普拉格雷
普拉格雷(英語:Prasugrel)(在美國,澳大利亞和印度的商品名為Effient ,在歐盟與台灣的商品名為Efient,抑凝安 )是預防血凝塊形成的藥物。它是血小板抑制劑,為P2Y12ADP受體的不可逆拮抗劑,屬於thienopyridine類藥物。
臨床資料 | |
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商品名 | Effient, Efient |
AHFS/Drugs.com | Monograph |
MedlinePlus | a609027 |
核准狀況 |
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懷孕分級 |
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给药途径 | Oral |
ATC碼 | |
法律規範狀態 | |
法律規範 |
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藥物動力學數據 | |
生物利用度 | ≥79% |
血漿蛋白結合率 | Active metabolite: ~98% |
生物半衰期 | ~7 h (range 2 h to 15 h) |
排泄途徑 | 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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普拉格雷於2009年2月(歐洲)[1]和2009年7月(美國)被核准使用於降低急性冠心症病人經經皮冠狀動脈治療後的血栓形成(包括使用支架者)。 [2]
醫療用途
普拉格雷與低劑量阿司匹靈並用,可預防急性冠心症病人(包括不穩定性心絞痛 ,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。與氯吡格雷相比,普拉格雷的出血風險較高,但在減少死亡、復發性心肌梗塞和中風方面較佳。 [3]
考慮到出血的危險,普拉格雷不可用於75歲以上,體重低或有短暫性缺血發作或中風病史的患者。 [3] [4] 在預計接受經皮血管成形術的病人以外,並不建議在冠狀動脈造影之前使用普拉格雷。 [5] [6]
禁忌症
由於中風的風險較高(血栓性中風和顱內出血),因此對於有活動性病理性出血的患者,例如消化性潰瘍或短暫性腦缺血發作或中風的患者,不應使用本藥。 [7]
副作用
不良影響包括: [8]
藥物交互作用
普拉格雷的藥物交互作用並不強,例如即使與質子泵浦抑制劑一起使用以降低胃腸道出血時,仍不會喪失其抗血小板作用。 [9] [10] [11] [12]
參考文獻
- ^ 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.