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布瑞哌唑

维基百科,自由的百科全书
布瑞哌唑
临床资料
读音/brɛkˈspɪprəzl/ brek-SPIP-rə-zohl
商品名英语Drug nomenclatureRexulti, Rxulti, others
其他名称OPC-34712
AHFS/Drugs.comMonograph
MedlinePlusa615046
核准状况
怀孕分级
给药途径口服给药
药物类别非典型抗精神病药物
ATC码
法律规范状态
法律规范
药物动力学数据
生物利用度95% (T最大 = 4 小时)[9]
血浆蛋白结合率>99%
药物代谢肝脏 (主要透过CYP3A4CYP2D6)
生物半衰期91 小时 (布瑞哌唑), 86 小时 (主要代谢物)
排泄途径粪便 (46%), 尿液 (25%)
识别信息
  • 7-[4-[4-(1-benzothiophen-4-yl)piperazin-1-yl]butoxy]quinolin-2(1H)-one
CAS号913611-97-9
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard英语CompTox Chemicals Dashboard (EPA)
ECHA InfoCard100.242.305 编辑维基数据链接
化学信息
化学式C25H27N3O2S
摩尔质量433.57 g·mol−1
3D模型(JSmol英语JSmol
  • O=C5/C=C\c4ccc(OCCCCN3CCN(c1cccc2sccc12)CC3)cc4N5
  • InChI=1S/C25H27N3O2S/c29-25-9-7-19-6-8-20(18-22(19)26-25)30-16-2-1-11-27-12-14-28(15-13-27)23-4-3-5-24-21(23)10-17-31-24/h3-10,17-18H,1-2,11-16H2,(H,26,29)
  • Key:ZKIAIYBUSXZPLP-UHFFFAOYSA-N

布瑞哌唑INN:Brexpiprazole)是一种非典型抗精神病药物,用于治疗精神分裂症重性抑郁障碍[12]。需用于12岁以上的精神分裂症患者[12]。也用于治疗失智症患者的躁动英语Agitation[13]。口服使用[14]

常见副作用包括体重增加和动作障碍疾病英语Movement disorder(即静坐不能[12]。其他副作用包括可能抗精神药物恶性症候群迟发性运动不能糖尿病、赌博问题和白血球减少症[12]。用于老年失智症患者会增加死亡风险[12]。孕期安全性不明[15]。一般认为它会影响大脑中的多巴胺血清素去甲肾上腺素[14]

布瑞哌唑于2015年及2018年在美国及欧洲取得医疗使用许可[12] [14]。自 2022年起,英国不再使用[16]

参考文献

[编辑]
  1. ^ Brexpiprazole (Rexulti) Use During Pregnancy. Drugs.com. 10 February 2020 [18 August 2020]. 
  2. ^ 2.0 2.1 Rexulti brexpiprazole 4 mg film coated tablets blisters (273224). Therapeutic Goods Administration英语Therapeutic Goods Administration (TGA). [26 February 2023]. 
  3. ^ AusPAR: Brexpiprazole
  4. ^ Prescription medicines: registration of new chemical entities in Australia, 2017. Therapeutic Goods Administration (TGA). 21 June 2022 [9 April 2023]. 
  5. ^ Prescription medicines and biologicals: TGA annual summary 2017. Therapeutic Goods Administration (TGA). 21 June 2022 [31 March 2024]. 
  6. ^ Rexulti Product information. Health Canada. [26 February 2023]. 
  7. ^ Rexulti monograph
  8. ^ Mental health. Health Canada. 9 May 2018 [13 April 2024]. 
  9. ^ 9.0 9.1 Rexulti- brexpiprazole tablet Rexulti- brexpiprazole kit. DailyMed. 21 February 2023 [26 February 2023]. 
  10. ^ Rxulti EPAR. European Medicines Agency (EMA). 17 September 2018 [26 February 2023].  Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
  11. ^ Anvisa. RDC Nº 784 - Listas de Substâncias Entorpecentes, Psicotrópicas, Precursoras e Outras sob Controle Especial [Collegiate Board Resolution No. 784 - Lists of Narcotic, Psychotropic, Precursor, and Other Substances under Special Control]. Diário Oficial da União英语Diário Oficial da União. 31 March 2023 (4 April 2023) [16 August 2023]. (原始内容存档于3 August 2023) (巴西葡萄牙语). 
  12. ^ 12.0 12.1 12.2 12.3 12.4 12.5 DailyMed - REXULTI- brexpiprazole tablet. dailymed.nlm.nih.gov. [11 January 2022]. (原始内容存档于11 May 2021). 
  13. ^ Drug to treat agitation in Alzheimer’s patients approved in Canada - National | Globalnews.ca. Global News. January 25, 2024 [26 January 2024]. (原始内容存档于26 January 2024). 
  14. ^ 14.0 14.1 14.2 Rxulti. [11 January 2022]. (原始内容存档于12 January 2022). 
  15. ^ Brexpiprazole (Rexulti) Use During Pregnancy. Drugs.com. [11 January 2022]. (原始内容存档于5 December 2020) (英语). 
  16. ^ Brexpiprazole. SPS - Specialist Pharmacy Service. 10 February 2016 [11 January 2022]. (原始内容存档于12 January 2022). 

外部链接

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