CAS: 51384-51-1; Metoprolol
该化合物是一种选择性的乙-1肾上腺受体阻塞器,主要用于治疗高血压,腹膜切除剂和心脏衰竭.它属于被称为乙型阻塞剂的药物类别,抑制肾上腺素对心脏的影响,导致心率和血压下降.Metoproololol的特点是其生物利用率相对较高,并经常以杂酸或酸盐形式施用.该物质一般来自胃肠道,半衰期允许一次或两次日服.Metoprool还因其能够跨越血压屏障而闻名,这可能导致某些病人的...
- ⚠️《2026年兴奋剂目录》
- 英文名称Metoprolol
- 中文名称美托洛尔
- IUPAC名称1-(isopropylamino)-3-(4-(2-methoxyethyl)phenoxy)propan-2-ol
- 其它别名1-[4-(2-Methoxyethyl)-phenoxy]-3-(isopropylamino)-2-propanol
- CAS编号51384-51-1
- MFCD编号:MFCD00599534
- EINECS号:257-166-4
- 分子式:C15H25NO3
- 分子量:267.36
- 产品CID: 1503262
- 同类组份化合物CAS51384-51-1 (free base)56392-17-7 (tartrate)56392-18-8 (HCl)80274-67-5 (fumarate)98418-47-4 (succinate)
- 产品分类原料药 → 循环系统用药 → 抗心律失常药
物理性质
MSDS等安全信息
- GHS象形图
- GHS符号GHS07;
注释: Exclamation mark - 危险类别特定目标器官毒性 - 单次接触 类别3
皮肤腐蚀/刺激 类别2
严重眼刺激 类别2
生殖毒性 类别2
水生慢性毒性 类别2 - 警示词Warning(警告)
- 危险描述H335 |可能引起呼吸道刺激.
H315 |造成皮肤刺激.
H319 |造成严重眼刺激.
H361d |怀疑对胎儿造成损害.
H411 |对水生生物有毒并具有长期持续影响. - 防范说明P264-P280-P305+P351+P338-P337+P313P-P264-P280-P302+P352-P321-P332+P313-P362
- 安全声明Signs and Symptoms of Metoprolol Overdose | Metoprolol overdose can affect the heart, blood pressure, breathing, and nervous system and may cause life-threatening complications. The signs and symptoms of metoprolol overdose may vary depending on the amount taken, the time elapsed, and the presence of other drugs or medical conditions. Some of the possible signs and symptoms are lightheadedness, dizziness, and fainting due to hypotension (low blood pressure), severe bradycardia, often accompanied by varying degrees of heart block, shortness of breath, gasping, and wheezing due to bronchospasm. | Management of Metoprolol Overdose | Treatment will vary based on the amount of metoprolol taken, comorbidities, age, and other substances ingested. On arrival, assess ABCs (airway, breathing, circulation) and monitor appropriate blood work, including co-ingestants, ECG, large-bore IVs, and pregnancy status. Consult poison control/toxicology early in the course. Treatment choices include volume resuscitation, activated charcoal, whole bowel irrigation, nasogastric lavage, atropine, glucagon, calcium gluconate/calcium chloride, high-dose insulin, vasopressors, intralipid, transcutaneous, or transvenous pacemaker. Cardiac status and a current fluid balance will guide volume resuscitation. Activated charcoal is typically given 1 g/kg and usually only has efficacy if dosed within 1 to 2 hours of ingestion. If the patient has any altered mentation, caution is necessary to the possibility of aspiration. Whole bowel irrigation should be a consideration for extended-release preparations or large-quantity ingestion. | Nasogastric lavage is usually ineffective, except for large-quantity ingestions. The clinician may consider using atropine, although it is typically ineffective in moderate-to-severe overdoses. Calcium administration increases intracellular calcium at 60 mg/kg over 5 to 10 minutes of calcium gluconate. Calcium chloride at a dose of 10 to 20 mL of a 10% solution is an option if central access is obtained. Glucagon dosing is 50 mcg/kg as a bolus with drip titration. High-dose insulin at a dose of 1 unit/kg bolus followed by 1 unit/kg/h drip. | Administration with dextrose with a drip titrating to euglycemia and potassium repletion as needed. Vasopressors with epinephrine or norepinephrine titrated rate and blood pressure. Intralipid IV lipid emulsion therapy can serve as a lipid sink that extracts the drug from the myocyte. It may also provide free fatty acids as a substrate. This medication may affect some laboratory monitoring. Consider a transcutaneous or transvenous pacemaker. Extracorporeal membrane oxygenation should be considered for refractory cases. If the clinician is concerned about intentional overdose, they should order a mandatory psychiatric evaluation, considering any co-ingestants. For non-extended or non-sustained-release preparations, 4 to 6 hours of observation without any derangement of mental status or vital signs is sufficient. Any extended- or sustained-release preparation requires 12 to 24 hours of telemetry observation, depending on the preparation. Extra caution should be considered in the pediatric population as very low amounts, including one pill or even one-half pill, can cause cardiovascular collapse and death.
