Methscopolamine | 155-41-9

• 物质功能分类: 原料药 - 消化系统用药 - 胃肠解痉药
• 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: Methscopolamine
• 英文别名: [(1R,2R,4S,5S)-9,9-dimethyl-3-oxa-9-azoniatricyclo[3.3.1.02,4]nonan-7-yl] (2S)-3-hydroxy-2-phenylpropanoate
• CAS: 155-41-9；13265-10-6
• 化学式: C18H24NO4+
• 分子量: 318.4
• InChiKey: LZCOQTDXKCNBEE-XJMZPCNVSA-N

物化性质

• 熔点：
  214-217 °C (decomp)
• 溶解度：
  H2O:50 mg/mL
• 颜色/状态：
  WHITE CRYSTALS OR WHITE CRYSTALLINE POWDER
• 气味：
  ODORLESS
• 蒸汽压力：
  1.04X10-14 mm Hg at 25 °C (est)

计算性质

• 辛醇/水分配系数(LogP)：
  1.3
• 重原子数：
  23
• 可旋转键数：
  5
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.61
• 拓扑面积：
  59.1
• 氢给体数：
  1
• 氢受体数：
  4

ADMET

代谢

...关于甲基硫酸阿托品溴化物在体内的分布或代谢命运，目前可用的信息很少。...甲基硫酸阿托品溴化物与其他季铵化合物一样，被认为主要通过尿液以未改变的药物和代谢物形式排泄，并且以未吸收的药物形式在粪便中排出。.../甲基硫酸阿托品溴化物/

... Little information is available on the distribution or metabolic fate of methscopolamine bromide in the body. ... Methscopolamine bromide, like other quaternary ammonium compounds, is believed to be excreted principally in urine as unchanged drug and metabolites and in the feces as unabsorbed drug. ... /Methscopolamine bromide/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 在妊娠和哺乳期间的影响

◉ 母乳喂养期间使用总结：目前没有关于哺乳期间使用溴化甲司坦的资料。由于溴化甲司坦是一种季铵化合物，它不太可能被吸收并达到婴儿的血液循环。长期使用溴化甲司坦可能会减少乳汁产量或乳汁排放，但单次剂量不太可能干扰哺乳。在长期使用期间，观察乳汁减少的迹象（例如，不饱，体重增长不良）。 为了显著减少使用眼药水后到达母乳中的药物量，可以在眼角处的泪囊上施加压力1分钟或更长时间，然后使用吸收性纸巾去除多余的溶液。 ◉ 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，没有在哺乳母亲中找到相关的已发布信息。抗胆碱药可以在动物中抑制泌乳，显然是通过抑制生长激素和催产素的分泌。抗胆碱药还可以减少非哺乳妇女的血清催乳素。在已建立泌乳的母亲中，催乳素水平可能不会影响她的哺乳能力。

◉ Summary of Use during Lactation:No information is available on the use of methscopolamine bromide during breastfeeding. Because methscopolamine bromide is a quaternary ammonium compound, it is not likely to be absorbed and reach the bloodstream of the infant. Long-term use of methscopolamine bromide might reduce milk production or milk letdown, but a single dose is unlikely to interfere with breastfeeding. During long-term use, observe for signs of decreased lactation (e.g., insatiety, poor weight gain). To substantially diminish the amount of drug that reaches the breastmilk after using eye drops, place pressure over the tear duct by the corner of the eye for 1 minute or more, then remove the excess solution with an absorbent tissue. ◉ Effects in Breastfed Infants:Relevant published information was not found as of the revision date. ◉ Effects on Lactation and Breastmilk:Relevant published information in nursing mothers was not found as of the revision date. Anticholinergics can inhibit lactation in animals, apparently by inhibiting growth hormone and oxytocin secretion. Anticholinergic drugs can also reduce serum prolactin in nonnursing women. The prolactin level in a mother with established lactation may not affect her ability to breastfeed.

