Dolasetron mesylate

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: Dolasetron mesylate
• 英文别名: methanesulfonic acid;[(3S,7R)-10-oxo-8-azatricyclo[5.3.1.03,8]undecan-5-yl] 1H-indole-3-carboxylate;hydrate
• 化学式: C20H26N2O7S
• 分子量: 438.5
• InChiKey: QTFFGPOXNNGTGZ-RCSCTSIBSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.2
• 重原子数：
  30
• 可旋转键数：
  3
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  126
• 氢给体数：
  3
• 氢受体数：
  8

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：关于在哺乳期间使用多拉司琼的信息很少。在获得更多数据之前，哺乳期间应谨慎使用多拉司琼。可以选择使用其他药物。 ◉ 对哺乳婴儿的影响：一项双盲研究随机选取了160名接受硬脊膜外麻醉下选择性剖宫产的妇女，一组接受患者自控静脉镇痛的标准治疗（ sufentanil ），另一组接受标准治疗加右美托咪定。右美托咪定以5 mcg/kg给药，随后以0.5 mcg/kg/小时的速度持续输注直到手术结束。后一组患者在术后2天内接受右美托咪定加 sufentanil 的患者自控静脉镇痛。两组都将25 mg的多拉司琼添加到患者自控静脉镇痛溶液中，所有母亲都给她们的婴儿哺乳。两组在产后第1天和第2天的婴儿行为神经学评估都良好。[1] ◉ 对泌乳和母乳的影响：一项双盲研究随机选取了160名接受硬脊膜外麻醉下选择性剖宫产的妇女，一组接受患者自控静脉镇痛的标准治疗（ sufentanil ），另一组接受标准治疗加右美托咪定。右美托咪定以5 mcg/kg给药，随后以0.5 mcg/kg/小时的速度持续输注直到手术结束。后一组患者在术后2天内接受右美托咪定加 sufentanil 的患者自控静脉镇痛。两组都将25 mg的多拉司琼添加到患者自控静脉镇痛溶液中。接受右美托咪定的患者首次泌乳的时间更短（28小时对比34小时），更快实现纯母乳喂养（8天对比11天），并且在产后第二天有更多的乳汁量。[1]

◉ Summary of Use during Lactation:Little information is available on the use of dolasetron during breastfeeding. Until more data become available, dolasetron should be used with caution during breastfeeding. An alternate drug may be preferred. ◉ Effects in Breastfed Infants:A double-blind study randomized 160 women receiving an elective cesarean section under spinal anesthesia to receive either sufentanil for patient-controlled intravenous analgesia (standard care) or standard care plus dexmedetomidine. Dexmedetomidine was given as 5 mcg/kg, followed by a continuous infusion of 0.5 mcg/kg per hour until the end of surgery. Patient in this latter group received dexmedetomidine plus sufentanil for patient-controlled intravenous analgesia postoperatively for 2 days. Both groups had 25 mg of dolasetron added to the patient-controlled intravenous analgesia solution and all mothers breastfed their infants. Both groups had good neonatal behavioral neurological assessments on days 1 and 2 postpartum.[1] ◉ Effects on Lactation and Breastmilk:A double-blind study randomized 160 women receiving an elective cesarean section under spinal anesthesia to receive either sufentanil for patient-controlled intravenous analgesia (standard care) or standard care plus dexmedetomidine. Dexmedetomidine was given as 5 mcg/kg, followed by a continuous infusion of 0.5 mcg/kg per hour until the end of surgery. Patient in this latter group received dexmedetomidine plus sufentanil for patient-controlled intravenous analgesia postoperatively for 2 days. Both groups had 25 mg of dolasetron added to the patient-controlled intravenous analgesia solution. Patients who received dexmedetomidine had a shorter time to the first lactation (28 vs 34 hours), achieved exclusive breastfeeding sooner (8 vs 11 days) and had a greater amount of milk on the second day postpartum.[1]

来源:Drugs and Lactation Database (LactMed)