Deleu D, Jacques M, Michotte Y, Ebinger G
Department of Neurology, University Hospital, Brussels, Belgium.
Neurology. 1989 Nov;39(11 Suppl 2):88-92; discussion 95.
The efficacy of an oral controlled-release preparation of carbidopa/levodopa (Sinemet CR 50/200 mg) was compared with conventional carbidopa/levodopa (25/250 mg) in an open-label study. Twenty patients with idiopathic Parkinson's disease and severe response fluctuations participated. At the end of 6 months of CR treatment, the major clinical benefits included improvement of disability, reduction in number of "off" periods (predominantly end-of-dose hypokinesia), and increase in percentage of "on" time. Although dosages of CR required for an optimal therapeutic response were not significantly higher compared with conventional levodopa, bioavailability significantly increased. Delayed onset of antiparkinsonian effect of CR, resulting from an increase of Tmax for levodopa, was one of the major patient complaints and required additional small amounts of standard levodopa in some patients.
在一项开放标签研究中，对卡比多巴/左旋多巴口服控释制剂（息宁控释片50/200毫克）与传统卡比多巴/左旋多巴（25/250毫克）的疗效进行了比较。20例患有特发性帕金森病且有严重反应波动的患者参与了研究。在控释制剂治疗6个月结束时，主要的临床益处包括残疾状况改善、“关”期（主要是剂量末期运动徐缓）次数减少以及“开”期百分比增加。尽管与传统左旋多巴相比，达到最佳治疗反应所需的控释制剂剂量并无显著更高，但生物利用度显著提高。控释制剂抗帕金森病作用起效延迟，这是由于左旋多巴的达峰时间增加所致，这是患者的主要抱怨之一，一些患者需要额外服用少量标准左旋多巴。
