Zangaglia Roberta, Stocchi Fabrizio, Sciarretta Massimo, Antonini Angelo, Mancini Francesca, Guidi Marco, Martignoni Emilia, Pacchetti Claudio
Parkinson's Disease and Movement Disorders Unit, IRCCS Neurological Institute C. Mondino, Pavia, Italy.
Clin Neuropharmacol. 2010 Mar-Apr;33(2):61-6. doi: 10.1097/WNF.0b013e3181c5e60c.
Slow gastric emptying decreasing levodopa (LD) bioavailability contributes to motor fluctuations in Parkinson disease (PD). Melevodopa (LD methylester), ensuring rapid duodenal absorption, has been proposed as rescue therapy for afternoon off periods.
To assess daily motor fluctuations by multiple administrations of Sirio (Chiesi Farmaceutici SpA, Parma, Italy) (melevodopa/carbidopa) in PD patients.
In this open-label naturalistic study, 75 PD patients (group A) completely switched standard LD (Sinemet or Madopar) with Sirio at an equivalent dosage (800-1000 mg/d). One hundred nineteen PD patients (group B) partially replaced their standard LD (Sinemet) with Sirio at an equivalent dosage (400-500 mg/d) while continuing Stalevo 100. In both groups, the observational period lasted 6 months. Assessments included an on/off diary, the Unified Parkinson's Disease Rating Scale (motor examination [UPDRS II] and activities of daily living [UPDRS III]), the dyskinesia scale, and an adverse event profile.
Group A showed a significant reduction of afternoon off hours at 6 months (P < 0.05). Forty-five patients (69%) reported a subjective early onset of on motor response. Twelve patients (18.5%) reported its shorter duration. The dyskinesia scale score remained unchanged. Ten patients (13.3%) discontinued melevodopa for gastric intolerance. Group B showed at 6 months a significant reduction of total hours of daily off periods (P < 0.05), particularly in the morning (P < 0.01) and afternoon (P < 0.05). Seventy subjects (59%) expressed positive judgment on quickness of onset of on motor response. The dyskinesia scale score was unchanged. No significant adverse events were reported.
Switching PD patients with motor fluctuations to melevodopa, particularly in the presence of entacapone, could optimize critical periods of the day such as the morning delay on and afternoon off periods.
胃排空缓慢导致左旋多巴（LD）生物利用度降低，这是帕金森病（PD）运动波动的原因之一。甲磺酸左旋多巴（左旋多巴甲酯）可确保十二指肠快速吸收，已被提议作为午后“关期”的急救疗法。
通过多次给予Sirio（意大利帕尔马的Chiesi Farmaceutici SpA公司生产）（甲磺酸左旋多巴/卡比多巴）来评估帕金森病患者的日常运动波动情况。
在这项开放标签的自然主义研究中，75例帕金森病患者（A组）以等效剂量（800 - 1000毫克/天）完全用Sirio替代标准左旋多巴（息宁或美多芭）。119例帕金森病患者（B组）以等效剂量（400 - 500毫克/天）用Sirio部分替代其标准左旋多巴（息宁），同时继续服用Stalevo 100。两组的观察期均为6个月。评估内容包括“开/关”日记、统一帕金森病评定量表（运动检查[UPDRS II]和日常生活活动[UPDRS III]）、异动症量表以及不良事件记录。
A组在6个月时午后“关期”小时数显著减少（P < 0.05）。45例患者（69%）报告主观上“开”运动反应提前出现。12例患者（18.5%）报告其持续时间缩短。异动症量表评分保持不变。10例患者（13.3%）因胃部不耐受停用甲磺酸左旋多巴。B组在6个月时每日“关期”总小时数显著减少（P < 0.05），尤其是在早晨（P < 0.01）和午后（P < 0.05）。70名受试者（59%）对“开”运动反应的起效速度给予积极评价。异动症量表评分未变。未报告显著不良事件。
将有运动波动的帕金森病患者换用甲磺酸左旋多巴，尤其是在同时使用恩他卡朋的情况下，可优化一天中的关键时段，如早晨延迟“开期”和午后“关期”。
