Lang A E
Movement Disorders Clinic, Toronto Western Hospital, Ontario, Canada.
Can J Neurol Sci. 1987 Aug;14(3 Suppl):474-82. doi: 10.1017/s031716710003794x.
Since the initiation of bromocriptine therapy for Parkinson's disease several newer dopamine agonists have been developed. Pergolide has reached the stage of Phase 3 clinical trials and will probably be available for general use sometime in the foreseeable future. Lisuride shows most promise in its parenteral form for infusion therapy of patients with severe fluctuations. Mesulergine, another ergot-derivative and ciladopa, a new non-ergot agonist, have been withdrawn from further clinical use due to tumorogenesis in rats. It is questionable how applicable these findings are to the use of the drugs in elderly humans with parkinsonism. Recently a small number of drugs have been found to have postsynaptic dopamine agonist properties only in the setting of denervated supersensitive dopamine receptors. These agents may be particularly effective in the early treatment of patients with Parkinson's disease. This paper will review a number of the dopamine agonists which have been developed since the introduction of bromocriptine therapy. Several of these have shown beneficial effects in early clinical trials while others show promise in preclinical studies of animal models of parkinsonism.
自从开始使用溴隐亭治疗帕金森病以来，已经开发出了几种更新的多巴胺激动剂。培高利特已进入3期临床试验阶段，可能在可预见的将来某个时候可供普遍使用。利苏力特以非肠道给药形式用于严重症状波动患者的输注治疗显示出最大的前景。麦角乙脲（另一种麦角衍生物）和西拉美多（一种新的非麦角激动剂）由于在大鼠中诱发肿瘤而停止进一步临床使用。这些发现对患有帕金森病的老年人使用这些药物的适用性如何，尚存在疑问。最近发现少数药物仅在去神经超敏多巴胺受体的情况下具有突触后多巴胺激动剂特性。这些药物在帕金森病患者的早期治疗中可能特别有效。本文将综述自溴隐亭治疗引入以来开发的多种多巴胺激动剂。其中一些在早期临床试验中已显示出有益效果，而其他一些在帕金森病动物模型的临床前研究中显示出前景。
