吡格列酮

吡格列酮（Pioglitazone）是一种专门用于治疗2型糖尿病^[1]的口服药物^[2]，属于噻唑烷二酮类（活化受体调节剂）药物的一种。

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吡格列酮

临床资料
商品名（英语：Drug nomenclature）	Actos, others
AHFS/Drugs.com	Monograph
MedlinePlus	a699016
核准状况	欧 EMA: yes 美 FDA: Actos
怀孕分级	C
给药途径	By mouth
药物类别	Thiazolidinedione
ATC码	A10BG03 (WHO)
法律规范状态
法律规范	英：处方药（℞-only） (POM) 美：处方药（℞-only）
药物动力学数据
血浆蛋白结合率	>99%
药物代谢	liver (CYP2C8)
生物半衰期	3–7 hours
排泄途径	in bile
识别信息
IUPAC命名法 (RS)-5-(4-[2-(5-ethylpyridin-2-yl)ethoxy]benzyl)thiazolidine-2,4-dione
CAS号	111025-46-8  Y
PubChem CID	4829
IUPHAR/BPS	2694
DrugBank	DB01132 Y
ChemSpider	4663 Y
UNII	X4OV71U42S
KEGG	D08378 Y
ChEBI	CHEBI:8228 Y
ChEMBL	ChEMBL595 Y
CompTox Dashboard（英语：CompTox Chemicals Dashboard） (EPA)	DTXSID3037129
ECHA InfoCard	100.114.441
化学信息
化学式	C19H20N2O3S
摩尔质量	356.44 g/mol
3D模型（JSmol（英语：JSmol））	交互式图像
手性	外消旋混合物
熔点	183至184 °C（361至363 °F）
SMILES O=C1NC(=O)SC1Cc3ccc(OCCc2ncc(cc2)CC)cc3
InChI InChI=1S/C19H20N2O3S/c1-2-13-3-6-15(20-12-13)9-10-24-16-7-4-14(5-8-16)11-17-18(22)21-19(23)25-17/h3-8,12,17H,2,9-11H2,1H3,(H,21,22,23) Y Key:HYAFETHFCAUJAY-UHFFFAOYSA-N Y

用途

其他用途

荟萃分析显示本品对重性抑郁障碍可能有效，起效率27%，安慰剂10%。^[3]也有用于双相障碍的，但荟萃分析未发现有用处。^[4]

荟萃分析显示对非酒精性脂肪肝有效果，已成为推荐之一。^[5]

研究

可导致果蝇延寿，对人效果不明。^[6]

有依照此物降低神经胶质细胞的观察，尝试用于自闭症的。但样本数较低，对于效果的观察暂不能认定正确。^[7]

对于阿尔茨海默症无效。^[8]

似乎可以治疗老鼠的阿片成瘾。^[9]

参考文献

1. British national formulary : BNF 76 76th. Pharmaceutical Press. 2018: 694. ISBN 9780857113382 （英语）.
2. Pioglitazone Hydrochloride Monograph for Professionals. Drugs.com. American Society of Health-System Pharmacists. [3 March 2019]. （原始内容存档于2020-08-15） （英语）.
3. Colle R, de Larminat D, Rotenberg S, Hozer F, Hardy P, Verstuyft C, Fève B, Corruble E. Pioglitazone could induce remission in major depression: a meta-analysis. Neuropsychiatric Disease and Treatment. 2017, 13: 9–16. PMC 5182046 . PMID 28031713. doi:10.2147/NDT.S121149 .
4. 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. September 2021, 143: 230–238. PMID 34509090. S2CID 237485915. doi:10.1016/j.jpsychires.2021.09.018.
5. Pouwels S, Sakran N, Graham Y, Leal A, Pintar T, Yang W, Kassir R, Singhal R, Mahawar K, Ramnarain D. Non-alcoholic fatty liver disease (NAFLD): a review of pathophysiology, clinical management and effects of weight loss. BMC Endocrine Disorders. March 2022, 22 (1): 63. PMC 8919523 . PMID 35287643. doi:10.1186/s12902-022-00980-1 .
6. Jafari M, Khodayari B, Felgner J, Bussel II, Rose MR, Mueller LD. Pioglitazone: an anti-diabetic compound with anti-aging properties (PDF). Biogerontology. December 2007, 8 (6): 639–51. PMID 17628757. S2CID 9714773. doi:10.1007/s10522-007-9105-7.
7. Doyle CA, McDougle CJ. Pharmacotherapy to control behavioral symptoms in children with autism. Expert Opinion on Pharmacotherapy. August 2012, 13 (11): 1615–29. PMID 22550944. S2CID 32144885. doi:10.1517/14656566.2012.674110.
8. Abyadeh M, Gupta V, Gupta V, Chitranshi N, Wu Y, Amirkhani A, Meyfour A, Sheriff S, Shen T, Dhiman K, Ghasem HS, Paul AH, Stuart LG, Mirzaei M. Comparative Analysis of Aducanumab, Zagotenemab and Pioglitazone as Targeted Treatment Strategies for Alzheimer's Disease. Aging and Disease. December 2021, 12 (8): 1964–1976. PMC 8612603 . PMID 34881080. doi:10.14336/AD.2021.0719.
9. de Guglielmo G, Kallupi M, Scuppa G, Demopulos G, Gaitanaris G, Ciccocioppo R. Pioglitazone attenuates the opioid withdrawal and vulnerability to relapse to heroin seeking in rodents. Psychopharmacology. January 2017, 234 (2): 223–234. PMID 27714428. doi:10.1007/s00213-016-4452-1.

外部链接

• Pioglitazone FAQ（页面存档备份，存于互联网档案馆）
• U.S. National Library of Medicine: Drug Information Portal - Pioglitazonee（页面存档备份，存于互联网档案馆）