Waters Cheryl H, Sethi Kapil D, Hauser Robert A, Molho Eric, Bertoni John M
Department of Neurology, Columbia University, New York, New York 10032, USA.
Mov Disord. 2004 Apr;19(4):426-32. doi: 10.1002/mds.20036.
Zydis selegiline dissolves on contact with saliva and undergoes pregastric absorption. This minimizes first-pass metabolism and provides high plasma concentrations of selegiline. In this study, the efficacy and safety of Zydis selegiline was assessed in Parkinson's disease (PD) patients who were experiencing motor fluctuations with levodopa. Patients were randomly assigned to either drug or placebo in a 2:1 ratio in this double-blind, multicenter trial. Significant reductions in daily off time occurred at 4 to 6 weeks with the 1.25 mg dose (9.9%, P = 0.003) and 10 to 12 weeks with the 2.5 mg dose (13.2%, P < 0.001). The total number of off hours was reduced by 2.2 hours at Week 12 from baseline (compared with 0.6 hours in the placebo group). The average number of dyskinesia-free on hours for the Zydis selegiline patients increased by 1.8 hours at Week 12. There was no change in mean percentage of "Asleep" time throughout the study. No apparent differences were detected in the occurrence of drug-related adverse events between the Zydis selegiline group and placebo-treated groups. Adverse events were consistent with known effects of levodopa therapy. Zydis selegiline safely reduces daily off time when used as adjunctive therapy with levodopa in patients with PD.
速释型司来吉兰与唾液接触后即溶解，并进行胃前吸收。这将首过代谢降至最低，并使司来吉兰在血浆中达到高浓度。在本研究中，对正在接受左旋多巴治疗且出现运动波动的帕金森病（PD）患者评估了速释型司来吉兰的疗效和安全性。在这项双盲、多中心试验中，患者按2:1的比例随机分配至药物组或安慰剂组。1.25毫克剂量组在4至6周时每日“关”期时间显著减少（9.9%，P = 0.003），2.5毫克剂量组在10至12周时显著减少（13.2%，P < 0.001）。在第12周时，与基线相比，药物组的每日“关”期总时长减少了2.2小时（安慰剂组减少了0.6小时）。速释型司来吉兰治疗的患者在第12周时无异动症的“开”期平均时长增加了1.8小时。在整个研究过程中，“睡眠”时间的平均百分比没有变化。速释型司来吉兰组与安慰剂治疗组之间在药物相关不良事件的发生上未发现明显差异。不良事件与左旋多巴治疗的已知效应相符。速释型司来吉兰与左旋多巴联合用于PD患者时，可安全地减少每日“关”期时间。
