Butylscopolamine

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羟基酸及其衍生物
• 英文名称: Butylscopolamine
• 英文别名: [(1R,2R,4S,5S)-9-butyl-9-methyl-3-oxa-9-azoniatricyclo[3.3.1.02,4]nonan-7-yl] (2S)-3-hydroxy-2-phenylpropanoate
• 化学式: C21H30NO4+
• 分子量: 360.5
• InChiKey: YBCNXCRZPWQOBR-MWGADRMYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  26
• 可旋转键数：
  8
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.67
• 拓扑面积：
  59.1
• 氢给体数：
  1
• 氢受体数：
  4

ADMET

代谢

代谢主要通过酯键的水解发生。代谢物不被认为是显著活性的。

Metabolism occurs mainly through hydrolysis of the ester bond. The metabolites are not considered to be significantly active.

来源:DrugBank

代谢

主要代谢途径是酯键的水解裂解。在肾脏中排泄的代谢产物几乎不与毒蕈碱受体结合，因此认为它们不会对丁溴东莨菪碱的药效产生影响。/丁溴东莨菪碱/

The main metabolic pathway is hydrolytic cleavage of the ester bond. The metabolites that are excreted in the kidneys bind barely to muscarinic receptors and are not considered to contribute to the effect of hyoscine butylbromide. /Hyoscine butylbromide/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 相互作用

与多巴胺受体拮抗剂（如甲氧氯普胺）同时给药可以减少两药对胃肠道的效应。丁溴东莨菪碱可增强β-肾上腺素受体激动剂（β-阻断剂）的心率加快效应。/丁溴东莨菪碱/

Concomitant administration of dopamine receptor antagonists such as metoclopramide can reduce the effect of both drugs on the GI tract. Hyoscine butylbromide can increase the tachycardic effect of beta-adrenoceptor agonists (beta-blockers). /Hyoscine butylbromide/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 相互作用

当山莨菪碱丁溴化物与其他抗胆碱药同时开具时，增强副交感神经作用的可能性较低（因其吸收率低），但也不能排除。因此，三环类抗抑郁药、抗组胺药、奎尼丁、金刚烷胺和双异丙酰胺的抗胆碱作用可能会被山莨菪碱丁溴化物加强。由于三环类抗抑郁药的抗胆碱不良反应可能会被山莨菪碱丁溴化物加强，并且没有临床数据表明通过调整一种或两种药物的剂量如何影响这种可能的相互作用，因此建议这些药物不应同时使用。/山莨菪碱丁溴化物/

When hyoscine butylbromide is concomitantly prescribed with other anticholinergics, the likelihood of an enhanced parasympathetic action is low (because of its low absorption) but cannot be excluded. As such, the anticholinergic effect of tricyclic antidepressants, antihistamines, quinidine, amantadine and disopyramide can be intensified by hyoscine butylbromide. Because the anticholinergic adverse effects of tricyclic antidepressants can be intensified by hyoscine butylbromide, and because there are no clinical data on how this possible interaction is affected by dose adjustment of one or both drugs, it is recommended that these drugs should not be used concomitantly. /Hyoscine butylbromide/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 解毒与急救

紧急和支持性措施：保持呼吸道通畅，必要时辅助呼吸。如果出现高热、昏迷、横纹肌溶解和癫痫，则进行治疗。/抗胆碱能药物/

Emergency and supportive measures: Maintain an open airway and assist ventilation if needed. Treat hyperthermia, coma, rhabdomyolysis, and seizures if they occur. /Anticholinergics/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 解毒与急救

特定药物和解药：可以给严重中毒的患者（例如，高热、严重谵妄或心动过速）小剂量毒扁豆碱……。注意：毒扁豆碱可能会导致房室传导阻滞、心搏停止和癫痫，特别是在三环类抗抑郁药过量的患者中。新斯的明，一种外周作用的胆碱酯酶抑制剂，可能有助于治疗抗胆碱能引起的肠梗阻。/抗胆碱能药物/

Specific drugs and antidotes: A small dose of physostigmine .... can be given to patients with severe toxicity (e.g., hyperthermia, severe delirium, or tachycardia). Caution: Physostigmine can cause AV block, asystole, and seizures, especially in patients with tricyclic antidepressant overdose. Neostigmine, a peripherally acting cholinesterase inhibitor, may be useful in treating anticholinergic-induced ileus. /Anticholinergics/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 解毒与急救

