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Sulfadoxine D3

(Synonyms: Sulphadoxine D3) 目录号 : GC67935

Sulfadoxine D3 是 Sulfadoxine 的氘代物。Sulfadoxine 是一种磺酰胺类化合物,通常与 Pyrimethamine 联合用于耐多药恶性疟原虫和间日疟原虫的防治。但与 Pyrimethamine 不同,Sulfadoxine 对 HIV 的复制和 MT-2 细胞周期进展没有影响。Sulfadoxine 还能抑制呼吸道、泌尿道感染。

Sulfadoxine D3 Chemical Structure

Cas No.:1262770-70-6

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10mg
¥3,150.00
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产品描述

Sulfadoxine D3 is a deuterium labeled Sulfadoxine . Sulfadoxine is a sulfonamide that is used, usually in combination with Pyrimethamine , for multidrug-resistant Plasmodium falciparum and P. vivax inhibition. Unlike PYR, Sulfadoxine has no impact on HIV replication or MT-2 cell cycle progression. But also Sulfadoxine exhibits suppression on respiratory, and urinary tract infections[1][2][3][4].

磺胺多辛 (0-100 μM;7 d) 对 MT-2 细胞中 HIV-1 的复制无影响[4].
磺胺多辛 (100 μM;48 h) 对 MT-2 细胞 S 期积累的诱导无影响[4].

磺胺多辛 (0.1, 0.3, 10 mg/kg/d; 口服; 每日1次, 连用 3天) 与阿奇霉素 (30 mg/kg/d; 口服; 每日1次, 连用 3天),能够抑制小鼠疟疾模型中的血期寄生虫或约氏疟原虫子孢子[5].

[1]. Ratcliff A, et al. Therapeutic response of multidrug-resistant Plasmodium falciparum and P. vivax to chloroquine and sulfadoxine-pyrimethamine in southern Papua, Indonesia. Trans R Soc Trop Med Hyg. 2007 Apr;101(4):351-9.
[2]. Fey K, et al. Empfindlichkeit bakterieller Krankheitserreger aus dem Respirationstrakt von Pferden gegenÜber Trimethoprim, Sulfadoxin, Sulfadimethoxin und Kombinationen dieser Wirkstoffe [Susceptibility of bacterial isolates from the equine respiratory tract to trimethoprim, sulfadoxine, sulfadimethoxine and combinations of these compounds]. Tierarztl Prax. 1995 Apr;23(2):148-54. German.
[3]. Baraff LJ. Emergency medicine-important advances in clinical medicine: single-dose treatment of urinary tract infections. West J Med. 1983 Jan;138(1):89-90.
[4]. Oguariri RM, et al. Evaluation of the effect of pyrimethamine, an anti-malarial drug, on HIV-1 replication. Virus Res. 2010 Nov;153(2):269-76.
[5]. Neerja J, et al. Plasmodium yoelii: activity of azithromycin in combination with pyrimethamine or sulfadoxine against blood and sporozoite induced infections in Swiss mice. Exp Parasitol. 2004 Jul-Aug;107(3-4):120-4.

Chemical Properties

Cas No. 1262770-70-6 SDF Download SDF
别名 Sulphadoxine D3
分子式 C12H11D3N4O4S 分子量 313.35
溶解度 储存条件 Store at -20°C
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1 mM 3.1913 mL 15.9566 mL 31.9132 mL
5 mM 0.6383 mL 3.1913 mL 6.3826 mL
10 mM 0.3191 mL 1.5957 mL 3.1913 mL
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Research Update

Pharmacokinetic disposition of sulfadoxine in children with acute uncomplicated falciparum malaria treated with sulfadoxine-pyrimethamine in South West Nigeria

Am J Ther 2012 Sep;19(5):338-45.PMID:19918170DOI:10.1097/MJT.0b013e3181baf266.

Sulfadoxine (SDX)-pyrimethamine is currently recommended as a partner drug with artesunate in the chemotherapy of malaria. However, information on pharmacokinetic disposition of SDX-pyrimethamine in children is limited. Efforts in this study were thus devoted to evaluation of pharmacokinetic disposition of SDX using high-pressure liquid chromatographic techniques and effects of pharmacokinetic variability on treatment outcome in Nigerian children with falciparum malaria. The blood concentration profile of SDX was similar in patients whose infection responded to treatment and those who failed treatment; mean SDX concentration values were similar for day 3 (179 vs 157 μg/mL, P = 0.734), day 7 (84 vs 51 μg/mL, P = 0.365), and day 14 (50 vs 14 μg/mL, P = 0.151). Extent of exposure (area under the curve) to SDX was also similar in the patients (1196 vs 1013 μg d/mL, P = 0.561). Pearson's correlation, showed significant correlation between area under the curve and D3 or D7 concentration of SDX (P = 0.001, r = 0.702 or P = 0.001, r = 0.835, respectively). Age-stratified analysis showed that SDX concentrations were significantly higher in older children (older than 5 years); the mean maximum concentration (125 vs 295 μg/mL, P = 0.001), extent of exposure (812 vs 1562 μg d/mL, P = 0.001), day 3 concentration (98 vs 250 μg/mL, P = 0.001), and day 7 concentration (54 vs 128 μg/mL, P = 0.007) were higher. The study revealed no differences in posttreatment blood SDX concentrations in patients who responded to treatment and those who failed to respond to treatment. Furthermore, there was an age-related pharmacokinetic variability of SDX in the group of children studied with potential impact on treatment outcome.