Varga L I, Ako-Agugua N, Colasante J, Hertweck L, Houser T, Smith J, Watty A A, Nagar S, Raffa R B
Department of Pharmaceutical Sciences, Temple University School of Pharmacy, Philadelphia, PA, USA.
J Clin Pharm Ther. 2009 Oct;34(5):493-505. doi: 10.1111/j.1365-2710.2009.01025.x.
Ropinirole hydrochloride (REQUIP, ADARTREL) and pramipexole dihydrochloride (MIRAPEX, SIFROL) are two putative dopamine D(3) receptor subtype-selective agonists recently approved by the FDA for the treatment of 'restless legs syndrome' (RLS). RLS is a difficult to define condition that is possibly more prevalent than previously thought. Direct-to-consumer advertising has raised public and professional awareness of RLS, but questions, even skepticism about the very existence of the condition, persist. The drugs have adverse effects that can negatively impact on quality of life and thus, as true for all drugs, require consideration of the benefit : risk ratio. We review the definition, diagnostic criteria, pathophysiology, and treatment of RLS, and assess the clinical and preclinical evidence for a pharmacologic rationale for D(3) agonism in general and of the claimed D(3) selectivity of ropinirole and pramipexole in particular.
盐酸罗匹尼罗（商品名 REQUIP、ADARTREL）和盐酸普拉克索（商品名 MIRAPEX、SIFROL）是两种被认为对多巴胺 D(3) 受体亚型具有选择性的激动剂，最近已获美国食品药品监督管理局（FDA）批准用于治疗“不宁腿综合征”（RLS）。RLS 是一种难以定义的病症，其实际患病率可能比之前认为的更高。直接面向消费者的广告提高了公众和专业人士对 RLS 的认识，但对于该病症是否真的存在，质疑甚至怀疑仍然存在。这些药物具有可能对生活质量产生负面影响的不良反应，因此，与所有药物一样，需要考虑其效益风险比。我们回顾了 RLS 的定义、诊断标准、病理生理学和治疗方法，并评估了支持 D(3) 激动剂总体药理学原理以及特别是罗匹尼罗和普拉克索所宣称的 D(3) 选择性的临床和临床前证据。
