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多巴胺(DA)受体激动剂能够控制帕金森病(PD)症状和延缓PD进程,并具有神经保护作用,在临床上广泛用于治疗PD和不安腿综合征。近年来发现,麦角碱类DA受体激动剂在临床应用过程中存在严重的安全问题,最主要的危害是造成心瓣膜损害而导致其反流增加。本文对培高利特、卡麦角林、溴隐亭和麦角乙脲4种麦角碱类DA受体激动剂与药源性心瓣膜病之间的关系予以探讨。卡麦角林和大剂量(>1.5mg·d-1)的培高利特可以显著增加心瓣膜病发生的风险性,小剂量的(<1.5mg·d-1)培高利特、溴隐亭和麦角乙脲引起心瓣膜病的风险性相对较低。麦角碱类DA受体激动剂引起心瓣膜病的可能分子机制是通过异常激动5-HT2B受体,刺激成纤维细胞增殖,从而使心瓣膜及其附属结构纤维化,导致关闭不全。
Dopamine (DA) receptor agonists are capable of controlling the symptoms of Parkinson’s disease (PD) and delaying PD progression and have neuroprotection and are widely used clinically to treat PD and restless legs syndrome. In recent years, it has been found that ergot alkaloid DA receptor agonists have serious safety problems in clinical application. The most important hazard is the damage caused by the heart valve, resulting in the increase of reflux. This article discusses the relationship between the four ergot-based DA receptor agonists such as pergolide, cabergoline, bromocriptine and lisuride and drug-induced valvular disease. Cabergoline and high dose (> 1.5 mg · d-1) of pergolide significantly increased the risk of valvular heart disease. Low dose (<1.5 mg · d-1) of pergolide, bromocriptine and The risk of valvular heart disease caused by lisuride is relatively low. The possible molecular mechanism of ergot-based DA receptor agonist in valvular heart disease is through abnormal activation of 5-HT2B receptor to stimulate the proliferation of fibroblasts, thereby causing fibrosis of the heart valve and its accessory structures, resulting in incomplete closure.