迈妥林

迈妥林
临床资料
商品名（英语：Drug nomenclature）	Amatine, Proamatine, Gutron, others
其他名称	2-amino-N-[2-(2,5-dimethoxyphenyl)-2-hydroxy-ethyl]-acetamide
AHFS/Drugs.com	Monograph
MedlinePlus	a602023
核准状况	美 DailyMed: Midodrine;
怀孕分级	澳: C ; ;
给药途径	口服
ATC码	C01CA17 (WHO) ;
法律规范状态
法律规范	澳：限医生处方（S4）; 美：处方药（℞-only）;
识别信息
	IUPAC命名法 (RS)- N-[2-(2,5-Dimethoxyphenyl)-2-hydroxyethyl]glycinamide; ;
CAS号	42794-76-3
PubChem CID	4195;
IUPHAR/BPS	7240;
DrugBank	DB00211 ;
ChemSpider	4050 ;
UNII	6YE7PBM15H;
KEGG	D08220 ;
ChEBI	CHEBI:6933 ;
ChEMBL	ChEMBL1076 ;
CompTox Dashboard（英语：CompTox Chemicals Dashboard） (EPA)	DTXSID0023321 ;
ECHA InfoCard	100.050.842、100.151.349
化学信息
化学式	C12H18N2O4
摩尔质量	254.29 g·mol−1
3D模型（JSmol（英语：JSmol））	交互式图像;
手性	外消旋混合物
	SMILES O=C(NCC(O)c1cc(OC)ccc1OC)CN;
	InChI InChI=1S/C12H18N2O4/c1-17-8-3-4-11(18-2)9(5-8)10(15)7-14-12(16)6-13/h3-5,10,15H,6-7,13H2,1-2H3,(H,14,16) ; Key:PTKSEFOSCHHMPD-UHFFFAOYSA-N ;

迈妥林是血管加压/抗低血压药物，在1996年被美国食品药品监督管理局（FDA）批准用于治疗自主神经功能障碍和姿位性低血压。FDA在2010年8月提议撤回该核准，因为制造商Shire plc在药物上市后后未能完成所需的研究。^[2]^[3]

2010年9月，Shire plc收集了有关该药效果和安全性的进一步数据，FDA撤回上述提议并允许其继续供患者使用。^[4]Shire plc于2011年9月27日宣布，它将继续与FDA合作以最终批准该药物。^[5]

医疗用途

迈妥林适用于有症状之姿位性低血压的治疗。它可以减少头晕和晕厥，但病人可能发生鸡皮疙瘩，皮肤瘙痒，胃肠道不适，发冷，躺卧时血压升高和尿液潴留。 ^[6] ^[7] 小型研究还表明，米多君可用于预防血液透析病人的血压过度下降。 ^[8]

迈妥林也用于肝硬化的并发症。它也与奥曲肽一并用于肝肾症候群。其可能机制是内脏血管收缩和肾血管扩张。但对于此药物在肝肾症候群的治疗地位尚未有充分的研究。^[9]

禁忌症

患有严重器质性心脏病，急性肾脏疾病，尿液潴留，嗜铬细胞瘤或甲状腺毒症的患者禁用本药。仰卧时持续和过度高血压患者不应使用本药。

副作用

头痛，头部压力/饱胀感，血管扩张/脸红，头皮发麻，意识模糊/思维异常，口干，神经质/焦虑和皮疹。 ^[10]

药理学

迈多林是前体药物，其活性代谢产物为desglymidodrine，刺激_α1肾上腺素受体，作用于小动脉与静脉，使血管收缩，血压升高。Desglymidodrine不会刺激心脏β-肾上腺素受体。 Desglymidodrine难以跨越血脑屏障，对中枢神经系统无作用。

药物动力学

迈妥林于口服后被迅速吸收，血浆中水平在约半小时后达到峰值，并以约25分钟的半衰期下降，而代谢产物在服用后约1-2小时达到峰值浓度，半衰期约为3至4小时。迈妥林的绝对生物利用度（以desglymidodrine衡量）为93％。

