Dose-ranging evaluation of the substituted benzamide dazopride when used as an antiemetic in patients receiving anticancer chemotherapy

  title={Dose-ranging evaluation of the substituted benzamide dazopride when used as an antiemetic in patients receiving anticancer chemotherapy},
  author={Stefan C. Grant and Mark G. Kris and Richard J Gralla and Rebecca A. Clark and Leslie B. Tyson},
  journal={Cancer Chemotherapy and Pharmacology},
SummaryDazopride, 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… 

Amisulpride in the short-term treatment of depressive and physical symptoms in cancer patients during chemotherapies

This study is the first trial on the use of amisulpride in a cohort of oncological, depressed patients during chemotherapy and demonstrated high efficacy and safety.

Cisplatin Resistance: A Cellular Self-Defense Mechanism Resulting from Multiple Epigenetic and Genetic Changes

Decreased accumulation is one of the most common features resulting in cisplatin resistance, and seems to be a consequence of numerous epigenetic and genetic changes leading to the loss of cell-surface binding sites and/or transporters for cisPlatin, and decreased fluid phase endocytosis.

5-HT3 antagonists under development

Most drug candidates in clinical trials were discovered in the early 1990s and their patent expiry is imminent, so structurally diverse compound libraries need to be extensively investigated for identification of novel 5-HT3 receptor antagonists.



Metoclopramide: dose-related toxicity and preliminary antiemetic studies in children receiving cancer chemotherapy.

A dose-increase MCP toxicity study in children receiving highly emetic chemotherapy such as cisplatin or cyclophosphamide, finding that children who received two consecutive days of MCP had a higher frequency of EPRs, and metoclopramide had promising antiemetic efficacy in a preliminary nonrandomized trial.

Dose-ranging evaluation of the serotonin antagonist GR-C507/75 (GR38032F) when used as an antiemetic in patients receiving anticancer chemotherapy.

Patients with cancer receiving chemotherapy known to produce nausea and vomiting received three intravenous infusions of GR-C507/75 every two hours beginning 30 minutes before chemotherapy, and antiemetic effects were seen in patients receiving cisplatin at 120 mg/m2.

Antiemetic control and prevention of side effects of anti‐cancer therapy with lorazepam or diphenhydramine when used in combination with metoclopramide plus dexamethasone. A double‐blind, randomized trial

During the time that patients are at the greatest risk for emesis, the 24 hours immediately following cisplatin, three drug antiemetic combinations of either lorazepam or diphenhydramine with metoclopramide plus dexamethasone stopped cis platin‐induced emesis for the majority of patients and lessen other treatment‐related side effects.

A single-blind comparison of intravenous ondansetron, a selective serotonin antagonist, with intravenous metoclopramide in the prevention of nausea and vomiting associated with high-dose cisplatin chemotherapy.

Ondansetron is more effective, produces fewer adverse events, and is easier to administer than metoclopramide for the prevention of emesis associated with high-dose cisplatin chemotherapy.

Phase II trials of the serotonin antagonist GR38032F for the control of vomiting caused by cisplatin.

Three phase II studies of the serotonin antagonist GR38032F were conducted, and Mild sedation, headache, and transient elevations of serum SGOT (AST) were observed, and no extrapyramidal symptoms occurred.

Antiemetic efficacy of high-dose metoclopramide: randomized trials with placebo and prochlorperazine in patients with chemotherapy-induced nausea and vomiting.

It is concluded that metoclopramide in high intravenous doses has greater antiemetic activity than placebo or prochlorperazine in patients receiving cisplatin chemotherapy in patients with advanced cancer.

Oral metoclopramide with or without diphenhydramine: potential for prevention of late nausea and vomiting induced by cisplatin.

Extrapyramidal reactions in the younger group and agitated depression in the older group were the major dose-terminating toxic effects, and patient acceptance of these regimens was excellent.

Emesis induced by cisplatin in the ferret as a model for the detection of anti-emetic drugs

Prevention of cisplatin-induced emesis: a double-blind multicenter randomized crossover study comparing ondansetron and ondansetron plus dexamethasone.

  • F. RoilaM. Tonato D. Donati
  • Medicine, Psychology
    Journal of clinical oncology : official journal of the American Society of Clinical Oncology
  • 1991
Ondansetron plus DEX is more efficacious than OND in protecting patients from CDDP-induced emesis and nausea, and dexamethasone added to OND increases antiemetic efficacy.

Antiemetic efficacy of dexamethasone. Randomized, double-blind, crossover study with prochlorperazine in patients receiving cancer chemotherapy.

Dexamethasone is an effective and safe antiemetic in patients receiving cancer chemotherapy without cisplatin, and patients experienced significantly less nausea and vomiting with dexamethAsone than with prochlorperazine.