Joss R A, Galeazzi R L, Bischoff A K, Brunner K W
Eur J Clin Pharmacol. 1985;27(6):721-5. doi: 10.1007/BF00547056.
In early clinical trials alizapride showed a better antiemetic activity with fewer side effects than metoclopramide. Alizapride has now been evaluated in an open dose-ranging study in 24 patients receiving strongly emetic chemotherapy. Alizapride 4-8 mg/kg was given as a 15 min infusion 0.5 h before and 1.5, 3.5, 5.5 and 8.5 h after the chemotherapy. At the dose levels of 6 and 8 mg/kg x 5, respectively 6 out-of 9 and 4 of 4 patients experienced side effects (hypotension, dizziness, profuse sweating, general malaise and diarrhoea). At 4 mg/kg x 54 of 15 patients experienced side effects due to alizapride (dyspnoea 1, diarrhoea 2, extrapyramidal syndrome 1 patient). Overall, 9 of 24 patients were partially or completely protected from nausea and vomiting. Based on this experience alizapride has antiemetic activity and few side effects in the dose of 4 mg/kg x 5.
在早期临床试验中,阿立必利显示出比甲氧氯普胺更好的止吐活性,且副作用更少。阿立必利现已在一项开放性剂量范围研究中进行评估,该研究纳入了24名接受强效致吐化疗的患者。阿立必利4 - 8mg/kg在化疗前0.5小时以及化疗后1.5、3.5、5.5和8.5小时以15分钟输注的方式给药。在剂量水平分别为6mg/kg×5和8mg/kg×5时,9名患者中有6名以及4名患者中的4名出现了副作用(低血压、头晕、大量出汗、全身不适和腹泻)。在4mg/kg×5的剂量水平时,15名患者中有4名因阿立必利出现了副作用(呼吸困难1例、腹泻2例、锥体外系综合征1例)。总体而言,24名患者中有9名在一定程度上或完全免受恶心和呕吐的困扰。基于这一经验,阿立必利在4mg/kg×5的剂量下具有止吐活性且副作用较少。