欧盟法规
ECHA物质C&L通报REACH预注册上下游产品
CAS号75-31-0 异丙胺 | CAS号56718-70-8 3-[4-(2-甲氧基乙基)苯... | CAS号56718-71-9 4-(2-甲氧乙基)苯酚 | CAS号81024-43-3 (R)-美托洛尔 | CAS号81024-42-2 (S)-美托洛尔 | CAS号56392-17-7 酒石酸美托洛尔 | CAS号56392-16-6 α-羟基美托洛尔(非对映异构体混合物)合成工艺路线路线简述
- 合成目标产物 Metoprolol 主要起始原料 Isopropylamine And [[p-(2-Methoxyethyl)Phenoxy]Methyl]Oxirane
- (文献来源)合成步骤主要原料 Isopropylamine 和 [[p-(2-Methoxyethyl)Phenoxy]Methyl]Oxirane
Metoprolol Tartrate置于dowex Marathon 11 Chloride Form体系中,用 水 作为反应溶剂,化学反应生成 美托洛尔
参考文献:The Solid-State Structure Of The β-Blocker Metoprolol: A Combined Experimental And In Silico Investigation
标题:The Solid-State Structure Of The β-Blocker Metoprolol: A Combined Experimental And In Silico Investigation
摘要:美托洛尔{系统标题:(Rs)-1-异丙基氨基-3-[4-(2-甲氧基乙基)苯氧基]丙-2-醇},C15H25No3,是一种心脏选择性β1-肾上腺素能阻断剂,其部分分子骨架与大量其他β-阻断剂相同.本文介绍了通过单晶和变温粉末 X 射线衍射以及差示扫描量热法对其进行固态表征的结果.通过分子建模,剑桥结构数据库(csd)调查和 Hirshfeld 表面分析,对其分子和晶体排列进行了进一步研究.在晶体中,带有异丙基的侧臂与其他 β 受体阻滞剂一样,采用了全反式构象,这是建模数据中最稳定的排列方式.美托洛尔的晶体结构以 O-H...N/n...H-O 对氢键为主(这一点也得到了 Hirshfeld 表面分析的证实),从而形成了沿 B 轴交替延伸的含有 R 和 S 美托洛尔分子的链,并辅以较弱的 O...H-N/n-H...O 对相互作用.此外,在同一堆分子中,部分沿 B 轴和 C 轴定向的 C-H...O 接触将同手性分子连接起来.在 Csd 中沉积的与美托洛尔结构相关的分子固态结构中,β-受体阻滞剂药物倍他洛尔在三维排列和相互作用方面显示出最接近的相似性.尽管两者非常相似,但这两种药物的晶格在温度升高时的反应却不同:美托洛尔呈各向异性膨胀,而倍他洛尔则呈各向同性热膨胀.
DOI:10.1107/s2053229618017084
海关参考信息
- 2902600000-乙苯
2905122000-异丙醇
2905310000-1,2-乙二醇
2905320000-1,2-丙二醇 - 💡 提示：海关信息按照顺序优先匹配，如需确认的海关信息，请参考相关资料。
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主要参考文献
1: Karlson BW, Dellborg M, Gullestad L, Aberg J, Sugg J, Herlitz J. A pharmacokinetic and pharmacodynamic comparison of immediate-release metoprolol and extended-release metoprolol CR/XL in patients with suspected acute myocardial infarction: a randomized, open-label study. Cardiology. 2014;127(2):73-82. doi: 10.1159/000355003. Epub 2013 Nov 14. Efficacy and safety of out-of-hospital intravenous metoprolol administration in anterior ST-segment elevation acute myocardial infarction: insights from the METOCARD-CNIC trial. Ann Emerg Med. 2015 Mar;65(3):318-24. doi: 10.1016/j.annemergmed.2014.07.010. Epub 2014 Aug 14. doi: 10.1111/bcp.12523.
4: Cho DY, Bae SH, Lee JK, Park JB, Kim YW, Lee S, Oh E, Kim BT, Bae SK. Effect of the potent CYP2D6 inhibitor sarpogrelate on the pharmacokinetics and pharmacodynamics of metoprolol in healthy male Korean volunteers. Xenobiotica. 2015 Mar;45(3):256-63. doi: 10.3109/00498254.2014.967824. Epub 2014 Sep 30. doi: 10.4103/0253-7613.140577.
6: Inoue S, Shimizu M, Arita K, Akimoto K. The effect of AST-120 on the single-dose pharmacokinetics of metoprolol extended-release tablets in healthy subjects. Drug Metabol Drug Interact. 2014;29(2):115-21. doi: 10.1515/dmdi-2013-0063. doi: 10.1038/clpt.2014.62. Epub 2014 Mar 17.
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