吡格列酮

化合物

吡格列酮Pioglitazone)是一種專門用於治療2型糖尿病[1]的口服藥物[2],屬於噻唑烷二酮类(活化受体调节剂)藥物的一種。

吡格列酮
臨床資料
商品名英语Drug nomenclatureActos, others
AHFS/Drugs.comMonograph
MedlinePlusa699016
核准狀況
懷孕分級
  • C
给药途径By mouth
藥物類別英语Drug classThiazolidinedione
ATC碼
法律規範狀態
法律規範
藥物動力學數據
血漿蛋白結合率>99%
药物代谢liver (CYP2C8)
生物半衰期3–7 hours
排泄途徑in bile
识别信息
  • (RS)-5-(4-[2-(5-ethylpyridin-2-yl)ethoxy]benzyl)thiazolidine-2,4-dione
CAS号111025-46-8  checkY
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard英语CompTox Chemicals Dashboard (EPA)
ECHA InfoCard100.114.441 編輯維基數據鏈接
化学信息
化学式C19H20N2O3S
摩尔质量356.44 g/mol
3D模型(JSmol英语JSmol
手性外消旋混合物
熔点183至184 °C(361至363 °F)
  • O=C1NC(=O)SC1Cc3ccc(OCCc2ncc(cc2)CC)cc3
  • 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) checkY
  • Key:HYAFETHFCAUJAY-UHFFFAOYSA-N checkY

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]

參考文獻

  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. 

外部連結