Lieberman A, Gopinathan G, Neophytides A, Pasternack P, Goldstein M
Neurology. 1987 May;37(5):863-5. doi: 10.1212/wnl.37.5.863.
Ciladopa is a partial dopamine agonist that is effective in patients with advanced Parkinson's disease who are no longer satisfactorily responding to levodopa. Thirty-one patients participated in a double-blind randomized study of ciladopa (added to levodopa) versus placebo. Among 21 patients randomized to treatment with ciladopa and levodopa, there was a 32% decrease in symptoms on the Modified Columbia University Disability Scale. This change was significant, p less than or equal to 0.05. Eight of the 21 patients (38%) improved by at least 50%. The mean number of hours "on" increased by 20%. This change was significant, p less than or equal to 0.05. Five of the 21 patients (24%) were on for at least 4 hours more than at baseline. Dyskinesias were not increased. The mean dose of ciladopa was 19.5 mg/d. The mean dose of levodopa in Sinemet was decreased by 10%. Studies with ciladopa in humans had to be discontinued because of the occurrence of microscopic testicular tumors in some rodents. Although improvement in patients taking ciladopa was modest, there were few adverse effects. These results are encouraging, because two other partial agonists are now available, and they may be as effective as ciladopa.
西拉多巴是一种部分多巴胺激动剂,对那些对左旋多巴反应不再令人满意的晚期帕金森病患者有效。31名患者参与了一项西拉多巴(加用至左旋多巴)与安慰剂对比的双盲随机研究。在随机接受西拉多巴和左旋多巴治疗的21名患者中,改良哥伦比亚大学残疾量表上的症状减少了32%。这一变化具有显著性,p≤0.05。21名患者中有8名(38%)改善至少达50%。“开”的平均时长增加了20%。这一变化具有显著性,p≤0.05。21名患者中有5名(24%)“开”的时间比基线至少多4小时。异动症未增加。西拉多巴的平均剂量为19.5毫克/天。息宁中左旋多巴的平均剂量减少了10%。由于一些啮齿动物出现了微小睾丸肿瘤,关于西拉多巴在人体的研究不得不停止。尽管服用西拉多巴的患者改善程度不大,但不良反应较少。这些结果令人鼓舞,因为现在有另外两种部分激动剂,它们可能与西拉多巴一样有效。