Cedarbaum J M, Silvestri M, Clark M, Harts A, Kutt H
Department of Neurology, Cornell University Medical College, Burke Rehabilitation Center, White Plains, New York 10605.
Clin Neuropharmacol. 1990 Feb;13(1):29-35. doi: 10.1097/00002826-199002000-00003.
Six patients with Parkinson's disease (PD) and therapeutic response fluctuations (RF) on levodopa treatment participated in an open-label trial of L-deprenyl (Eldepryl) in conjunction with Sinemet. Deprenyl (10 mg/day) allowed a slight but not statistically significant 22% reduction of total daily levodopa intake after 4 weeks of treatment, with a significant but unsustained reduction in the number of daily "off" periods and an increase in the portion of waking day spent "on." Pharmacokinetic studies revealed no effect of deprenyl on the plasma levodopa concentration vs. time curve, or the coefficient of variation (C.V.) of plasma levodopa levels measured over an 8-h period. Plasma DOPAC levels were unaffected, suggesting that the majority of peripheral DOPAC is generated by action of MAO-A. For most patients, benefit was not maintained. Two patients have continued taking the drug, and both have enjoyed significant reductions in total levodopa dose. Both have mild end-of-dose failure and little dyskinesia. Since no changes in peripheral pharmacokinetics of levodopa could be demonstrated, any therapeutic action of deprenyl in PD would appear to be due to prolongation of dopaminergic activity within the CNS.
6名患有帕金森病（PD）且左旋多巴治疗存在疗效波动（RF）的患者参与了一项关于L-司来吉兰（ Eldepryl）联合息宁的开放标签试验。司来吉兰（10毫克/天）在治疗4周后使每日左旋多巴总摄入量略有减少，但无统计学意义，减少了22%，每日“关”期数量显著减少但未持续，且“开”期在清醒日中所占比例增加。药代动力学研究表明，司来吉兰对血浆左旋多巴浓度-时间曲线或8小时内测得的血浆左旋多巴水平的变异系数（C.V.）没有影响。血浆3,4-二羟基苯乙酸（DOPAC）水平未受影响，提示外周DOPAC大部分是由单胺氧化酶A（MAO-A）作用产生的。对大多数患者而言，疗效未得到维持。2名患者持续服用该药，且二者的左旋多巴总剂量均显著减少。二者均有轻度剂末失效且几乎没有异动症。由于未证实左旋多巴外周药代动力学有变化，司来吉兰在帕金森病中的任何治疗作用似乎都归因于中枢神经系统内多巴胺能活性的延长。
