Grant S C, Kris M G, Gralla R J, Clark R A, Tyson L B
Department of Medicine, Memorial Sloan-Kettering Cancer Center, New York, NY 10021.
Cancer Chemother Pharmacol. 1993;31(6):442-4. doi: 10.1007/BF00685032.
Dazopride, a substituted benzamide structurally related to metoclopramide, is a potent gastric prokinetic agent that prevents cisplatin-induced emesis in animals. Unlike metoclopramide, dazopride has no effect on dopamine receptors and therefore should not produce extrapyramidal side effects. In this dose-ranging trial, 23 patients with cancer receiving chemotherapy known to produce nausea and vomiting received three i.v. infusions of dazopride every 2 h beginning 30 min before the chemotherapy. Seven dose levels were explored ranging from 0.5 to 4.0 mg/kg in each of the three infusions. Toxicities were mild and included sedation, dizziness, visual disturbances, and headaches. All side effects were transient and were not dose-related. Antiemetic effects were observed. Dazopride can be safely given on this schedule at doses of up to 4.0 mg/kg to patients receiving chemotherapy. On the basis of the results of this trial, further studies of this agent are warranted.
多佐胺是一种结构上与甲氧氯普胺相关的取代苯甲酰胺，是一种强效的胃促动力剂，可预防动物顺铂诱导的呕吐。与甲氧氯普胺不同，多佐胺对多巴胺受体无作用，因此不应产生锥体外系副作用。在这项剂量范围试验中，23名接受已知会引起恶心和呕吐的化疗的癌症患者在化疗前30分钟开始，每2小时静脉输注三次多佐胺。在三次输注中的每次输注中，探索了从0.5至4.0mg/kg的七个剂量水平。毒性轻微，包括镇静、头晕、视觉障碍和头痛。所有副作用都是短暂的，且与剂量无关。观察到了止吐效果。多佐胺按此方案以高达4.0mg/kg的剂量给予接受化疗的患者是安全的。基于该试验结果，有必要对该药物进行进一步研究。
