Torres Fernando, Rubin Lewis J
UT Southwestern Medical Center, 5323 Harry Hines Boulevard, Dallas, TX 75390, USA.
Expert Rev Cardiovasc Ther. 2013 Jan;11(1):13-25. doi: 10.1586/erc.12.160.
Pulmonary arterial hypertension (PAH) is a progressive and fatal disease characterized by increasing pulmonary vascular resistance leading to right ventricular failure and death. Treprostinil is a stable prostacyclin analog approved for the treatment of PAH to improve exercise capacity. In the setting of PAH, the major pharmacological actions of treprostinil include vasodilatation of the pulmonary and systemic vascular beds, inhibition of platelet aggregation and inhibition of smooth muscle cell proliferation. Treprostinil therapy may be delivered via parenteral (subcutaneous and intravenous) or inhaled routes of administration, with oral tablets in the later stages of clinical development. In clinical trials, treprostinil has been shown to improve clinical status, functional class, exercise capacity and quality of life. Common side effects of treprostinil therapy include headache, flushing, jaw pain, diarrhea, and for subcutaneous administration, infusion site pain or reaction. This article provides an overview of treprostinil therapy for the treatment of PAH with a focus on the available efficacy and safety data for parenteral, inhaled and oral administration.
肺动脉高压（PAH）是一种进行性致命疾病，其特征是肺血管阻力增加，导致右心室衰竭和死亡。曲前列尼尔是一种稳定的前列环素类似物，已被批准用于治疗PAH以提高运动能力。在PAH的情况下，曲前列尼尔的主要药理作用包括肺和体循环血管床的血管舒张、抑制血小板聚集以及抑制平滑肌细胞增殖。曲前列尼尔治疗可通过胃肠外（皮下和静脉内）或吸入给药途径进行，在临床开发的后期阶段还有口服片剂。在临床试验中，曲前列尼尔已被证明可改善临床状况、功能分级、运动能力和生活质量。曲前列尼尔治疗的常见副作用包括头痛、潮红、颌部疼痛、腹泻，对于皮下给药，还有输注部位疼痛或反应。本文概述了曲前列尼尔治疗PAH的情况，重点介绍了胃肠外、吸入和口服给药的现有疗效和安全性数据。
