Jellinger K
J Neurol. 1982;227(2):75-88. doi: 10.1007/BF00313773.
Bromocriptine (CB-154) and the 8-alpha-ergoline CU 32-085, two dopamine receptor agonists, were administered at different times to two series of 22 patients with Parkinson's disease, most of whom took levodopa (plus benserazide) at optimum dosage. The addition of bromocriptine (mean daily dose 32 mg; after 6 months 40 mg) led to a 38.5% reduction of levodopa, while CU 32-085 (mean daily dose 15.2 mg; after 6 months 17.5 mg) permitted a 33.7% reduction in levodopa. The mean dose in two patients on CU 32-085 monotherapy was 55 mg/day. A total of 15 patients tolerated adequate doses of bromocriptine (5-75 mg/day, mean duration of treatment 7.5 months) and 15 patients long-term treatment up to 14 months with CU 32-085 (dose range 1-60 mg/day; mean duration 8.8 months). Both groups showed a significant improvement of "total disability score' at 6 months by 56% and 67%, respectively, and after 6 months by 69% and 69.4%, respectively, with a significant decrease of all types of disability. All patients with fluctuations and "on-off' effects rapidly improved on both compounds. Bromocriptine and CU 32-085 were discontinued in seven patients each (32%) because of adverse effect including mental changes (for with bromocriptine, two with CU 32-085), nausea and vomiting (one and two, respectively), hypotension (one each) and increased tremor plus vomiting (one with CU 32-085). Although adverse effects were similar to those observed with levodopa, CU 32-085 in general showed less severe dyskinesia and mental changes but more frequent nausea than bromocriptine and levodopa. While the results of treatment with bromocriptine and CU 32-085 were comparable, the antitremor effect of the latter drug developed more rapidly, even at low dosage. Both compounds were useful in the management of patients with advanced Parkinson's disease, CU 32-085 having a stronger effect on tremor, bradykinesia, fluctuations and "on-off' effects than bromocriptine.
将两种多巴胺受体激动剂溴隐亭（CB - 154）和8-α-麦角灵CU 32 - 085，在不同时间给予两组各22例帕金森病患者，其中大多数患者正服用最佳剂量的左旋多巴（加苄丝肼）。加用溴隐亭（平均日剂量32毫克；6个月后为40毫克）使左旋多巴用量减少38.5%，而CU 32 - 085（平均日剂量15.2毫克；6个月后为17.5毫克）使左旋多巴用量减少33.7%。两名仅接受CU 32 - 085单一疗法的患者平均剂量为55毫克/天。共有15例患者耐受了足够剂量的溴隐亭（5 - 75毫克/天，平均治疗时长7.5个月），15例患者接受了长达14个月的CU 32 - 085长期治疗（剂量范围1 - 60毫克/天；平均时长8.8个月）。两组患者在6个月时“总残疾评分”分别显著改善56%和67%，6个月后分别改善69%和69.4%，各类残疾均显著减轻。所有有症状波动和“开 - 关”效应的患者使用这两种药物后均迅速改善。溴隐亭和CU 32 - 085各有7例患者（32%）因不良反应停药，不良反应包括精神改变（溴隐亭组4例，CU 32 - 085组2例）、恶心和呕吐（分别为1例和2例）、低血压（各1例）以及震颤加重伴呕吐（CU 32 - 085组1例）。虽然不良反应与左旋多巴所见相似，但总体而言，CU 32 - 085的运动障碍和精神改变较轻，但恶心比溴隐亭和左旋多巴更常见。虽然溴隐亭和CU 32 - 085的治疗结果相当，但后者即使在低剂量时抗震颤作用起效也更快。两种化合物对晚期帕金森病患者的治疗均有效，CU 32 - 085在震颤、运动迟缓、症状波动和“开 - 关”效应方面比溴隐亭作用更强。
