Pearce R K, Banerji T, Jenner P, Marsden C D
Neurodegenerative Diseases Research Centre, Biomedical Sciences Division, King's College , London, England.
Mov Disord. 1998 Mar;13(2):234-41. doi: 10.1002/mds.870130207.
In contrast to levodopa (L-dopa), de novo administration of the D2-like receptor agonist bromocriptine to patients with Parkinson's disease (PD) or to 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-treated subhuman primates is not associated with the onset of significant dyskinesia. We now compare the ability of the novel D2-like selective dopamine agonist ropinirole with that of bromocriptine and L-dopa to induce dyskinesia in MPTP-treated common marmosets. MPTP-treated common marmosets were treated with placebo, L-dopa plus carbidopa, ropinirole, or bromocriptine daily for 30 days (n = 4 per group) in doses that were titrated to similarly increase locomotion and improve motor disability. L-dopa rapidly induced dyskinesia of moderate to severe intensity, whereas ropinirole and bromocriptine produced mild dyskinesia over the course of the study that was significantly less severe than in the L-dopa-treated group (p < 0.05). However, in a separate group of marmosets previously primed with L-dopa to exhibit dyskinesia, ropinirole administration elicited severe dyskinesias comparable with that of L-dopa in a dose-dependent fashion. Ropinirole, in common with bromocriptine, has a lesser tendency than L-dopa to produce dyskinesia while similarly improving motor performance in drug-naive MPTP-treated marmosets. However, in common with other dopamine agonists, ropinirole will elicit comparable dyskinesia once L-dopa priming has occurred. These results predict a similar response to ropinirole and other long-acting dopamine agonists in L-dopa-naive patients with PD and emphasize the importance of avoiding initial dyskinesia induction through early use of dopamine agonist drugs.
与左旋多巴(L-多巴)不同,对帕金森病(PD)患者或经1-甲基-4-苯基-1,2,3,6-四氢吡啶(MPTP)处理的非人灵长类动物从头给予D2样受体激动剂溴隐亭,不会引发明显的运动障碍。我们现在比较新型D2样选择性多巴胺激动剂罗匹尼罗与溴隐亭和L-多巴在MPTP处理的普通狨猴中诱发运动障碍的能力。对MPTP处理的普通狨猴每日给予安慰剂、L-多巴加卡比多巴、罗匹尼罗或溴隐亭,持续30天(每组n = 4),给药剂量经过调整,以同样增加运动能力并改善运动功能障碍。L-多巴迅速诱发中度至重度运动障碍,而罗匹尼罗和溴隐亭在研究过程中产生轻度运动障碍,其严重程度明显低于L-多巴治疗组(p < 0.05)。然而,在另一组预先用L-多巴引发运动障碍的狨猴中,给予罗匹尼罗会以剂量依赖的方式引发与L-多巴相当的严重运动障碍。与溴隐亭一样,罗匹尼罗在未经药物治疗的MPTP处理的狨猴中产生运动障碍的倾向比L-多巴小,同时能同样改善运动表现。然而,与其他多巴胺激动剂一样,一旦发生L-多巴引发,罗匹尼罗会引发相当的运动障碍。这些结果预测,在未使用过L-多巴的PD患者中,罗匹尼罗和其他长效多巴胺激动剂会有类似反应,并强调了通过早期使用多巴胺激动剂药物避免初始运动障碍诱发的重要性。