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吸入用伊洛前列素:用于原发性肺动脉高压。

Inhaled iloprost: in primary pulmonary hypertension.

作者信息

Goldsmith David R, Wagstaff Antona J

机构信息

Adis International Limited, 41 Centorian Drive, PB 65901, Mairangi Bay, Auckland, New Zealand.

出版信息

Drugs. 2004;64(7):763-73; discussion 774-5. doi: 10.2165/00003495-200464070-00009.

Abstract

Iloprost is a stable prostacyclin analogue with a pharmacokinetic profile allowing nebulised administration in patients with primary pulmonary hypertension (PPH). Inhaled iloprost is a potent acute pulmonary vasodilator with a duration of action of about 60 minutes. It may exert additional long-term benefit through antiproliferative and antithrombotic effects. Inhaled iloprost 2.5 or 5 microg six or nine times daily for 12 weeks (n = 101) significantly (p < 0.01) improved a combined clinical endpoint of a > or =10% increase in distance walked in 6 minutes and an improvement of > or =1 class in New York Heart Association functional class without clinical deterioration or death (16.8 versus 4.9% of placebo recipients, n = 102) in patients with severe PPH or selected forms of nonprimary pulmonary hypertension. Statistical analysis of the response for the PPH subgroup (20.8 versus 5.5% with placebo; n = 51 and 51) was not reported. Improvements from baseline in exercise capacity and haemodynamic/gas exchange variables have been reported in patients with PPH with continued use of inhaled iloprost. In addition, improvement in preinhalation vascular resistance occurred after 12 weeks of inhaled iloprost (p < 0.01 versus placebo) in a large randomised trial. Increased cough, headache, flushing and an influenza-like syndrome were the most common adverse events in the largest trial of patients receiving inhaled iloprost. Headache, flushing and jaw pain occurred significantly more frequently with inhaled iloprost than with placebo.

摘要

依洛前列素是一种稳定的前列环素类似物,其药代动力学特征允许对原发性肺动脉高压(PPH)患者进行雾化给药。吸入依洛前列素是一种强效的急性肺血管扩张剂,作用持续时间约为60分钟。它可能通过抗增殖和抗血栓作用带来额外的长期益处。对于重度PPH或某些非原发性肺动脉高压患者,每天吸入6次或9次2.5或5微克依洛前列素,持续12周(n = 101),显著(p < 0.01)改善了一个综合临床终点,即6分钟步行距离增加≥10%且纽约心脏协会功能分级改善≥1级,同时无临床病情恶化或死亡(16.8%对比安慰剂组的4.9%,n = 102)。未报告对PPH亚组(20.8%对比安慰剂组的5.5%;n = 51和51)反应的统计分析情况。已有报告称,持续使用吸入依洛前列素的PPH患者运动能力以及血流动力学/气体交换变量较基线有所改善。此外,在一项大型随机试验中,吸入依洛前列素12周后,吸入前血管阻力有所改善(与安慰剂相比,p < 0.01)。在接受吸入依洛前列素治疗的患者的最大规模试验中,咳嗽、头痛、面部潮红和流感样综合征是最常见的不良事件。与安慰剂相比,吸入依洛前列素时头痛、面部潮红和颌部疼痛的发生频率显著更高。

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