Hutton J T, Albrecht J W, Román G C, Kopetzky M T
Department of Medical and Surgical Neurology, Texas Tech University Health Sciences Center, Lubbock 79430.
Arch Neurol. 1988 Jan;45(1):55-7. doi: 10.1001/archneur.1988.00520250061022.
Twenty parkinsonian patients (Hoehn and Yahr scale, I through III) were treated with controlled-release carbidopa-levodopa (CR-2 or CR-3) and standard carbidopa-levodopa (Sinemet, 25 mg/100 mg) in a double-blind, crossover pharmacokinetic and clinical efficacy study. The controlled-release agents had a slower rise to peak plasma values and flatter pharmacokinetic curves than did the standard. The area under the curve for CR-3 was significantly increased by 55.5% as compared with standard agent and by 84.2% as compared with CR-2. No differences in clinical efficacy were found between controlled-release agents and the standard agent for this group of parkinsonian patients with mild to moderate severity. The dissociation between the prolonged serum levodopa levels and unimproved clinical efficacy may have resulted from the absence of patients with prominent motor fluctuations and/or substantial serum levodopa variability that was especially prominent with CR-3.
在一项双盲、交叉的药代动力学和临床疗效研究中，20名帕金森病患者（霍恩和亚尔分级，I至III级）接受了控释卡比多巴-左旋多巴（CR-2或CR-3）和标准卡比多巴-左旋多巴（息宁，25毫克/100毫克）治疗。与标准制剂相比，控释制剂达到血浆峰值的速度较慢，药代动力学曲线较平缓。与标准制剂相比，CR-3的曲线下面积显著增加了55.5%，与CR-2相比增加了84.2%。对于这组轻度至中度严重程度的帕金森病患者，控释制剂与标准制剂之间未发现临床疗效差异。血清左旋多巴水平延长与临床疗效未改善之间的分离可能是由于缺乏有明显运动波动的患者和/或血清左旋多巴变异性大的患者，而这在CR-3中尤为突出。
