美金刚胺

美金刚胺
临床资料
商品名（英语：Drug nomenclature）	Axura, Ebixa, Namenda, others
AHFS/Drugs.com	Monograph
MedlinePlus	a604006
核准状况	欧 EMA: yes; 美 DailyMed: Namenda;
怀孕分级	澳: B2 ; ;
给药途径	口服
ATC码	N06DX01 (WHO) ;
法律规范状态
法律规范	澳：限医生处方（S4）; 欧：Rx-only; 英：处方药（℞-only） (POM); 美：处方药（℞-only）;
药物动力学数据
生物利用度	~100%
药物代谢	肝（<10%）
生物半衰期	60–100 小时
排泄途径	肾
识别信息
	IUPAC命名法 3,5-dimethyltricyclo[3.3.1.13,7]decan-1amine; or; 3,5-dimethyladamantan-1-amine; ;
CAS号	19982-08-2
PubChem CID	4054;
IUPHAR/BPS	4253;
DrugBank	DB01043 ;
ChemSpider	3914 ;
UNII	W8O17SJF3T;
KEGG	D08174 ;
ChEMBL	ChEMBL807 ;
CompTox Dashboard（英语：CompTox Chemicals Dashboard） (EPA)	DTXSID5045174 ;
ECHA InfoCard	100.217.937
化学信息
化学式	C12H21N
摩尔质量	179.31 g·mol−1
3D模型（JSmol（英语：JSmol））	交互式图像;
	SMILES NC12CC3(CC(C1)(CC(C2)C3)C)C;
	InChI InChI=1S/C12H21N/c1-10-3-9-4-11(2,6-10)8-12(13,5-9)7-10/h9H,3-8,13H2,1-2H3 ; Key:BUGYDGFZZOZRHP-UHFFFAOYSA-N ;

美金刚胺（Memantine）是用于减缓中度至重度阿尔茨海默症进展的药物^[2]^[3]，通过口服使用。^[2]

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美金刚胺的常见副作用包括头痛、便秘、嗜睡和头晕，^[2]^[3]严重的副作用可能包括血栓、精神病和心力衰竭。^[3]它的作用机理认为是阻挡N-甲基-D-天冬氨酸受体。^[2]

在美国于2003年批准用于美金刚胺医疗用途。^[2]它可作为通用名药物使用。^[3]2019年，美金刚胺是美国第169常用的处方药，有超过三百万张处方。^[4]^[5]

阿尔茨海默症与失智症

美金刚胺用于治疗中度至重度阿尔茨海默症，尤其是使用乙酰胆碱酶抑制剂耐受性不佳或是有禁忌症的病人。^[6]^[7]有治疗指引建议对于早期至中度失智症病人可考虑使用美金刚胺或乙酰胆碱酶抑制剂。^[8]

研究显示美金刚胺可造成中等程度的症状改善，^[9]对于中度至重度阿兹海默症病人可带来认知、性情、行为、日常活动方面，有小的正面效应。^[10]^[11]但对于早期病人似乎并无益处。^[12]

在2017年的一篇回顾文献指出，对于中度至重度失智症病人，并用美金刚胺与多奈哌齐（Donepezil）可带来有限的改善。^[13]英国英国国家健康与临床卓越机构（National Institute for Health and Clinical Excellence; NICE）在2018年提出了治疗指引，建议对于中度至中度失智症病人可考虑并用美金刚胺与多奈哌齐。^[14]

心理医学

双相情绪障碍症

曾研究使用美金刚胺治疗处于抑郁期的双相情绪障碍症患者，但统合分析的结果并不支持此用途。^[15]

自闭症

本药物对于自闭症的效果不明。^[16]^[17]

