Abstract：
BACKGROUND: It has been suggested that carbidopa at high blood concentrations may counter the therapeutic effect of levodopa in Parkinson\'s disease by entering the brain and blocking central levodopa conversion to dopamine. We previously demonstrated equivalent plasma levodopa concentration in patients with Parkinson\'s disease during 16 h of (1) intravenous carbidopa/levodopa (DIZ101) infusion, (2) subcutaneous carbidopa/levodopa (DIZ102) infusion or (3) intestinal carbidopa/levodopa gel infusion. Plasma levels of carbidopa were however approximately four times higher with DIZ101 and DIZ102 than with LCIG, and higher than those usually observed with oral levodopa/carbidopa.
OBJECTIVE: To investigate if high carbidopa blood concentrations obtained with parenteral levodopa/carbidopa (ratio 8:1) counter the effect of levodopa on motor symptoms.
METHODS: Eighteen patients with advanced Parkinson\'s disease were administered DIZ101, DIZ102, and intestinal levodopa/carbidopa gel for 16 h on different days in randomized order. Video recordings of a subset of the motor examination in the Unified Parkinson\'s Disease Rating Scale (UPDRS) were evaluated by raters blinded for treatment and time. Motor function was also measured using a wrist-worn device monitoring bradykinesia, dyskinesia, and tremor (Parkinson KinetiGraph).
RESULTS: There was no tendency for poorer levodopa effect with DIZ101 or DIZ102 as compared to LCIG.
CONCLUSIONS: Although DIZ101 or DIZ102 causes approximately four times higher plasma carbidopa levels than LCIG, patients responded equally well to all treatments. The results do not indicate that high plasma carbidopa levels hamper the motor efficacy of levodopa.
OBJECTIVE: To investigate if high carbidopa blood concentrations obtained with parenteral levodopa/carbidopa (ratio 8:1) counter the effect of levodopa on motor symptoms.
METHODS: Eighteen patients with advanced Parkinson\'s disease were administered DIZ101, DIZ102, and intestinal levodopa/carbidopa gel for 16 h on different days in randomized order. Video recordings of a subset of the motor examination in the Unified Parkinson\'s Disease Rating Scale (UPDRS) were evaluated by raters blinded for treatment and time. Motor function was also measured using a wrist-worn device monitoring bradykinesia, dyskinesia, and tremor (Parkinson KinetiGraph).
RESULTS: There was no tendency for poorer levodopa effect with DIZ101 or DIZ102 as compared to LCIG.
CONCLUSIONS: Although DIZ101 or DIZ102 causes approximately four times higher plasma carbidopa levels than LCIG, patients responded equally well to all treatments. The results do not indicate that high plasma carbidopa levels hamper the motor efficacy of levodopa.
摘要：
背景：有人提出，高浓度的卡比多巴可能通过进入大脑并阻断中枢左旋多巴向多巴胺的转化来对抗左旋多巴在帕金森病中的治疗作用。我们以前证明了在（1）静脉卡比多巴/左旋多巴（DIZ101）输注的16小时内，帕金森病患者的血浆左旋多巴浓度相等，（2）皮下卡比多巴/左旋多巴（DIZ102）输注或（3）肠道卡比多巴/左旋多巴凝胶输注。然而，DIZ101和DIZ102的卡比多巴血浆水平比LCIG高大约四倍，并且高于口服左旋多巴/卡比多巴通常观察到的那些。
目的：研究使用非肠道左旋多巴/卡比多巴（比例8：1）获得的高卡比多巴血药浓度是否能抵消左旋多巴对运动症状的影响。
方法：18例晚期帕金森病患者在不同的天数内随机给药DIZ101、DIZ102和肠左旋多巴/卡比多巴凝胶16h。统一帕金森氏病评定量表（UPDRS）中运动检查子集的视频记录由对治疗和时间盲目的评估者进行评估。还使用腕部佩戴的设备监测运动迟缓来测量运动功能，运动障碍,和震颤（帕金森运动图）。
结果：与LCIG相比，DIZ101或DIZ102的左旋多巴效果没有更差的趋势。
结论：尽管DIZ101或DIZ102导致血浆卡比多巴水平比LCIG高大约四倍，患者对所有治疗反应同样良好。结果不表明高血浆卡比多巴水平妨碍左旋多巴的运动功效。
目的：研究使用非肠道左旋多巴/卡比多巴（比例8：1）获得的高卡比多巴血药浓度是否能抵消左旋多巴对运动症状的影响。
方法：18例晚期帕金森病患者在不同的天数内随机给药DIZ101、DIZ102和肠左旋多巴/卡比多巴凝胶16h。统一帕金森氏病评定量表（UPDRS）中运动检查子集的视频记录由对治疗和时间盲目的评估者进行评估。还使用腕部佩戴的设备监测运动迟缓来测量运动功能，运动障碍,和震颤（帕金森运动图）。
结果：与LCIG相比，DIZ101或DIZ102的左旋多巴效果没有更差的趋势。
结论：尽管DIZ101或DIZ102导致血浆卡比多巴水平比LCIG高大约四倍，患者对所有治疗反应同样良好。结果不表明高血浆卡比多巴水平妨碍左旋多巴的运动功效。
