Papavasilliou P S, Cotzias G C, McDowell F H, Rosal V L, Sheehan P J
Clin Pharmacol Ther. 1978 Feb;23(2):195-8. doi: 10.1002/cpt1978232195.
The neuroendocrine properties and the beneficial effects of cyproheptadine in tardive dyskinesia led to the testing of this drug in levodopa-induced dyskinesia. Cyproheptadine administered to 6 parkinsonian patients in doses of up to 42 mg/day was of no significant benefit in either dyskinesia or symptom control. Improvement in appetite was reported by 3 patients. These observations suggested that different mechanisms may be responsible in the pathogenesis of phenothiazine and amine-induced dyskinesia. The failure to control levodopa-induced dyskinesia selectively with serotonin agonists and antagonists and the accentuation of the dyskinesia in the presence of anticholinergic agents further suggest that substances that increase directly central cholinergic activity may be effective in the control of levodopa-induced dyskinesia.
赛庚啶的神经内分泌特性及其在迟发性运动障碍中的有益作用促使人们对该药物在左旋多巴诱发的运动障碍中进行试验。对6例帕金森病患者给予剂量高达42毫克/天的赛庚啶,在控制运动障碍或症状方面均无显著益处。3例患者报告食欲有所改善。这些观察结果表明,吩噻嗪和胺诱发的运动障碍的发病机制可能涉及不同的机制。使用5-羟色胺激动剂和拮抗剂无法选择性地控制左旋多巴诱发的运动障碍,以及在抗胆碱能药物存在的情况下运动障碍加剧,这进一步表明直接增加中枢胆碱能活性的物质可能对控制左旋多巴诱发的运动障碍有效。