Director of Parkinson Institute, Istituti Clinici di Perfezionamento, Via Bignami 1, Milan, Italy.
Expert Opin Pharmacother. 2010 Mar;11(4):627-35. doi: 10.1517/14656561003598919.
Levodopa is the mainstay of symptomatic treatment for Parkinson's disease (PD). Although other treatments have been developed in the last 30 years, most patients use levodopa in view of its superior efficacy in controlling PD symptoms. Unfortunately, levodopa is associated with long-term motor complications (motor fluctuations and dyskinesias). The main causes of these undesirable effects are the narrowing of the therapeutic window with the natural progression of the disease, pulsatile dopaminergic stimulation due to the short half-life of the drug and erratic absorption. Several studies suggest that PD control could be enhanced by changing the mode of levodopa delivery so as to ensure continuous and stable supply of the drug to the brain. The objective of this text is to review the ascertained strengths and limitations of levodopa in PD, starting from its history, and propose novel modes of usage designed to cover currently unmet medical needs.
Medline literature search (from 1973 to date).
A perspective on the evolution of PD pharmacological treatment.
Levodopa still is the best treatment for PD. Truly stable and controlled formulations that ensure clinical response should be developed to reduce the undesirable effects that restrict its efficacy.
左旋多巴是治疗帕金森病(PD)的主要药物。尽管在过去的 30 年中已经开发出了其他治疗方法,但由于其在控制 PD 症状方面的卓越疗效,大多数患者仍使用左旋多巴。不幸的是,左旋多巴与长期运动并发症(运动波动和运动障碍)有关。这些不良影响的主要原因是随着疾病的自然进展,治疗窗变窄,由于药物半衰期短和吸收不规则,导致多巴胺能刺激呈脉冲式。几项研究表明,通过改变左旋多巴的给药方式,可以增强 PD 的控制,从而确保药物持续稳定地供应到大脑。本文的目的是从历史的角度回顾左旋多巴在 PD 中的已确定的优势和局限性,并提出旨在满足当前未满足的医疗需求的新的使用方式。
Medline 文献检索(从 1973 年至今)。
对 PD 药物治疗演变的认识。
左旋多巴仍然是治疗 PD 的最佳药物。应该开发真正稳定和可控的制剂,以确保临床反应,从而减少限制其疗效的不良影响。