3-羟基苯环己哌啶
Rhynchophylline（英语：Rhynchophylline）

[1]
International brands for memantine. Drugs.com. [7 August 2017]. （原始内容存档于2019-04-25）.
[2]
Memantine Hydrochloride Monograph for Professionals. Drugs.com. American Society of Health-System Pharmacists. [3 March 2019]. （原始内容存档于2019-04-25）（英语）.
[3]
British national formulary : BNF 76 76. Pharmaceutical Press. 2018: 303–304. ISBN 9780857113382.
[4]
The Top 300 of 2019. ClinCalc. [16 October 2021]. （原始内容存档于2020-03-18）.
[5]
Memantine - Drug Usage Statistics. ClinCalc. [16 October 2021]. （原始内容存档于2022-01-03）.
[6]
Mount C, Downton C. Alzheimer disease: progress or profit?. Nature Medicine. July 2006, 12 (7): 780–784. PMID 16829947. doi:10.1038/nm0706-780 .
[7]
NICE review of technology appraisal guidance 111 January 18, 2011 Alzheimer's disease - donepezil, galantamine, rivastigmine and memantine (review): final appraisal determination 互联网档案馆的存档，存档日期21 March 2019.
[8]
Page AT, Potter K, Clifford R, McLachlan AJ, Etherton-Beer C. Medication appropriateness tool for co-morbid health conditions in dementia: consensus recommendations from a multidisciplinary expert panel. Internal Medicine Journal. October 2016, 46 (10): 1189–1197. PMC 5129475 . PMID 27527376. doi:10.1111/imj.13215.
^ 引用错误：没有为名为AMH2006的参考文献提供内容
[10]
McShane R, Westby MJ, Roberts E, Minakaran N, Schneider L, Farrimond LE, et al. Memantine for dementia. The Cochrane Database of Systematic Reviews. March 2019, 3 (3): CD003154. PMC 6425228 . PMID 30891742. doi:10.1002/14651858.CD003154.pub6.
[11]
van Dyck CH, Tariot PN, Meyers B, Malca Resnick E. A 24-week randomized, controlled trial of memantine in patients with moderate-to-severe Alzheimer disease. Alzheimer Disease and Associated Disorders. 2007, 21 (2): 136–143. PMID 17545739. S2CID 25621202. doi:10.1097/WAD.0b013e318065c495.
[12]
Schneider LS, Dagerman KS, Higgins JP, McShane R. Lack of evidence for the efficacy of memantine in mild Alzheimer disease. Archives of Neurology. August 2011, 68 (8): 991–998. PMID 21482915. doi:10.1001/archneurol.2011.69 .
[13]
Chen R, Chan PT, Chu H, Lin YC, Chang PC, Chen CY, Chou KR. Chen K , 编. Treatment effects between monotherapy of donepezil versus combination with memantine for Alzheimer disease: A meta-analysis. PLOS ONE. 21 August 2017, 12 (8): e0183586. Bibcode:2017PLoSO..1283586C. PMC 5565113 . PMID 28827830. doi:10.1371/journal.pone.0183586 .
[14]
Overview | Dementia: assessment, management and support for people living with dementia and their carers | Guidance | NICE. www.nice.org.uk. [6 August 2020]. （原始内容存档于12 August 2020）.
[15]
Bartoli F, Cavaleri D, Bachi B, Moretti F, Riboldi I, Crocamo C, Carrà G. Repurposed drugs as adjunctive treatments for mania and bipolar depression: A meta-review and critical appraisal of meta-analyses of randomized placebo-controlled trials. Journal of Psychiatric Research. November 2021, 143: 230–238. PMID 34509090. S2CID 237485915. doi:10.1016/j.jpsychires.2021.09.018.
[16]
Parr J. Autism. BMJ Clinical Evidence. January 2010, 2010. PMC 2907623 . PMID 21729335.
[17]
Hong MP, Erickson CA. Investigational drugs in early-stage clinical trials for autism spectrum disorder. Expert Opinion on Investigational Drugs (Informa UK Limited). August 2019, 28 (8): 709–718. PMID 31352835. S2CID 198967266. doi:10.1080/13543784.2019.1649656.

Lipton SA. The molecular basis of memantine action in Alzheimer's disease and other neurologic disorders: low-affinity, uncompetitive antagonism. Current Alzheimer Research. April 2005, 2 (2): 155–65. PMID 15974913. doi:10.2174/1567205053585846.

Memantine. Drug Information Portal. U.S. National Library of Medicine. [2022-02-15]. （原始内容存档于2022-02-15）.

[brands-1] [1]
International brands for memantine. Drugs.com. [7 August 2017]. （原始内容存档于2019-04-25）.

[AHFS2019-2] [2]
Memantine Hydrochloride Monograph for Professionals. Drugs.com. American Society of Health-System Pharmacists. [3 March 2019]. （原始内容存档于2019-04-25）（英语）.

[BNF76-3] [3]
British national formulary : BNF 76 76. Pharmaceutical Press. 2018: 303–304. ISBN 9780857113382.

[4] [4]
The Top 300 of 2019. ClinCalc. [16 October 2021]. （原始内容存档于2020-03-18）.

[5] [5]
Memantine - Drug Usage Statistics. ClinCalc. [16 October 2021]. （原始内容存档于2022-01-03）.

[MountC2006-6] [6]
Mount C, Downton C. Alzheimer disease: progress or profit?. Nature Medicine. July 2006, 12 (7): 780–784. PMID 16829947. doi:10.1038/nm0706-780 .

[NICE_Guidelines-7] [7]
NICE review of technology appraisal guidance 111 January 18, 2011 Alzheimer's disease - donepezil, galantamine, rivastigmine and memantine (review): final appraisal determination 互联网档案馆的存档，存档日期21 March 2019.

[8] [8]
Page AT, Potter K, Clifford R, McLachlan AJ, Etherton-Beer C. Medication appropriateness tool for co-morbid health conditions in dementia: consensus recommendations from a multidisciplinary expert panel. Internal Medicine Journal. October 2016, 46 (10): 1189–1197. PMC 5129475 . PMID 27527376. doi:10.1111/imj.13215.

