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A series of new substituted benzamides has been synthesized and evaluated for dopamine antagonist activity and for antagonism of cisplatin-induced emesis in the dog and in the ferret. It was found that modification of the 2-methoxy substituent of metoclopramide was detrimental to dopaminergic D2
The antiemetic effect of two benzamides, metoclopramide (MCL; Paspertin) and alizapride (AZP; Vergentan), was compared in two double-blind sequential analytical trials in cisplatin-treated patients (60-90 mg/m2). In the first trial, the drugs were given as loading infusions (0.5 mg/kg of body
None of the available antiemetics is entirely effective, perhaps because most of them act through the blockade of one receptor. There is a possibility that a combination of antiemetics with different sites of activity would be more effective than one drug alone for prophylaxis against postoperative
Breast cancer surgery performed under general anesthesia is associated with a high incidence of postoperative nausea and vomiting (PONV). A number of approaches are available for the management of PONV after breast cancer surgery. First, the risk factors related to patient characteristics, surgical
Postoperative nausea and vomiting (PONV) are distressing and frequent adverse events of anesthesia and surgery, with a relatively high incidence after laparoscopic cholecystectomy. Numerous antiemetics have been studied for the prevention and treatment of PONV in patients scheduled for laparoscopic
The common and distressing complications of postoperative nausea and vomiting (PONV) are the main concern of 40-70% of patients undergoing laparoscopic cholecystectomy (LC). The first step in preventing PONV after LC is to reduce the risk factors involving patient characteristics, surgical
1. The aim of this study is to review the mechanisms implicated in nausea and vomiting and the treatment of these symptoms. 2. Metoclopramide, a benzamide, is the drug most frequently used to alleviate or abolish the majority of nausea and vomiting of different origin. Domperidone, which scarcely
The novel benzamide derivative itopride was assayed for its effect on gastrointestinal motility in conscious dogs when it was administered intraduodenally (i.d.). Gastrointestinal motility was measured by means of chronically implanted force transducers, and itopride at a dose of 10 mg/kg, i.d. or
OBJECTIVE
To review the emetic potential of chemotherapeutic agents and the specific factors that may help to identify patients who are most vulnerable to nausea and vomiting following chemotherapy. To review the classes of antiemetic drugs that effectively control nausea and vomiting associated
The antiemetic effect of a new benzamide, alizapride, was investigated with escalating doses through four levels starting at 5 mg/kg/cycle up to 20 mg/kg/cycle. 39 patients were accrued who received cancer chemotherapy which included the following drugs in various combinations: cyclophosphamide,
To evaluate the antiemetic effectiveness and toxicity of a novel congener of metoclopramide (MCP), alizapride (AZP), 29 patients receiving cisplatin (50 mg/m2) alone or with adriamycin (40 mg/m2) were entered into a randomized cross-over trial comparing moderate-dose AZP (2 mg/kg for 4 doses)
Azaadamantanone 1 was converted to a series of aminoazaadamantane benzamides 9a-d, which were profiled for serotonin receptor activity. Aminomethylazaadamantane SC-54750 is a potent 5-HT(4) agonist and 5-HT(3) antagonist with in vivo efficacy in gastroparesis models and also inhibits
A series of 4-amino-5-chloro-2-methoxy- and 2-ethoxy-N-[(4-substituted 2-morpholinyl)methyl]benzamides (11-64) were prepared and evaluated for gastrokinetic activity by determining their effects on the gastric emptying of phenol red semisolid meal in rats. The N-4 substituent includes alkyl,