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氢氧化铁还原葡聚糖

中文名称
氢氧化铁还原葡聚糖
中文别名
德异麦芽糖铁
英文名称
iron(3+);(2S,3R,4R,5R)-6-[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-[[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxymethyl]oxan-2-yl]oxyhexane-1,2,3,4,5-pentol
英文别名
——
氢氧化铁还原葡聚糖化学式
CAS
——
化学式
C18H34FeO16+3
mdl
——
分子量
562.3
InChiKey
JTQTXQSGPZRXJF-DOJSGGEQSA-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):
    -7.94
  • 重原子数:
    35
  • 可旋转键数:
    11
  • 环数:
    2.0
  • sp3杂化的碳原子比例:
    1.0
  • 拓扑面积:
    280
  • 氢给体数:
    12
  • 氢受体数:
    16

ADMET

代谢
血液循环中的被巨噬细胞吞噬,并与蛋白质结合形成血红素、铁蛋白或转铁蛋白。在这一步骤之后,结合的会补充低血红蛋白(Hb)和
Iron in the circulation is taken up by the plasma by cells of the RES. This binds proteins that form hemosiderin or ferritin, as well transferrin. Following this step, the bound iron replenishes low hemoglobin (Hb) and iron.
来源:DrugBank
毒理性
  • 毒性总结
(III)右旋糖酐的LD50信息在文献中不易获得,然而,果糖(另一种静脉注射的形式)在雄性大鼠中的LD50为140 mg/kg。(III)右旋糖酐过量可能会导致储存的积累,引起含血黄素沉着病。症状可能包括腹痛、虚弱和乏力等。应监测血清铁蛋白。采用支持性治疗,包括使用螯合剂
LD50 information for ferric derisomaltose is not readily available in the literature, however, the LD50 for iron sucrose (another form of intravenous iron) was 140 mg/kg in male rats. An overdose with ferric derisomaltose may lead to accumulation of stored iron, causing hemosiderosis. Symptoms may include abdominal pain, weakness, and lethargy, among others. Serum ferritin should be monitored. Employ supportive treatment including chelating agents.
来源:DrugBank
毒理性
  • 蛋白质结合
转铁蛋白结合,转铁蛋白是负责将运输到红系前体细胞以生产血红蛋白的运输分子。
Iron binds to transferrin, the transport molecule responsible for transporting iron to erythroid precursor cells for the production of hemoglobin.
来源:DrugBank
吸收、分配和排泄
  • 吸收
在单次1000毫克剂量后,血清的Cmax和AUC分别为408微克/毫升和17730微克·小时/毫升。单次静脉注射蔗糖铁(III)后,血清铁蛋白浓度在大约7天达到峰值。关于同时口服的说明口服与静脉同时使用时,吸收会降低。应在最后一次蔗糖铁(III)注射后至少5天再给予口服
After a single 1000 mg dose, the Cmax and AUC of serum iron were 408 μg/mL and 17730 μg.h /mL, respectively. Serum ferritin concentrations reach their peak about 7 days after a single dose of intravenous ferric derisomaltose. A note on concomitant oral iron The absorption of oral iron is decreased when administered with intravenous iron. The administration of oral iron should be delayed until at least 5 days after the last ferric derisomaltose injection.
来源:DrugBank
吸收、分配和排泄
  • 消除途径
肾脏排泄在单次给药的药代动力学研究中并非主要的消除途径。在体内往往会积累,导致过载,随后产生毒性效应。少量的右旋糖酐会通过尿液和粪便排出。
Renal elimination was not a significant route of elimination in single-dose pharmacokinetic studies. Iron can often accumulate in the body leading to iron overload followed by toxic effects. Small amounts of ferric derisomaltose are excreted in the urine and feces.
来源:DrugBank
吸收、分配和排泄
  • 分布容积
葡聚糖或释放的在网状内皮系统(RES)的细胞中被发现。它在肝脏和脾脏中浓度较高。其他静脉注射剂的分布体积在70公斤成人大约为3升。尽管葡聚糖的具体分布体积在文献中不易获得,但它可能与其他静脉注射的剂形式相似。
Ferric derisomaltose or released iron that was released is found in cells of the reticuloendothelial system (RES). It is found to be highly concentrated in the liver and spleen. The volume of distribution of other forms of intravenous iron is 3L, on average, in a 70 kg adult. Though the specific volume of distribution of ferric derisomaltose is not readily available in the literature, it is likely similar to other intravenous forms of iron.
来源:DrugBank
吸收、分配和排泄
  • 清除
静脉从血浆中清除。由于复合物的大小较大,无法通过肾单位排出,因此费里克斯德里斯莫尔糖不是通过肾脏排出。
Intravenous iron is cleared from the plasma. Ferric derisomaltose is not eliminated via the kidneys, as the size of the complex is large and cannot be excreted via the nephron.
来源:DrugBank