阿戈美拉汀

阿戈美拉汀
臨床資料
商品名（英语：Drug nomenclature）	维度新、煩多閃（Valdoxan）
AHFS/Drugs.com	国际药品名称
核准狀況	歐 EMA: yes;
懷孕分級	澳: B1 ; ;
给药途径	Oral
ATC碼	N06AX22 (WHO) ;
法律規範狀態
法律規範	澳：限医生处方（S4）; 英：处方药（℞-only） (POM);
藥物動力學數據
生物利用度	1%
血漿蛋白結合率	95%
药物代谢	肝脏 (90% CYP1A2 和10% CYP2C9)
生物半衰期	1-2 小时
排泄途徑	尿液 (80%, 大部分是代谢产物)
识别信息
	IUPAC命名法 N-[2-(7-methoxynaphthalen-1-yl)ethyl]acetamide; ;
CAS号	138112-76-2
PubChem CID	82148;
IUPHAR/BPS	198;
DrugBank	DB06594 ;
ChemSpider	74141 ;
UNII	137R1N49AD;
KEGG	D02578 ;
ChEMBL	ChEMBL10878 ;
CompTox Dashboard（英语：CompTox Chemicals Dashboard） (EPA)	DTXSID3057642 ;
ECHA InfoCard	100.157.896
化学信息
化学式	C15H17NO2
摩尔质量	243.31 g·mol−1
3D模型（JSmol（英语：JSmol））	交互式图像;
	SMILES O=C(NCCc1c2c(ccc1)ccc(OC)c2)C;
	InChI InChI=1S/C15H17NO2/c1-11(17)16-9-8-13-5-3-4-12-6-7-14(18-2)10-15(12)13/h3-7,10H,8-9H2,1-2H3,(H,16,17) ; Key:YJYPHIXNFHFHND-UHFFFAOYSA-N ;

阿戈美拉汀（英語：Agomelatine） ，商品名为煩多閃 / 維度新（Valdoxan），是一种褪黑素受体激动剂类抗抑郁药，由法国施维雅（Servier）公司研制。阿戈美拉汀主要用来治疗重度抑郁症（MDD），并且证据指出阿戈美拉汀不会产生停药综合症和导致性功能障碍（对比SSRI、SNRI与三环类抗抑郁药）。阿戈美拉汀对改善睡眠和认知也有积极的作用。澳大利亚也批准用于广泛性焦虑症。^[2]^[3]

最主要的副作用是转氨酶升高。2.5%的患者会在吃药的前两周出现转氨酶超过参考值三倍以上，但不改变剂量继续服药也会自动改善。^[2]^[4]如果转氨酶在两个月左右仍然不正常，则不应继续使用。吃药前转氨酶就异常的患者也不应使用。在维持这两个措施的前提下，此药不会增加肝衰竭的可能性。^[5]

一般不会造成日间嗜睡，反而能提升日间清醒程度。^[2]总体有效程度和典型抗抑郁药相仿，但由于副作用退出的患者少很多。^[6]^[7]

除了批准用途外，对睡眠节律的障碍也有效果。^[8]有用于季节性抑郁的，但效果暂不足Cochrane下定论。^[9]

结构

引用

^ ^1.0 ^1.1 ^1.2 ^1.3 ^1.4 VALDOXAN® Product Information (PDF). TGA eBusiness Services. Servier Laboratories Pty Ltd. 2013-09-23 [2013-10-14]. （原始内容存档于2017-03-24）.
^ ^2.0 ^2.1 ^2.2 Valdoxan Product Information (PDF). TGA eBusiness Services. Servier Laboratories Pty Ltd. 2013-09-23 [2013-10-14]. （原始内容存档于2017-03-24）.
^ Guaiana G, Gupta S, Chiodo D, Davies SJ, Haederle K, Koesters M. Agomelatine versus other antidepressive agents for major depression. The Cochrane Database of Systematic Reviews. December 2013, (12): CD008851. PMC 11289707 . PMID 24343836. doi:10.1002/14651858.CD008851.pub2.
^ https://pubmed.ncbi.nlm.nih.gov/27342740/
^ Pladevall-Vila M, Pottegård A, Schink T, Reutfors J, Morros R, Poblador-Plou B, Timmer A, Forns J, Hellfritzsch M, Reinders T, Hägg D, Giner-Soriano M, Prados-Torres A, Cainzos-Achirica M, Hallas J, Brandt L, Cortés J, Aguado J, Perlemuter G, Falissard B, Castellsagué J, Jacquot E, Deltour N, Perez-Gutthann S. Risk of Acute Liver Injury in Agomelatine and Other Antidepressant Users in Four European Countries: A Cohort and Nested Case-Control Study Using Automated Health Data Sources. CNS Drugs. April 2019, 33 (4): 383–395. PMC 6441103 . PMID 30830574. doi:10.1007/s40263-019-00611-9.
^ Taylor D, Sparshatt A, Varma S, Olofinjana O. Antidepressant efficacy of agomelatine: meta-analysis of published and unpublished studies. BMJ. March 2014, 348: g1888. PMC 3959623 . PMID 24647162. doi:10.1136/bmj.g1888.
^ Cipriani A, Furukawa TA, Salanti G, Chaimani A, Atkinson LZ, Ogawa Y, Leucht S, Ruhe HG, Turner EH, Higgins JP, Egger M, Takeshima N, Hayasaka Y, Imai H, Shinohara K, Tajika A, Ioannidis JP, Geddes JR. Comparative efficacy and acceptability of 21 antidepressant drugs for the acute treatment of adults with major depressive disorder: a systematic review and network meta-analysis. Lancet. April 2018, 391 (10128): 1357–1366. PMC 5889788 . PMID 29477251. doi:10.1016/S0140-6736(17)32802-7 （英语）.
^ Williams WP, McLin DE, Dressman MA, Neubauer DN. Comparative Review of Approved Melatonin Agonists for the Treatment of Circadian Rhythm Sleep-Wake Disorders. Pharmacotherapy. September 2016, 36 (9): 1028–41. PMC 5108473 . PMID 27500861. doi:10.1002/phar.1822.
^ Nussbaumer-Streit B, Greenblatt A, Kaminski-Hartenthaler A, Van Noord MG, Forneris CA, Morgan LC, Gaynes BN, Wipplinger J, Lux LJ, Winkler D, Gartlehner G. Melatonin and agomelatine for preventing seasonal affective disorder. The Cochrane Database of Systematic Reviews. June 2019, 2019 (6): CD011271. PMC 6578031 . PMID 31206585. doi:10.1002/14651858.CD011271.pub3.

