12H14N4O4S

포뮬러 무게310.33

MOL 파일2447-57-6.mol

동의어(한글)

설파독신

화학적 성질

녹는점	190-194°C
끓는 점	298°C (rough estimate)
밀도	1.4006 (rough estimate)
굴절률	1.6270 (estimate)
저장 조건	Keep in dark place,Inert atmosphere,Room temperature
용해도	에탄올에 용해됩니다. 수산화암모늄(9:1) 20mg/ml
물리적 상태	가루
산도 계수 (pKa)	6.16±0.50(Predicted)
색상	하얀색
수용성	209.8mg/L(온도 미표시)
Merck	14,8906
BRN	625453
BCS Class	3/1

위험 및 안전 성명

위험품 표기

위험 카페고리 넘버

36/37/38

안전지침서

WGK 독일

RTECS 번호

DA9500000

HS 번호

29350090

독성

LD50 in mice (microcrystals, mg/kg): 5200 orally, 2900 s.c., 2900 i.p. (Bhni)

NFPA 704:

	0
2		0

그림문자(GHS)

설파독신 MSDS

설파독신 화학적 특성, 용도, 생산

개요
Sulfadoxin is a sulfonamide antibiotic that inhibits dihydropteroate synthetase (DHPS), an enzyme involved in folic acid synthesis. Sulfadoxin competes with 4-aminobenzoate (PABA), the native substrate of DHPS, and inhibits PABA incorporation into folic acid. Folate is essential for purine and pyrimidine synthesis, therefore, sulfadoxin has antiproliferative activity in non-resistant P. falciparum. Sulfadoxin inhibits growth of P. falciparum in vitro, but potency varies between non-resistant (IC₅₀ = 4 ng/ml) and resistant strains (IC₅₀ = 3,970 ng/ml).
화학적 성질
White Crystalline Solid
정의
ChEBI: A sulfonamide consisting of pyrimidine having methoxy substituents at the 5- and 6-positions and a 4-aminobenzenesulfonamido group at the 4-position. In combination with the antiprotozoal pyrimethamine (CHEBI:8673) it is used as an antimalarial.
Antimicrobial activity
Its antibacterial activity is relatively poor. Used alone it has a slow and uncertain effect against malaria parasites. Resistance of malaria parasites to the combination with pyrimethamine is common in many endemic areas.
Pharmaceutical Applications
An ultra-long-acting sulfonamide. It is no longer prescribed alone, but is used in combination with pyrimethamine as the antimalarial agent Fansidar. It is poorly soluble in water.
Pharmacology
In terms of antibacterial action, this drug is analogous to other sulfanilamides; however, it possesses very prolonged action. Its half-life is from 120 to 200 h. Sulfadoxine is used for infectious diseases caused by microorganisms that are sensitive to the sulfanilamide drugs, such as infections of respiratory organs, gastric and urinary tracts; purulent infections of various localization, osteomyelitis, sinusitis, and other infections. It is used in combination with antimalarial drugs. Synonyms of this drug are sulfarmethoxine, fanasil, and fansidar.
Pharmacokinetics
Oral absorption ：Extensive
C_max 500 mg oral： c. 60 mg/L after 3–4 h
Plasma half-life：c.6 days
Volume of distribution：0.13 L/kg
Plasma protein binding：94%
The extremely long half-life allows administration at weekly intervals. The acetyl metabolite has a similarly long half-life, but sulfadoxine is less extensively metabolized than many other sulfonamides.
Clinical Use
Sulfadoxine is used only in combination with pyrimethamine.
부작용
Side effects are those common to the group. There have been many reports of Stevens–Johnson syndrome following its use and the combination with pyrimethamine is no longer recommended for the prophylaxis of malaria.

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