Beraprost:回顾其药理学和治疗效果治疗外周动脉疾病和肺动脉高血压。

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米洛斯岛人EB,果阿吉隆坡

Beraprost:回顾其药理学和治疗效果治疗外周动脉疾病和肺动脉高血压。

药。2002;62(1):107 - 33所示。

PubMed ID
11790158 (在PubMed
]
文摘

Beraprost钠(Beraprost)是一个稳定、口服环前列腺素类似物与血管扩张性,抗血小板和cytoprotective效果。Beraprost行为抑制内皮细胞膜受体最终释放钙离子从细胞内存储的网站。这种减少Ca2 +的涌入已经假定导致放松平滑肌细胞和血管舒张。数据从一个大,随机,双盲,多中心研究表明,beraprost ticlopidine一样有效治疗外周动脉疾病患者(血栓闭塞性脉管炎和动脉硬化闭塞性脉管炎)。大多数病人接受beraprost表现出减少溃疡大小,改进报道肉芽组织和显示的外观改善疼痛静止和四肢冰冷的感觉。在一个大的关键临床试验患者间歇性跛行,beraprost治疗与显著增加有关无痛行走和绝对距离与接受安慰剂的病人。在统计上有显著差异的重要的心血管事件的发生率在两个治疗组接受beraprost没有观察到但患者更有可能改变他们的生活质量感到满意。然而,尽管初步未发表的数据从一个大,第三阶段,安慰剂对照研究在美国提出了一个更少的关键趋势心血管事件(没有提出具体的数据),这项研究并没有证实欧洲三期临床试验的阳性结果统计学意义并没有取得相关研究的端点运动。一系列小型noncomparative临床试验患者的肺动脉高血压(多环芳烃)的罕见状况表明,大幅降低肺动脉压力和阻力,增加心输出量,并增加相关的运动能力似乎beraprost治疗;然而,这些数据是非常有限的,在大多数情况下都没有完全公布。 Beraprost is a well tolerated agent. Overall, the main adverse events include headache, hot flushes, diarrhoea and nausea. However, patients with PAH showed higher incidence of adverse events than those with peripheral arterial disease. CONCLUSION: Beraprost, an orally administered PGI2 analogue, is generally well tolerated and appears to be an effective agent in the treatment of patients with Buerger's disease and arteriosclerosis obliterans. Comparative data from a large randomised trial indicated that the drug appears as effective as ticlopidine in patients with these conditions. In patients with intermittent claudication, significant benefits of beraprost compared with placebo were reported in a randomised clinical trial; however, the use of beraprost in these patients is not supported by recent preliminary unpublished data from a large, phase III, placebo-controlled study. Limited data suggest some efficacy with long-term beraprost treatment of patients with PAH, where options are few and where oral administration of the drug could be a considerable advantage over intravenous prostacyclin (PGI2) therapy. Additional well-designed and, where possible, large trials with active comparators are necessary to define more precisely the place of beraprost in the treatment of patients with PAH, Buerger's disease and arteriosclerosis obliterans.

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药物
药物靶点
药物 目标 生物 药理作用 行动
Beraprost 环前列腺素受体 蛋白质 人类
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