Huang Nina S, Master Huzefa H, Fusco Julie A, Park Zoon H
Midwestern University Chicago College of Pharmacy, Downers Grove, IL, USA.
Consult Pharm. 2010 Nov;25(11):745-55. doi: 10.4140/TCP.n.2010.745.
To review the pharmacology, clinical efficacy, and tolerability of ticagrelor and to discuss implications for use in the elderly.
A literature search was conducted in MEDLINE from 1966 to July 2010 using the MESH terms and key words AZD6140, ticagrelor, P2Y12 receptor antagonist. The search was limited to studies in English language with human subjects.
Randomized controlled clinical trials were reviewed. References that were deemed relevant to pharmacodynamic/pharmacokinetic studies of P2Y₁₂ antagonists and their historical background were also included.
Ticagrelor is the first reversible oral P2Y₁₂ antagonist currently undergoing Food and Drug Administration review for approval. The advantages of ticagrelor over clopidogrel are a more rapid onset of action, offset, and reversibility at the platelet P2Y₁₂ receptor site. In the Study of Platelet Inhibition and Patient Outcomes trial, ticagrelor reduced the incidence of death as a result of cardiovascular causes, with no increase in major bleeding or bleeding related to coronary artery bypass graft (CABG) compared with clopidogrel. Subgroup analyses suggested that elderly patients may benefit more from ticagrelor than from clopidogrel. However, the increase in non-CABG-related bleeding and unique adverse events may limit ticagrelor's use in the elderly.
The use of ticagrelor in the elderly should be determined on a case-by-case basis. More studies need to be conducted prior to establishing a role in therapy for the elderly.
综述替格瑞洛的药理学、临床疗效及耐受性，并探讨其在老年人中应用的意义。
于1966年至2010年7月期间在MEDLINE中进行文献检索，使用医学主题词表（MESH）术语及关键词AZD6140、替格瑞洛、P2Y12受体拮抗剂。检索限于以人类为研究对象的英文研究。
对随机对照临床试验进行综述。还纳入了被认为与P2Y₁₂拮抗剂的药效学/药代动力学研究及其历史背景相关的参考文献。
替格瑞洛是首个目前正在接受美国食品药品监督管理局审批的可逆性口服P2Y₁₂拮抗剂。替格瑞洛相对于氯吡格雷的优势在于其在血小板P2Y₁₂受体位点起效更快、作用消失更快且具有可逆性。在血小板抑制与患者预后研究试验中，与氯吡格雷相比，替格瑞洛降低了心血管原因导致的死亡发生率，且未增加大出血或与冠状动脉旁路移植术（CABG）相关的出血。亚组分析表明，老年患者可能从替格瑞洛中获益多于氯吡格雷。然而，非CABG相关出血的增加及独特的不良事件可能会限制替格瑞洛在老年人中的应用。
替格瑞洛在老年人中的应用应逐案确定。在确立其在老年患者治疗中的作用之前，需要进行更多研究。
