2-[(E)-[1-(2-amino-1,3-thiazol-4-yl)-2-[[(2R,3S)-2-methyl-4-oxo-1-sulfoazetidin-3-yl]amino]-2-oxoethylidene]amino]oxy-2-methylpropanoic acid

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 内酰胺类
• 英文名称: 2-[(E)-[1-(2-amino-1,3-thiazol-4-yl)-2-[[(2R,3S)-2-methyl-4-oxo-1-sulfoazetidin-3-yl]amino]-2-oxoethylidene]amino]oxy-2-methylpropanoic acid
• 化学式: C₁₃H₁₇N₅O₈S₂
• 分子量: 435.4
• InChiKey: WZPBZJONDBGPKJ-HMTIBFNOSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.3
• 重原子数：
  28
• 可旋转键数：
  7
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.46
• 拓扑面积：
  238
• 氢给体数：
  4
• 氢受体数：
  12

ADMET

毒理性

• 肝毒性

氨曲南具有与其他β-内酰胺类抗生素相似的全身毒性，但目前尚不清楚它是否会引起类似青霉素或头孢菌素类抗生素引起的肝损伤。在高剂量、静脉注射氨曲南治疗期间（10%至38%），无症状的血清转氨酶升高是常见的。酶异常通常是轻至中度、无症状、自限性的，不需要停药。在氨曲南治疗期间，酶升高的发生率略高于其他比较抗生素。由于没有报道过单个病例，因此可以认为由氨曲南引起的明显肝损伤和黄疸的情况极为罕见。因此，关于损伤的潜伏期或模式没有数据。有报道称在开始使用氨曲南后3到5天内出现明显的转氨酶升高的情况，但这些病例没有黄疸，并且一旦停药就迅速缓解。

Aztreonam has systemic toxicities that are similar to those of other beta lactam antibiotics, but it is unclear whether it can cause hepatic injury similar to that of the penicillins or cephalosporins. Asymptomatic serum aminotransferase elevations are common during high dose, intravenous aztreonam therapy (10% to 38%). The enzyme abnormalities are usually mild-to-moderate, asymptomatic, self-limited and not requiring drug discontinuation. Enzyme elevations occur slightly more commonly during aztreonam therapy than with other comparative antibiotics. Cases of frank liver injury and jaundice attributable to aztreonam must be extremely rare as no individual cases have been reported. For this reason, there is no data regarding the latency or pattern of the injury. Instances of marked aminotransferase elevations within 3 to 5 days of starting aztreonam have been reported, but these cases were without jaundice and resolved rapidly once the drug was stopped.

来源:LiverTox