Dupont E, Mikkelsen B, Jakobsen J
J Neurol Neurosurg Psychiatry. 1986 Apr;49(4):390-5. doi: 10.1136/jnnp.49.4.390.
The efficacy and tolerance of treatment with an 8-alpha-amino-ergoline derivative CU32-o85, Mesulergine, were compared with levodopa/benserazide (Madopar) in a 3 month double-blind controlled trial in 31 patients with Parkinson's disease, not previously treated with levodopa. The two treatments were equally well tolerated, and neither dyskinesias nor dose-related fluctuations developed. In 90% of the patients treated with Mesulergine, Parkinsonian symptoms improved, and at the dose given the overall therapeutical response was two-thirds that of levodopa. During further 9 months of open study the beneficial effect was maintained equally well in both groups. Compared with other dopamine agonists Mesulergine has a considerable antiparkinsonian effect. Unfortunately, further clinical evaluation of the compound recently has been stopped owing to sex and species specific histological alterations in rats. It is suggested that Mesulergine derivatives might well be of value in future treatment of early Parkinson's disease and of late incompensated stages.
在一项为期3个月的双盲对照试验中,对31例未经左旋多巴治疗的帕金森病患者,比较了8-α-氨基麦角灵衍生物CU32-o85(美舒麦角)与左旋多巴/苄丝肼(美多芭)的治疗效果和耐受性。两种治疗的耐受性相当,均未出现运动障碍或与剂量相关的波动。在接受美舒麦角治疗的患者中,90%的帕金森症状得到改善,在给定剂量下,总体治疗反应为左旋多巴的三分之二。在随后9个月的开放研究中,两组的有益效果均得到同样良好的维持。与其他多巴胺激动剂相比,美舒麦角具有相当大的抗帕金森病作用。不幸的是,由于大鼠出现性别和物种特异性组织学改变,该化合物最近已停止进一步的临床评估。有人认为,美舒麦角衍生物在未来早期帕金森病和晚期失代偿阶段的治疗中可能很有价值。