Rabey J M, Nissipeanu P, Inzelberg R, Korczyn A D
Department of Neurology, Ichilov Hospital, Tel-Aviv Sourasky Medical Center, Sackler School of Medicine, Tel-Aviv University, Israel.
Clin Neuropharmacol. 1994 Jun;17(3):286-93. doi: 10.1097/00002826-199406000-00008.
Cabergoline, a new ergoline derivative with potent and long-lasting dopaminergic activity, is a promising drug for overcoming the akinetic episodes in L-Dopa-treated Parkinson's disease patients with motor fluctuations. Its long plasma half-life (65 h) allows a single daily dose administration. Seventeen patients with Parkinson's disease (mean age 66 years; mean disease duration 8.8 years; median Hoehn and Yahr stage, III) were included in an open-label study. All had persistent motor fluctuations while treated with L-Dopa plus carbidopa (mean dose, 660 mg + 66 mg). Cabergoline was added until a maximal dose was achieved (5 mg daily), while L-Dopa was slightly diminished. Eight patients completed 1 year of treatment. They showed significant improvement in their motor performance (Unified Parkinson's Disease Rating Scale) (bradykinesia score decreased from 8.2 to 4.2, p < 0.005), and in the proportion of "off" time spent during waking hours (32-23%, p < 0.05). Three patients abandoned the trial because of increasing severity of dyskinesias, hallucinations, and depression (one each), six were withdrawn because of poor compliance and refusal to continue the treatment. This study suggests that cabergoline may play an important role in the treatment of Parkinson's disease with motor fluctuations.
卡麦角林是一种新型麦角林衍生物，具有强效且持久的多巴胺能活性，是一种有前景的药物，可用于克服左旋多巴治疗的帕金森病患者出现运动波动时的运动不能发作。其血浆半衰期长（65小时），允许每日单次给药。17例帕金森病患者（平均年龄66岁；平均病程8.8年；Hoehn和Yahr分期中位数为III期）纳入一项开放标签研究。所有患者在接受左旋多巴加卡比多巴治疗（平均剂量，660毫克+66毫克）时均有持续的运动波动。添加卡麦角林直至达到最大剂量（每日5毫克），同时略微减少左旋多巴剂量。8例患者完成了1年的治疗。他们的运动表现（统一帕金森病评定量表）有显著改善（运动迟缓评分从8.2降至4.2，p<0.005），以及清醒时间内“关”期所占比例降低（从32%降至23%，p<0.05）。3例患者因异动症、幻觉和抑郁症状加重（各1例）而放弃试验，6例因依从性差和拒绝继续治疗而退出。这项研究表明，卡麦角林在治疗伴有运动波动的帕金森病中可能发挥重要作用。
