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乙胺嘧啶-磺胺多辛混合物 | 37338-39-9

中文名称
乙胺嘧啶-磺胺多辛混合物
中文别名
——
英文名称
Suldox
英文别名
4-amino-N-(5,6-dimethoxypyrimidin-4-yl)benzenesulfonamide;5-(4-chlorophenyl)-6-ethylpyrimidine-2,4-diamine
乙胺嘧啶-磺胺多辛混合物化学式
CAS
37338-39-9
化学式
C24H27ClN8O4S
mdl
——
分子量
559.0
InChiKey
LUBUTTBEBGYNJN-UHFFFAOYSA-N
BEILSTEIN
——
EINECS
——
  • 物化性质
  • 计算性质
  • ADMET
  • 安全信息
  • SDS
  • 制备方法与用途
  • 上下游信息
  • 反应信息
  • 文献信息
  • 表征谱图
  • 同类化合物
  • 相关功能分类
  • 相关结构分类

计算性质

  • 辛醇/水分配系数(LogP):
    3.4
  • 重原子数:
    38
  • 可旋转键数:
    7
  • 环数:
    4.0
  • sp3杂化的碳原子比例:
    0.17
  • 拓扑面积:
    203
  • 氢给体数:
    4
  • 氢受体数:
    12

ADMET

毒理性
  • 在妊娠和哺乳期间的影响
哺乳期使用概要:由于在哺乳期间使用磺胺多辛的经验很少,可能更倾向于使用另一种药物,特别是在哺乳新生儿或早产儿时。制造商指出,磺胺多辛-乙胺嘧啶组合用于哺乳期预防和对2个月以下儿童是禁忌的。然而,一些作者认为在哺乳期间使用磺胺多辛-乙胺嘧啶并无禁忌。有建议称,哺乳期间母体乙胺嘧啶的清除可能会增加,但数据不足以得出明确结论。 一旦在婴儿中出现黄疸、皮疹,或者观察到任何成型血细胞数量显著减少,或者发生活动性细菌或真菌感染,应立即停止对母亲的磺胺多辛-乙胺嘧啶预防治疗。 对哺乳婴儿的影响:给26名2至6个月大、主要接受母乳喂养且感染疟疾的婴儿的母亲服用乙胺嘧啶是治愈性的。治疗方案包括首次服用75毫克,随后在4至7天后再次服用50-75毫克。疗效似乎与哺乳习惯有关,因为另一个部落群体中哺乳较少的婴儿并未得到保护。另一份病例报告表明,母亲口服75毫克,随后每周服用25毫克,治愈了她的婴儿的疟疾,并保护她的母乳喂养婴儿在6个月内免受疟疾感染。任何婴儿中均未报告不良影响。 一项研究调查了接受假定性疟疾治疗的HIV感染妇女,其中包括12名正在服用磺胺多辛-乙胺嘧啶组合的哺乳母亲。这种药物组合似乎比氯喹治疗更少地减少母乳中的病毒载量。未提及对哺乳婴儿的影响。 在刚果民主共和国,一组33名婴儿(哺乳程度未说明)被住院的母亲喂养,这些母亲正在服用尼夫特莫克斯。30名母亲服用了完整的30剂口服尼夫特莫克斯,每天15毫克/千克,并且所有母亲都接受了14剂静脉注射的依鸟氨酸,每天400毫克/千克,连续7天,用于治疗非洲人类锥虫病(睡眠病)。8位母亲也服用了磺胺多辛-乙胺嘧啶。任何哺乳婴儿中均未报告严重不良事件。 对哺乳和母乳的影响:截至修订日期,未找到相关已发布信息。
◉ Summary of Use during Lactation:Because there is little published experience with sulfadoxine during breastfeeding, an alternate drug may be preferred, especially while nursing a newborn or preterm infant. The manufacturer states that the combination of sulfadoxine-pyrimethamine is contraindicated for prophylaxis during nursing and in children under 2 months of age. However, some authors have found no contraindication to the use of sulfadoxine-pyrimethamine during breastfeeding. It has been suggested that maternal pyrimethamine clearance might be increased during lactation, but data are insufficient to make a definitive conclusion. Sulfadoxine-pyrimethamine prophylaxis of the mother should be discontinued at the first appearance in the infant of jaundice, skin rash, if a significant reduction in the count of any formed blood elements is noted, or upon the occurrence of active bacterial or fungal infections. ◉ Effects in Breastfed Infants:Administration of pyrimethamine to mothers of 26 predominantly breastfed infants 2 to 6 months old who were infected with malaria was curative in the infants. The regimen consisted of 75 mg followed by a subsequent dose of 50-75 mg 4 to 7 days later. The efficacy apparently is related to breastfeeding habits, because infants in another tribal group who breastfed their infants less extensively were not protected. An additional case report indicates that a maternal dose of 75 mg orally followed by 25 mg weekly cured malaria in her infant and protected her breastfed infant against becoming infected with malaria for 6 months. No adverse effects were reported in any of the infants. A study of women with HIV infection being treated for presumptive malaria included 12 nursing mothers who were taking the sulfadoxine-pyrimethamine combination. The drug combination appeared to reduce breastmilk viral load less than chloroquine treatment. No mention was made of the effects in breastfed infants. A cohort of 33 infants who were breastfed (extent not stated) by hospitalized mothers taking nifurtimox was followed in the Democratic Republic of the Congo. Thirty mothers took a full course of 30 doses of oral nifurtimox 15 mg/kg daily and all received 14 doses of intravenous eflornithine 400 mg/kg daily for 7 days for human African trypanosomiasis. (sleeping sickness). Eight mothers also took sulfadoxine-pyrimethamine. No serious adverse events were reported in any of the breastfed infants. ◉ Effects on Lactation and Breastmilk:Relevant published information was not found as of the revision date.
来源:Drugs and Lactation Database (LactMed)