参考文献

^ Proamatine- midodrine hydrochloride tablet. DailyMed. [14 August 2021]. （原始内容存档于2021-08-15）.
^ U.S. proposes withdrawal of Shire hypotension drug （页面存档备份，存于互联网档案馆）, Aug 16, 2010.
^ O'Riordan, Michael. FDA recommends withdrawal of midodrine. Food and Drug Administration. FDA proposes withdrawal of low blood pressure drug [press release]. August 16, 2010. TheHeart.org. [1 April 2011]. （原始内容存档于2012-03-11）.
^ Midodrine (ProAmatine, generic) Proposed Market Withdrawal – Update （页面存档备份，存于互联网档案馆） September 10, 2010.
^ Shire Announces Update on ProAmatime^{[永久失效链接]} September 27, 2011.
^ Izcovich, A.; Gonzalez Malla, C.; Manzotti, M.; Catalano, H. N.; Guyatt, G. Midodrine for orthostatic hypotension and recurrent reflex syncope: A systematic review. Neurology. 22 August 2014, 83 (13): 1170–1177. PMID 25150287. doi:10.1212/WNL.0000000000000815.
^ Standing and Supine Blood Pressure Outcomes Associated With Droxidopa and Midodrine in Patients With Neurogenic Orthostatic Hypotension: A Bayesian Meta-analysis and Mixed Treatment Comparison of Randomized Trials. Ann Pharmacother. July 2018: 1060028018786954. PMID 29972032. doi:10.1177/1060028018786954.
^ Prakash, S; Garg, AX; Heidenheim, AP; House, AA. Midodrine appears to be safe and effective for dialysis-induced hypotension: a systematic review.. Nephrology, Dialysis, Transplantation. Oct 2004, 19 (10): 2553–8. PMID 15280522. doi:10.1093/ndt/gfh420.
^ Karwa, R.; Woodis, C B. Midodrine and Octreotide in Treatment of Cirrhosis-Related Hemodynamic Complications. Annals of Pharmacotherapy. 31 March 2009, 43 (4): 692–699. PMID 19299324. doi:10.1345/aph.1L373.
^ MayoClinic.org. [2020-04-01]. （原始内容存档于2021-05-10）.

[1] Proamatine- midodrine hydrochloride tablet. DailyMed. [14 August 2021]. （原始内容存档于2021-08-15）.

[2] U.S. proposes withdrawal of Shire hypotension drug （页面存档备份，存于互联网档案馆）, Aug 16, 2010.

[3] O'Riordan, Michael. FDA recommends withdrawal of midodrine. Food and Drug Administration. FDA proposes withdrawal of low blood pressure drug [press release]. August 16, 2010. TheHeart.org. [1 April 2011]. （原始内容存档于2012-03-11）.

[4] Midodrine (ProAmatine, generic) Proposed Market Withdrawal – Update （页面存档备份，存于互联网档案馆） September 10, 2010.

[5] Shire Announces Update on ProAmatime^{[永久失效链接]} September 27, 2011.

[6] Izcovich, A.; Gonzalez Malla, C.; Manzotti, M.; Catalano, H. N.; Guyatt, G. Midodrine for orthostatic hypotension and recurrent reflex syncope: A systematic review. Neurology. 22 August 2014, 83 (13): 1170–1177. PMID 25150287. doi:10.1212/WNL.0000000000000815.

[7] Standing and Supine Blood Pressure Outcomes Associated With Droxidopa and Midodrine in Patients With Neurogenic Orthostatic Hypotension: A Bayesian Meta-analysis and Mixed Treatment Comparison of Randomized Trials. Ann Pharmacother. July 2018: 1060028018786954. PMID 29972032. doi:10.1177/1060028018786954.

[8] Prakash, S; Garg, AX; Heidenheim, AP; House, AA. Midodrine appears to be safe and effective for dialysis-induced hypotension: a systematic review.. Nephrology, Dialysis, Transplantation. Oct 2004, 19 (10): 2553–8. PMID 15280522. doi:10.1093/ndt/gfh420.

[9] Karwa, R.; Woodis, C B. Midodrine and Octreotide in Treatment of Cirrhosis-Related Hemodynamic Complications. Annals of Pharmacotherapy. 31 March 2009, 43 (4): 692–699. PMID 19299324. doi:10.1345/aph.1L373.

[10] MayoClinic.org. [2020-04-01]. （原始内容存档于2021-05-10）.

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