Rho激酶抑制剂法舒地尔在肺动脉高压治疗中的应用

摘要/Abstract

摘要： 肺动脉高压（pulmonary arterial hypertension，PAH）是一类以肺动脉渐进性闭塞导致肺血管阻力逐渐升高继而诱发右心室衰竭的恶性肺血管疾病，病因复杂，致死率高，病理机制尚未明确。目前临床上PAH治疗药物有限，治疗效果差，不良反应多。据最新研究发现新型靶向药物如血管活性肽、氨基酸激酶抑制剂、免疫抑制剂等对PAH的病情进展有一定抑制作用，其中Rho/Rho激酶信号通路的激活与PAH的发病机制密切相关。Rho激酶可能与内皮细胞功能障碍有关，引起血管收缩、重塑，致使PAH患者的肺动脉平滑肌细胞中Rho激酶活性增加。Rho激酶抑制剂目前已经作为靶向药物治疗PAH，其疗效及前景备受瞩目。法舒地尔是目前唯一用于临床的Rho激酶抑制剂，可改善平均肺动脉压力、BNP水平和肺血管重构，进而改善患者的生存。本研究拟就法舒地尔在PAH治疗中的药理特点和应用进展做一综述，以期为今后PAH治疗药物的研究和临床应用提供借鉴和参考。

关键词: font-size:medium, ">法舒地尔；Rho激酶抑制剂；肺动脉高压；药理特点；应用进展

Abstract: Pulmonary arterial hypertension(PAH) is a kind of malignant pulmonary vascular disease that causes pulmonary vascular resistance to increase gradually and then induces right ventricular failure due to progressive pulmonary artery occlusion， which is complex cause and high mortality. At present there is no single unifying theory to explain the pathogenesis of PAH. The effectiveness and safety of treatments for PAH are unsatisfactory. Emerging researches highlight novel-targeted drugs such as vasoactine intrestinal peptide， protein kinase inhibitor， immune inhibitor and so on. The Rho/Rho-kinase pathway has been shown to be involved in the pathogenesis of PAH. Rho-kinase is activated in PAH patients associated with enhanced pulmonary vasoconstricting and proliferating responses， impaired endothelial vasodilator functions， and pulmonary remodeling. Rho-kinase inhibitor has been emerged as an essential target therapeutic strategy for PAH with a bright future. Fasudil， as the only Rho-kinase inhibitor in clinic now， is effective in improving pulmonary arterial pressure， BNP level， vascular remodeling and improvement in survival. In this paper， the pharmacological characteristics of fasudil and its application at home and abroad were reviewed in order to provide reference for the development of PAH-targeted drug research and its clinical application.

Key words: font-size:medium, ">Fasudil； Rho-kinase inhibitor； Pulmonary arterial hypertension； Pharmacological characteristics； Application progress

中图分类号:

马晓辉, 张志国. Rho激酶抑制剂法舒地尔在肺动脉高压治疗中的应用[J]. 中国医药导刊, 2021, 23(7): 510-513.

MA Xiaohui, ZHANG Zhiguo. Effects of Rho-kinase Inhibitor Fasudil on Pulmonary Arterial Hypertension[J]. CHINESE JOURNAL OF MEDICINAL GUIDE, 2021, 23(7): 510-513.

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