[PI-1] 1.0 ^1.1 ^1.2 ^1.3 ^1.4 VALDOXAN® Product Information (PDF). TGA eBusiness Services. Servier Laboratories Pty Ltd. 2013-09-23 [2013-10-14]. （原始内容存档于2017-03-24）.

[AU_PI-2] 2.0 ^2.1 ^2.2 Valdoxan Product Information (PDF). TGA eBusiness Services. Servier Laboratories Pty Ltd. 2013-09-23 [2013-10-14]. （原始内容存档于2017-03-24）.

[Gua2013-3] Guaiana G, Gupta S, Chiodo D, Davies SJ, Haederle K, Koesters M. Agomelatine versus other antidepressive agents for major depression. The Cochrane Database of Systematic Reviews. December 2013, (12): CD008851. PMC 11289707 . PMID 24343836. doi:10.1002/14651858.CD008851.pub2.

[4] ttps://pubmed.ncbi.nlm.nih.gov/27342740/

[5] Pladevall-Vila M, Pottegård A, Schink T, Reutfors J, Morros R, Poblador-Plou B, Timmer A, Forns J, Hellfritzsch M, Reinders T, Hägg D, Giner-Soriano M, Prados-Torres A, Cainzos-Achirica M, Hallas J, Brandt L, Cortés J, Aguado J, Perlemuter G, Falissard B, Castellsagué J, Jacquot E, Deltour N, Perez-Gutthann S. Risk of Acute Liver Injury in Agomelatine and Other Antidepressant Users in Four European Countries: A Cohort and Nested Case-Control Study Using Automated Health Data Sources. CNS Drugs. April 2019, 33 (4): 383–395. PMC 6441103 . PMID 30830574. doi:10.1007/s40263-019-00611-9.

[Taylor2014-6] Taylor D, Sparshatt A, Varma S, Olofinjana O. Antidepressant efficacy of agomelatine: meta-analysis of published and unpublished studies. BMJ. March 2014, 348: g1888. PMC 3959623 . PMID 24647162. doi:10.1136/bmj.g1888.

[Cip2018-7] Cipriani A, Furukawa TA, Salanti G, Chaimani A, Atkinson LZ, Ogawa Y, Leucht S, Ruhe HG, Turner EH, Higgins JP, Egger M, Takeshima N, Hayasaka Y, Imai H, Shinohara K, Tajika A, Ioannidis JP, Geddes JR. Comparative efficacy and acceptability of 21 antidepressant drugs for the acute treatment of adults with major depressive disorder: a systematic review and network meta-analysis. Lancet. April 2018, 391 (10128): 1357–1366. PMC 5889788 . PMID 29477251. doi:10.1016/S0140-6736(17)32802-7 （英语）.

[Williams2016-8] Williams WP, McLin DE, Dressman MA, Neubauer DN. Comparative Review of Approved Melatonin Agonists for the Treatment of Circadian Rhythm Sleep-Wake Disorders. Pharmacotherapy. September 2016, 36 (9): 1028–41. PMC 5108473 . PMID 27500861. doi:10.1002/phar.1822.

[Nussbaumer2019-9] Nussbaumer-Streit B, Greenblatt A, Kaminski-Hartenthaler A, Van Noord MG, Forneris CA, Morgan LC, Gaynes BN, Wipplinger J, Lux LJ, Winkler D, Gartlehner G. Melatonin and agomelatine for preventing seasonal affective disorder. The Cochrane Database of Systematic Reviews. June 2019, 2019 (6): CD011271. PMC 6578031 . PMID 31206585. doi:10.1002/14651858.CD011271.pub3.

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