[AMH2006-9] 引用错误：没有为名为AMH2006的参考文献提供内容

[10] [10]
McShane R, Westby MJ, Roberts E, Minakaran N, Schneider L, Farrimond LE, et al. Memantine for dementia. The Cochrane Database of Systematic Reviews. March 2019, 3 (3): CD003154. PMC 6425228 . PMID 30891742. doi:10.1002/14651858.CD003154.pub6.

[11] [11]
van Dyck CH, Tariot PN, Meyers B, Malca Resnick E. A 24-week randomized, controlled trial of memantine in patients with moderate-to-severe Alzheimer disease. Alzheimer Disease and Associated Disorders. 2007, 21 (2): 136–143. PMID 17545739. S2CID 25621202. doi:10.1097/WAD.0b013e318065c495.

[Review11-12] [12]
Schneider LS, Dagerman KS, Higgins JP, McShane R. Lack of evidence for the efficacy of memantine in mild Alzheimer disease. Archives of Neurology. August 2011, 68 (8): 991–998. PMID 21482915. doi:10.1001/archneurol.2011.69 .

[Chen2017-13] [13]
Chen R, Chan PT, Chu H, Lin YC, Chang PC, Chen CY, Chou KR. Chen K , 编. Treatment effects between monotherapy of donepezil versus combination with memantine for Alzheimer disease: A meta-analysis. PLOS ONE. 21 August 2017, 12 (8): e0183586. Bibcode:2017PLoSO..1283586C. PMC 5565113 . PMID 28827830. doi:10.1371/journal.pone.0183586 .

[14] [14]
Overview | Dementia: assessment, management and support for people living with dementia and their carers | Guidance | NICE. www.nice.org.uk. [6 August 2020]. （原始内容存档于12 August 2020）.

[repurposed2021-15] [15]
Bartoli F, Cavaleri D, Bachi B, Moretti F, Riboldi I, Crocamo C, Carrà G. Repurposed drugs as adjunctive treatments for mania and bipolar depression: A meta-review and critical appraisal of meta-analyses of randomized placebo-controlled trials. Journal of Psychiatric Research. November 2021, 143: 230–238. PMID 34509090. S2CID 237485915. doi:10.1016/j.jpsychires.2021.09.018.

[16] [16]
Parr J. Autism. BMJ Clinical Evidence. January 2010, 2010. PMC 2907623 . PMID 21729335.

[Hong_Erickson_2019_pp._709–718-17] [17]
Hong MP, Erickson CA. Investigational drugs in early-stage clinical trials for autism spectrum disorder. Expert Opinion on Investigational Drugs (Informa UK Limited). August 2019, 28 (8): 709–718. PMID 31352835. S2CID 198967266. doi:10.1080/13543784.2019.1649656.

[2]

[3]

[1]

[4]

[5]

[6]

[7]

[8]

[9]

[10]

[11]

[12]

[13]

[14]

[15]

[16]

[17]

阿尔茨海默症与失智症

心理医学

双相情绪障碍症

自闭症

Wikiwand in your browser!

美金刚胺

阿尔茨海默症与失智症

心理医学

双相情绪障碍症

自闭症

Wikiwand in your browser!

医疗用途

参见

参考资料

扩展阅读

外部链接

临床资料


商品名（英语：Drug nomenclature）	Axura, Ebixa, Namenda, others^[1]
AHFS/Drugs.com	Monograph
MedlinePlus	a604006
核准状况	欧 EMA: yes 美 DailyMed: Namenda
怀孕分级	澳: B2
给药途径	口服
ATC码	N06DX01 (WHO)
法律规范状态
法律规范	澳：限医生处方（S4）欧：Rx-only 英：处方药（℞-only） (POM) 美：处方药（℞-only）
药物动力学数据
生物利用度	~100%
药物代谢	肝（<10%）
生物半衰期	60–100 小时
排泄途径	肾
识别信息
IUPAC命名法 3,5-dimethyltricyclo[3.3.1.1^3,7]decan-1amine or 3,5-dimethyladamantan-1-amine
CAS号	19982-08-2 ^Y
PubChem CID	4054
IUPHAR/BPS	4253
DrugBank	DB01043^Y
ChemSpider	3914^Y
UNII	W8O17SJF3T
KEGG	D08174^Y
ChEMBL	ChEMBL807^Y
CompTox Dashboard（英语：CompTox Chemicals Dashboard） (EPA)	DTXSID5045174
ECHA InfoCard	100.217.937
化学信息
化学式	C₁₂H₂₁N
摩尔质量	179.31 g·mol⁻¹
3D模型（JSmol（英语：JSmol））	交互式图像
SMILES NC12CC3(CC(C1)(CC(C2)C3)C)C
InChI InChI=1S/C12H21N/c1-10-3-9-4-11(2,6-10)8-12(13,5-9)7-10/h9H,3-8,13H2,1-2H3^Y Key:BUGYDGFZZOZRHP-UHFFFAOYSA-N^Y