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5毫克普拉格雷的理论依据及临床药理学

The Rationale for and Clinical Pharmacology of Prasugrel 5 mg.

作者信息

Jakubowski Joseph A, Erlinge David, Alexopoulos Dimitrios, Small David S, Winters Kenneth J, Gurbel Paul A, Angiolillo Dominick J

机构信息

Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana, 46285, USA.

Department of Cardiology, Lund University, Lund, Sweden.

出版信息

Am J Cardiovasc Drugs. 2017 Apr;17(2):109-121. doi: 10.1007/s40256-016-0202-3.

Abstract

Prasugrel is a third-generation thienopyridine platelet P2Y adenosine diphosphate (ADP) receptor antagonist administered with aspirin for the treatment of patients with acute coronary syndrome (ACS) with planned percutaneous coronary intervention. Prasugrel is administered periprocedurally at an oral loading dose of 60 mg followed by daily maintenance doses (MDs) of 10 mg for most patients and 5 mg for patients weighing <60 kg or aged ≥75 years. Data from a prasugrel phase III study, TRITON-TIMI 38, suggested that a lower MD might be more suitable for patients weighing <60 kg or aged ≥75 years; subsequent pharmacokinetic and pharmacodynamic studies have indicated that prasugrel 5 mg reduced platelet reactivity in these populations to an extent similar to that of prasugrel 10 mg in heavier or younger patients. Clinical experience with prasugrel 5 mg is limited, and additional studies are needed to verify the clinical efficacy and safety of this dose in these challenging populations.

摘要

普拉格雷是一种第三代噻吩并吡啶类血小板P2Y二磷酸腺苷(ADP)受体拮抗剂,与阿司匹林联合使用,用于治疗计划进行经皮冠状动脉介入治疗的急性冠状动脉综合征(ACS)患者。普拉格雷在围手术期口服负荷剂量为60 mg,随后大多数患者每日维持剂量(MD)为10 mg,体重<60 kg或年龄≥75岁的患者为5 mg。普拉格雷III期研究TRITON-TIMI 38的数据表明,较低的维持剂量可能更适合体重<60 kg或年龄≥75岁的患者;随后的药代动力学和药效学研究表明,5 mg普拉格雷在这些人群中降低血小板反应性的程度与较重或较年轻患者中10 mg普拉格雷相似。5 mg普拉格雷的临床经验有限,需要更多研究来验证该剂量在这些具有挑战性的人群中的临床疗效和安全性。

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