Stocchi F, Barbato L, Bramante L, Bonamartini A, Ruggieri S
Department of Neurosciences, La Sapienza University, Rome, Italy.
Funct Neurol. 1994 Sep-Oct;9(5):259-64.
Levodopa methyl ester (LDME) is a highly water soluble derivative produced by esterification of the carboxilic acid moiety of the L-Dopa molecule that is rapidly hydrolyzed to L-Dopa and can be administered orally in an easily dosable liquid form. In this study the relative efficacy and tolerability of a single dose of an oral solution of 250 mg of LDME was compared to that of placebo in reversing afternoon off period. A controlled double-blind cross-over study versus placebo had previously been carried out in 25 idiopathic parkinsonian patients with predictable fluctuations in motor performances. The study design stipulated the sequential administration of LDME and placebo in group A and placebo and LDME in group B on two consecutive days. All patients turned "on" with LDME and none with placebo solution. The mean latency to "on" was 25.3 +/- 13.5 min for the A group and 27.6 +/- 3.9 min for group B (Fig. 2) and the "on" duration was 147.7 +/- 50.3 min and 163.3 +/- 39.3 min for the A and B groups respectively. Five patients suffering from drug resistant "off" phenomena turned "on" with LDME solution showing a mean latency to "on" of 31.4 +/- 6.2 min.
左旋多巴甲酯（LDME）是一种高度水溶性的衍生物，由左旋多巴分子的羧酸部分酯化产生，它能迅速水解为左旋多巴，并且可以以易于给药的液体形式口服。在本研究中，将单剂量250mg LDME口服溶液与安慰剂在逆转下午“关”期方面的相对疗效和耐受性进行了比较。此前，对25名运动表现有可预测波动的特发性帕金森病患者进行了一项与安慰剂对照的双盲交叉研究。研究设计规定，A组连续两天依次给予LDME和安慰剂，B组依次给予安慰剂和LDME。所有患者服用LDME后均出现“开”期，服用安慰剂溶液则无此现象。A组“开”期的平均潜伏期为25.3±13.5分钟，B组为27.6±3.9分钟（图2），A组和B组的“开”期持续时间分别为147.7±50.3分钟和163.3±39.3分钟。5名患有耐药性“关”期现象的患者服用LDME溶液后出现“开”期，“开”期的平均潜伏期为31.4±6.2分钟。
