Massachusetts General Hospital, 55 Fruit Street, Boston, MA 02114, USA.
Expert Rev Respir Med. 2012 Jun;6(3):255-65. doi: 10.1586/ers.12.23.
Treprostinil is a prostacyclin derivative approved for the treatment of pulmonary arterial hypertension by intravenous, subcutaneous and inhalational administration. Unlike its precursor epoprostenol, treprostinil is chemically stable at room temperature and neutral pH, and its plasma half-life is longer. In addition to promoting smooth muscle relaxation in the pulmonary vasculature, treprostinil has suppressive effects on platelet aggregation, smooth muscle proliferation and inflammation. A Phase III study, investigating the addition of inhaled treprostinil to oral bosentan or sildenafil, confirmed significant improvements in exercise capacity and quality of life. This review examines the pharmacodynamics, pharmacokinetics, clinical efficacy and safety of inhaled treprostinil for use in pulmonary arterial hypertension.
曲前列尼尔是前列环素衍生物,通过静脉、皮下和吸入途径给药,用于治疗肺动脉高压。与前体依前列醇不同,曲前列尼尔在室温及中性 pH 值时化学性质稳定,其血浆半衰期更长。除了促进肺血管平滑肌松弛外,曲前列尼尔还具有抑制血小板聚集、平滑肌增殖和炎症的作用。一项评估吸入用曲前列尼尔联合口服波生坦或西地那非治疗肺动脉高压的 III 期研究证实,可显著改善运动能力和生活质量。本文就吸入用曲前列尼尔治疗肺动脉高压的药效学、药代动力学、临床疗效和安全性进行了综述。