Decontamination: 如果条件适当，口服活性炭。如果可以迅速给予活性炭，中小量摄入后不需要洗胃。由于胃肠道运动减慢，即使在晚期就诊的患者中，肠道去污程序也可能有所帮助。/抗胆碱能药物/

Decontamination: Administer activated charcoal orally if conditions are appropriate. Gastric lavage is not necessary after small to moderate ingestions if activated charcoal can be given promptly. Because of slowed gastrointestinal motility, gut decontamination procedures may be helpful even in late-presenting patients. /Anticholinergics/

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

• 吸收

丁溴东莨菪碱的口服生物利用度极低，仅有0.25-0.82%能够达到系统循环。血浆浓度峰值在0.25-2小时达到。丁溴东莨菪碱不会穿过血脑屏障。

Scopolamine butylbromide has extremely low oral bioavailability with only 0.25-0.82% reaching systemic circulation. Peak plasma concentration is reached 0.25-2 hours. Scopolamine butylbromide does not cross the blood brain barrier.

来源:DrugBank

吸收、分配和排泄

• 消除途径

主要随粪便排出（69.7%），尿液中仅有极少部分（4.4%）。由于丁溴东莨菪碱吸收不良，仅有2.8%通过胆汁排出。

Mainly eliminated in the feces (69.7%) with very little in the urine (4.4%). Only 2.8% is eliminated via the bile owing to scopolamine butylbromide's poor absorption.

来源:DrugBank

吸收、分配和排泄

• 分布容积

分布容积为128升。

The volume of distribution is 128 liters.

来源:DrugBank

吸收、分配和排泄

• 清除

总清除率为每分钟1.2升。

Total clearace is 1.2 liters per minute.

来源:DrugBank

吸收、分配和排泄

静脉给药（以输注形式100毫克）后，氢溴酸山莨菪碱的血药浓度迅速下降，消除半衰期介于1到5小时之间。总清除率为1.2升/分钟，其中50%以原药形式通过肾脏排出。口服给药后的消除主要是通过粪便排出，伴有少量的尿液成分。/氢溴酸山莨菪碱/

After intravenous administration (100 mg as infusion), the plasma concentration of hyoscine butylbromide declines rapidly and the elimination half-life ranges between 1 and 5 hours. The total clearance is 1.2 L/min, of which 50% is excreted as unchanged drug through the kidneys . ... Elimination following oral administration is primarily via fecal excretion with a minor urinary component. /Hyoscine butylbromide/

来源:Hazardous Substances Data Bank (HSDB)

文献信息

• PREVENTIVE AND/OR REMEDY FOR HAND AND FOOT SYNDROME
  申请人：ONO Pharmaceutical Co., Ltd.

  公开号：EP2554184A1

  公开（公告）日：2013-02-06

  The agent for the prevention and/or treatment of Hand-Foot Syndrome comprising a compound with anticholinergic activity can be provided. The agent for the prevention and/or treatment of Hand-Foot Syndrome comprising a compound with anticholinergic activity can be safely administered to the patients with Hand-Foot Syndrome, and has shown the superior preventive and/or treatment effect against Hand-Foot Syndrome.

  可以提供由具有抗胆碱能活性的化合物组成的预防和/或治疗手足综合征的制剂。由具有抗胆碱能活性的化合物组成的预防和/或治疗手足综合征的制剂可安全地用于手足综合征患者，并显示出对手足综合征具有卓越的预防和/或治疗效果。
• PREVENTIVE AND/OR THERAPEUTIC AGENT OF HAND-FOOT SYNDROME
  申请人：Ishizaka Kazuhiro

  公开号：US20130045956A1

  公开（公告）日：2013-02-21

  The agent for the prevention and/or treatment of Hand-Foot Syndrome comprising a compound with anticholinergic activity can be provided. The agent for the prevention and/or treatment of Hand-Foot Syndrome comprising a compound with anticholinergic activity can be safely administered to the patients with Hand-Foot Syndrome, and has shown the superior preventive and/or treatment effect against Hand-Foot Syndrome.
• US8729056B2
  申请人：——

  公开号：US8729056B2

  公开（公告）日：2014-05-20