普拉格雷
普拉格雷(英语:Prasugrel)(在美国,澳大利亚和印度的商品名为Effient ,在欧盟与台湾的商品名为Efient,抑凝安 )是预防血凝块形成的药物。它是血小板抑制剂,为P2Y12ADP受体的不可逆拮抗剂,属于thienopyridine类药物。
临床资料 | |
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商品名 | Effient, Efient |
AHFS/Drugs.com | Monograph |
MedlinePlus | a609027 |
核准状况 |
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怀孕分级 |
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给药途径 | Oral |
ATC码 | |
法律规范状态 | |
法律规范 |
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药物动力学数据 | |
生物利用度 | ≥79% |
血浆蛋白结合率 | Active metabolite: ~98% |
生物半衰期 | ~7 h (range 2 h to 15 h) |
排泄途径 | Urine (~68% inactive metabolites); feces (27% inactive metabolites) |
识别信息 | |
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CAS号 | 150322-43-3 389574-19-0(hydrochloride) |
PubChem CID | |
IUPHAR/BPS | |
DrugBank | |
ChemSpider | |
UNII | |
KEGG | |
ChEBI | |
ChEMBL | |
CompTox Dashboard (EPA) | |
ECHA InfoCard | 100.228.719 |
化学信息 | |
化学式 | C20H20FNO3S |
摩尔质量 | 373.44 g·mol−1 |
3D模型(JSmol) | |
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普拉格雷于2009年2月(欧洲)[1]和2009年7月(美国)被核准使用于降低急性冠心症病人经经皮冠状动脉治疗后的血栓形成(包括使用支架者)。 [2]
医疗用途
编辑普拉格雷与低剂量阿司匹灵并用,可预防急性冠心症病人(包括不稳定性心绞痛 ,非ST段上升型心肌梗塞 ( NSTEMI )和ST段上升型心肌梗塞( STEMI ))的血栓形成。与氯吡格雷相比,普拉格雷的出血风险较高,但在减少死亡、复发性心肌梗塞和中风方面较佳。 [3]
考虑到出血的危险,普拉格雷不可用于75岁以上,体重低或有短暂性缺血发作或中风病史的患者。 [3] [4] 在预计接受经皮血管成形术的病人以外,并不建议在冠状动脉造影之前使用普拉格雷。 [5] [6]
禁忌症
编辑由于中风的风险较高(血栓性中风和颅内出血),因此对于有活动性病理性出血的患者,例如消化性溃疡或短暂性脑缺血发作或中风的患者,不应使用本药。 [7]
副作用
编辑不良影响包括: [8]
药物交互作用
编辑普拉格雷的药物交互作用并不强,例如即使与质子泵浦抑制剂一起使用以降低胃肠道出血时,仍不会丧失其抗血小板作用。 [9] [10] [11] [12]
参考文献
编辑- ^ European Public Assessment Report for Efient (PDF). EMA. 2009 [2020-09-20]. (原始内容存档 (PDF)于2018-03-19).
- ^ Role of prasugrel, a novel P2Y(12) receptor antagonist, in the management of acute coronary syndromes. American Journal of Cardiovascular Drugs. 2009, 9 (4): 213–29. PMID 19655817. doi:10.2165/1131209-000000000-00000.
- ^ 3.0 3.1 Wiviott, Stephen D.; Braunwald, Eugene; McCabe, Carolyn H.; Montalescot, Gilles; Ruzyllo, Witold; Gottlieb, Shmuel; Neumann, Franz-Joseph; Ardissino, Diego; De Servi, Stefano. Prasugrel versus Clopidogrel in Patients with Acute Coronary Syndromes. New England Journal of Medicine. 15 November 2007, 357 (20): 2001–2015. PMID 17982182. doi:10.1056/NEJMoa0706482.
- ^ Chew, Derek P; Scott, Ian A; Cullen, Louise; French, John K; Briffa, Tom G; Tideman, Philip A; Woodruffe, Stephen; Kerr, Alistair; Branagan, Maree. National Heart Foundation of Australia and Cardiac Society of Australia and New Zealand: Australian clinical guidelines for the management of acute coronary syndromes 2016. Medical Journal of Australia. August 2016, 205 (3): 128–133. PMID 27465769. doi:10.5694/mja16.00368.
- ^ Bellemain-Appaix, A.; Kerneis, M.; O'Connor, S. A.; Silvain, J.; Cucherat, M.; Beygui, F.; Barthelemy, O.; Collet, J.-P.; Jacq, L. Reappraisal of thienopyridine pretreatment in patients with non-ST elevation acute coronary syndrome: a systematic review and meta-analysis. BMJ. 24 October 2014, 347 (aug06 2): g6269. PMC 4208629 . PMID 25954988. doi:10.1136/bmj.g6269.
- ^ Montalescot, Gilles; Bolognese, Leonardo; Dudek, Dariusz; Goldstein, Patrick; Hamm, Christian; Tanguay, Jean-Francois; ten Berg, Jurrien M.; Miller, Debra L.; Costigan, Timothy M. Pretreatment with Prasugrel in Non–ST-Segment Elevation Acute Coronary Syndromes. New England Journal of Medicine. 12 September 2013, 369 (11): 999–1010. PMID 23991622. doi:10.1056/NEJMoa1308075.
- ^ Effient (prasugrel hydrochloride) Prescribing Information. FDA. September 2011 [2020-09-20]. (原始内容存档于2017-01-18).
- ^ Efient: Highlights of prescribing information (PDF). [2020-09-20]. (原始内容存档 (PDF)于2019-07-10).
- ^ Current oral antiplatelets: focus update on prasugrel. Journal of the American Board of Family Medicine. 2012, 25 (3): 343–9. PMID 22570398. doi:10.3122/jabfm.2012.03.100270.
- ^ PPIs Are Not Responsible for Elevating Cardiovascular Risk in Patients on Clopidogrel-A Systematic Review and Meta-Analysis. Frontiers in Physiology. 2018-11-19, 9: 1550. PMC 6252380 . PMID 30510515. doi:10.3389/fphys.2018.01550.
- ^ Pharmacodynamic effect and clinical efficacy of clopidogrel and prasugrel with or without a proton-pump inhibitor: an analysis of two randomised trials. Lancet. September 2009, 374 (9694): 989–997. PMID 19726078. doi:10.1016/S0140-6736(09)61525-7.
- ^ Efficacy and Safety of Proton-Pump Inhibitors in High-Risk Cardiovascular Subsets of the COGENT Trial. The American Journal of Medicine. September 2016, 129 (9): 1002–5. PMID 27143321. doi:10.1016/j.amjmed.2016.03.042.