Müller T, Erdmann C, Muhlack S, Bremen D, Przuntek H, Goetze O, Woitalla D
Department of Neurology, St. Josef Hospital, Ruhr University Bochum, Bochum, Germany.
J Neural Transm (Vienna). 2006 Oct;113(10):1441-8. doi: 10.1007/s00702-006-0442-5. Epub 2006 Apr 11.
Addition of the catechol-O-methyltransferase (COMT) inhibitor entacapone (EN) prolongs plasma metabolism of levodopa (LD). Objectives were to determine the clinical response after EN addition and the plasma degradation of LD and 3-O-methyldopa [3-OMD]. Not optimum treated hospitalised patients with Parkinson's disease received the same LD dosage on the first day only with carbidopa (CD) and on the second day with CD and EN (t.i.d.) within a standardised setting. We scored motor symptoms and measured LD- and 3-OMD levels on both days at fixed moments. Motor impairment significant better improved probably due to significant higher maximum concentrations [C(max)] and computed area under the curve values of LD levels during the LD/CD/EN condition. Time to C(max) of LD was significantly delayed after the first two LD/CD/EN intakes. An impact of EN on 3-OMD levels appeared. A possibly augmented LD absorption and a prolonged LD metabolism after EN supplementation may contribute to a more continuous LD delivery to the brain.
添加儿茶酚-O-甲基转移酶（COMT）抑制剂恩他卡朋（EN）可延长左旋多巴（LD）的血浆代谢时间。目的是确定添加EN后的临床反应以及LD和3-O-甲基多巴[3-OMD]的血浆降解情况。在标准化环境中，未得到最佳治疗的帕金森病住院患者在第一天仅接受与卡比多巴（CD）联合使用的相同剂量LD治疗，第二天接受与CD和EN联合使用（每日三次）的相同剂量LD治疗。我们在两天的固定时间对运动症状进行评分，并测量LD和3-OMD水平。在LD/CD/EN治疗期间，运动障碍得到了显著改善，这可能是由于LD水平的最大浓度[C(max)]显著升高以及计算得出的曲线下面积值所致。在前两次LD/CD/EN摄入后，LD达到C(max)的时间显著延迟。EN对3-OMD水平产生了影响。补充EN后，LD吸收可能增加且LD代谢时间延长，这可能有助于向大脑更持续地输送LD。
