阿戈美拉汀

阿戈美拉汀
臨床資料
商品名（英語：Drug nomenclature）	維度新、煩多閃（Valdoxan）
AHFS/Drugs.com	國際藥品名稱
核准狀況	歐 EMA: yes;
懷孕分級	澳: B1 ; ;
給藥途徑	Oral
ATC碼	N06AX22 (WHO) ;
法律規範狀態
法律規範	澳：限醫生處方（S4）; 英：處方藥（℞-only） (POM);
藥物動力學數據
生物利用度	1%
血漿蛋白結合率	95%
藥物代謝	肝臟 (90% CYP1A2 和10% CYP2C9)
生物半衰期	1-2 小時
排泄途徑	尿液 (80%, 大部分是代謝產物)
識別資訊
	IUPAC命名法 N-[2-(7-methoxynaphthalen-1-yl)ethyl]acetamide; ;
CAS號	138112-76-2
PubChem CID	82148;
IUPHAR/BPS	198;
DrugBank	DB06594 ;
ChemSpider	74141 ;
UNII	137R1N49AD;
KEGG	D02578 ;
ChEMBL	ChEMBL10878 ;
CompTox Dashboard（英語：CompTox Chemicals Dashboard） (EPA)	DTXSID3057642 ;
ECHA InfoCard	100.157.896
化學資訊
化學式	C15H17NO2
摩爾質量	243.31 g·mol−1
3D模型（JSmol（英語：JSmol））	交互式圖像;
	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） ，商品名為煩多閃 / 維度新（Valdoxan），是一種褪黑素受體激動劑類抗抑鬱藥，由法國施維雅（Servier）公司研製。阿戈美拉汀主要用來治療重度抑鬱症（MDD），並且證據指出阿戈美拉汀不會產生停藥綜合症和導致性功能障礙（對比SSRI、SNRI與三環類抗抑鬱藥）。阿戈美拉汀對改善睡眠和認知也有積極的作用。澳大利亞也批准用於廣泛性焦慮症。^[2]^[3]

最主要的副作用是轉氨酶升高。2.5%的患者會在吃藥的前兩周出現轉氨酶超過參考值三倍以上，但其中36%患者不改變劑量繼續服藥也會自動改善。^[2]^[4]如果轉氨酶在兩個月左右仍然不正常，則不應繼續使用。吃藥前轉氨酶就異常的患者也不應使用。在維持這兩個措施的前提下，此藥不會增加肝衰竭的可能性。^[5]

一般不會造成日間嗜睡，反而能提升日間清醒程度。^[2]總體有效程度和典型抗抑鬱藥相仿，但由於副作用退出的患者少很多。^[6]^[7]

除了批准用途外，對睡眠節律的障礙也有效果。^[8]有用於季節性抑鬱的，但效果暫不足Cochrane下定論。^[9]

結構

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]. （原始內容存檔於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]. （原始內容存檔於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 （英語）.
^ 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]. （原始內容存檔於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]. （原始內容存檔於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 （英語）.

[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.

[1]

[2]

[3]

[4]

[5]

[6]

[7]

[8]

[9]