(2S)-4-amino-N-[(1R,2S,3S,4R,5S)-5-amino-2-[(2S,3R,4S,5S,6R)-4-amino-3,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-4-[(2R,3R,4S,5S,6R)-6-(aminomethyl)-3,4,5-trihydroxyoxan-2-yl]oxy-3-hydroxycyclohexyl]-2-hydroxybutanamide;hydron;disulfate

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: (2S)-4-amino-N-[(1R,2S,3S,4R,5S)-5-amino-2-[(2S,3R,4S,5S,6R)-4-amino-3,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-4-[(2R,3R,4S,5S,6R)-6-(aminomethyl)-3,4,5-trihydroxyoxan-2-yl]oxy-3-hydroxycyclohexyl]-2-hydroxybutanamide;hydron;disulfate
• 化学式: C22H47N5O21S2
• 分子量: 781.8
• InChiKey: FXKSEJFHKVNEFI-GCZBSULCSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -9.73
• 重原子数：
  50
• 可旋转键数：
  10
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.95
• 拓扑面积：
  498
• 氢给体数：
  17
• 氢受体数：
  25

ADMET

毒理性

• 在妊娠和哺乳期间的影响

◉ 母乳喂养期间使用总结：阿米卡星在母乳中的排泄很少。新生儿显然会吸收少量其他氨基糖苷类药物，但使用典型的每日三次剂量时，血清水平远低于治疗新生儿感染时的水平，因此阿米卡星的系统性影响不太可能发生。较大的婴儿吸收的阿米卡星会更少。由于在多次每日剂量方案期间，母乳中阿米卡星水平的变异性很小，因此相对于剂量安排哺乳时间对减少婴儿接触几乎没有或没有好处。关于单次每日剂量方案的数据不可用。监测婴儿可能对胃肠道菌群的影响，如腹泻、念珠菌病（例如，鹅口疮、尿布疹）或罕见的情况下，大便中带血，提示可能的抗生素相关性结肠炎。 ◉ 对哺乳婴儿的影响：截至修订日期，没有找到相关的已发布信息。 ◉ 对泌乳和母乳的影响：截至修订日期，没有找到相关的已发布信息。

◉ Summary of Use during Lactation:Amikacin is poorly excreted into breastmilk. Newborn infants apparently absorb small amounts of other aminoglycosides, but serum levels with typical three times daily dosages are far below those attained when treating newborn infections and systemic effects of amikacin are unlikely. Older infants would be expected to absorb even less amikacin. Because there is little variability in the milk amikacin levels during multiple daily dose regimens, timing breastfeeding with respect to the dose is of little or no benefit in reducing infant exposure. Data are not available with single daily dose regimens. Monitor the infant for possible effects on the gastrointestinal flora, such as diarrhea, candidiasis (e.g., thrush, diaper rash) or rarely, blood in the stool indicating possible antibiotic-associated colitis. ◉ Effects in Breastfed Infants:Relevant published information was not found as of the revision date. ◉ 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

• Inorganic-polymer complexes for the controlled release of compounds including medicinals
  申请人：Royer Biomedical, Inc.

  公开号：US20030170307A1

  公开（公告）日：2003-09-11

  This invention relates generally to the production and use of inorganic-polymer complexes for the controlled release of compounds including medicinals. Advantageously, the inorganic used is calcium sulfate.

  本发明一般涉及无机聚合物复合物的生产和使用，用于控制化合物（包括药物）的释放。所使用的无机物最好是硫酸钙。
• EP1017364A4
  申请人：——

  公开号：EP1017364A4

  公开（公告）日：2006-06-28
• INORGANIC-POLYMER COMPLEXES FOR THE CONTROLLED RELEASE OF COMPOUNDS INCLUDING MEDICINALS
  申请人：Buford Biomedical Inc.

  公开号：EP1017364A1

  公开（公告）日：2000-07-12
• TREATMENT FOR PROGRESSIVE MULTIPLE SCLEROSIS
  申请人：UTI LIMITED PARTNERSHIP

  公开号：US20190262353A1

  公开（公告）日：2019-08-29

  In one aspect, there is provided a method of treating, prophylaxis, or amelioration of a neurological disease by administering to a subject in need thereof one or more compounds described herein. In a specific example, the neurological disease is multiple sclerosis (also referred to as “MS”).
• US6391336B1
  申请人：——

  公开号：US6391336B1

  公开（公告）日：2002-05-21