来源:Drugs and Lactation Database (LactMed)

毒理性

• 相互作用

在麻醉状态下、自然呼吸的狗中，0.01%的甲氧阿托品溴化物气溶胶可以抑制乙酰胆碱（静脉注射或气溶胶形式）引起的肺力学变化。

IN ANESTHETIZED, SPONTANEOUSLY BREATHING DOGS, A 0.01% AEROSOL /OF METHSCOPOLAMINE BROMIDE/ INHIBITED ACETYLCHOLINE (IV OR AEROSOL)-INDUCED CHANGES IN PULMONARY MECHANICS. /METHSCOPOLAMINE BROMIDE/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 相互作用

附加的抗胆碱能效果可能是由与抗精神病药、三环类抗抑郁药以及其他具有抗胆碱能效果的药物同时使用所导致。与抗酸药同时使用可能会干扰溴化甲司卡林（美斯卡林）的吸收。

Additive anticholinergic effects may result from concomitant use with antipsychotics, tricyclic antidepressants, and other drugs with anticholinergic effects. Concomitant administration with antacids may interfere with the absorption of methscopolamine bromide. /Methscopolamine bromide/

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

特定药物和解毒剂：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)

吸收、分配和排泄

甲基硫酸阿托品是一种季铵盐，是东莨菪碱的四级铵衍生物。这类药物吸收差且不可靠。碱性四级铵衍生物的总吸收率为10-25%。吸收速率不详。季铵盐从完整皮肤的吸收有限，结膜渗透差。大多数这类药物的命运和排泄情况知之甚少。口服给药后，药物效果在大约一小时内出现，持续4到6小时。甲基硫酸阿托品穿过血脑屏障的能力有限。该药物主要在尿液中排出，部分通过胆汁或未吸收的药物随粪便排出。目前没有关于甲基硫酸阿托品在母乳中的数据；在给予阿托品后，已经发现了阿托品的痕迹。/甲基硫酸阿托品/

Methscopolamine bromide is a quaternary ammonium derivative of scopolamine. As a class, these agents are poorly and unreliably absorbed. Total absorption of quaternary ammonium derivatives of the alkaloids is 10-25%. Rate of absorption is not available. Quaternary ammonium salts have limited absorption from intact skin, and conjunctival penetration is poor. Little is known of the fate and excretion of most of these agents. Following oral administration, drug effects appear in about one hour and persist for 4 to 6 hours. Methscopolamine bromide has limited ability to cross the blood-brain barrier. The drug is excreted primarily in the urine and bile, or as unabsorbed drug in feces. There is no data on the presence of methscopolamine in breast milk; traces of atropine have been found after administration of atropine. /Methscopolamine bromide/

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

溴化甲司卡林，像其他季铵类药物一样，由于完全离子化，因此从胃肠道吸收不完全。关于溴化甲司卡林在体内的分布或代谢命运，目前可用的信息很少。季铵类抗胆碱药完全离子化，具有很差的脂溶性。因此，它们不易穿透中枢神经系统或眼睛。溴化甲司卡林，像其他季铵化合物一样，被认为主要通过尿液以未改变的药物和代谢物形式排泄，并通过粪便以未吸收的药物形式排出。口服给药的药物中，大量可能以未吸收的药物形式在粪便中排出。/溴化甲司卡林/

Methscopolamine bromide, like other quaternary ammonium drugs, is incompletely absorbed from the GI tract since it is completely ionized. Little information is available on the distribution or metabolic fate of methscopolamine bromide in the body. Quaternary ammonium antimuscarinics are completely ionized and possess poor lipid solubility. Accordingly, they do not readily penetrate the CNS or the eye. Methscopolamine bromide, like other quaternary ammonium compounds, is believed to be excreted principally in urine as unchanged drug and metabolites and in the feces as unabsorbed drug. Substantial amounts of orally administered drug are probably eliminated in feces as unabsorbed drug. /Methscopolamine bromide/

来源:Hazardous Substances Data Bank (HSDB)

安全信息

• 危险等级：
  6.1
• 危险品标志：
  T,N
• 安全说明：
  S36/37,S36/37/39,S45,S60,S61
• 危险类别码：
  R23/24/25,R20/21/22,R50/53
• WGK Germany：
  3
• 海关编码：
  2934999090
• 危险品运输编号：
  UN 1544 6.1/PG 3

制备方法与用途

用途

甲溴东莨菪碱主要用于治疗胃肠道疾病。

生物活性

Methscopolamine 是一种毒蕈碱型乙酰胆碱受体抑制剂。

靶点

Target: mAChR