文献信息

  • [EN] NUCLEOTIDE AND NUCLEOSIDE THERAPEUTIC COMPOSITIONS AND USES RELATED THERETO<br/>[FR] COMPOSITIONS THÉRAPEUTIQUES À BASE DE NUCLÉOTIDES ET NUCLÉOSIDES ET UTILISATIONS ASSOCIÉES
    申请人:UNIV EMORY
    公开号:WO2017155923A1
    公开(公告)日:2017-09-14
    This disclosure relates to nucleotide and nucleoside therapeutic compositions and uses in treating infectious diseases, viral infections, and cancer, where the base of the nucleotide or nucleoside contains at least one thiol, thione or thioether.
    这份披露涉及到核苷酸和核苷类治疗组合物,用于治疗传染病、病毒感染和癌症,在这些组合物中,核苷酸或核苷的碱基至少含有一个醇、酮或醚。
  • [EN] ALKYNE CONTAINING NUCLEOTIDE AND NUCLEOSIDE THERAPEUTIC COMPOSITIONS AND USES RELATED THERETO<br/>[FR] COMPOSITIONS THÉRAPEUTIQUES À BASE DE NUCLÉOTIDES ET NUCLÉOSIDES CONTENANT UN ALCYNE ET UTILISATIONS ASSOCIÉES
    申请人:UNIV EMORY
    公开号:WO2017189978A1
    公开(公告)日:2017-11-02
    This disclosure relates to nucleotide and nucleoside therapeutic compositions and uses in treating infectious diseases, viral infections, and cancer, where the base of the nucleotide or nucleoside contains at least one thiol, thione or thioether.
    这份披露涉及到核苷酸和核苷类治疗组合物,用于治疗传染病、病毒感染和癌症,其中核苷酸或核苷的碱基至少含有一个醇、酮或醚。
  • [EN] NUCLEOTIDE AND NUCLEOSIDE COMPOSITIONS AND USES RELATED THERETO<br/>[FR] COMPOSITIONS À BASE DE NUCLÉOTIDE ET DE NUCLÉOSIDE ET UTILISATIONS CORRESPONDANTES
    申请人:UNIV EMORY
    公开号:WO2015038596A1
    公开(公告)日:2015-03-19
    This disclosure relates to nucleotide and nucleoside therapeutic compositions and uses in treating infectious diseases, viral infections, and cancer, where the base of the nucleotide or nucleoside contains at least one thiol, thione or thioether.
    这份披露涉及到核苷酸和核苷类治疗组合物,用于治疗传染病、病毒感染和癌症,在这些组合物中,核苷酸或核苷的碱基至少含有一个醇、酮或醚。
  • HIV protease inhibiting compounds
    申请人:Flentge Charles A.
    公开号:US20110003827A1
    公开(公告)日:2011-01-06
    A compound of the formula is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.
    公开了一种具有以下公式的化合物,作为HIV蛋白酶抑制剂。还公开了抑制HIV感染的方法和组合物。
  • [EN] HIV PROTEASE INHIBITING COMPOUNDS<br/>[FR] COMPOSES INHIBITEURS DE LA PROTEASE DU VIH
    申请人:ABBOTT LAB
    公开号:WO2005061487A1
    公开(公告)日:2005-07-07
    A compound of the formula (I) is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.
    公开了一种公式(I)的化合物作为HIV蛋白酶抑制剂。还公开了用于抑制HIV感染的方法和组合物。
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