Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0027497 (nausea)
 23,468 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Azasetron, a selective 5-HT3 receptor antagonist, has been previously shown to be highly effective in the prophylaxis of nausea and vomiting induced by anticancer drugs and is widely used in the clinical setting in Japan. In order to improve the antiemetic effect of azasetron, we designed a continuous intravenous infusion method of this drug and compared the antiemetic effect of this method with that of standard bolus intravenous injection on nausea and vomiting associated with anticancer drugs including 75 mg/m2 cisplatin (CDDP). A continuous group is intravenous bolus injection of 2.5 mg azasetron followed by 7.5 mg continuous intravenous infusion for 24 hrs, and a bolus group is intravenous bolus injection of 10 mg azasetron. The inhibitory effect on nausea of the continuous group was significantly superior to those of the bolus group on day 3 and 4 (p < 0.05) and inhibitory effect on vomiting of the continuous group was significantly superior to those of bolus group on day 2 (p < 0.05). No adverse effects were observed in either group of this study. From these data, continuous intravenous infusion of azasetron was considered to be highly effective in prophylaxis of nausea and vomiting induced by anticancer drugs.
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PMID:[Study on clinical effect of a continuous intravenous infusion of azasetron against nausea and vomiting induced by anticancer drugs including CDDP]. 867 1

Anticipatory nausea and vomiting (ANV) are learned responses to chemotherapy that develop in up to 25% of patients by the fourth treatment cycle. Post-treatment nausea and emesis must occur before development of ANV can take place. Certain patient characteristics and other responses to chemotherapy can also be used to predict their occurrence. Once they develop, ANV cannot be controlled by pharmacologic means including use of new 5-HT3 receptor antagonists. By contrast, behavioral therapies involving relaxation, most notably systematic desensitization, can be used to effectively treat ANV. Clinic personnel including oncologists and oncology nurses as well as behavioral psychologists can effectively administer systematic desensitization to chemotherapy patients.
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PMID:Models, mechanisms and management of anticipatory nausea and emesis. 869 50

A number of non-cisplatin cytotoxic regimens induce moderate to severe nausea and emesis. Moreover, the majority of these regimens are given to outpatients where an effective, well-tolerated anti-emetic therapy is particularly important to maintain patients' well-being. This review focuses on the management of nausea and emesis induced by non-cisplatin chemotherapy particularly regimens that do not contain cyclophosphamide or carboplatin, as these are reviewed elsewhere in this volume. For patients receiving highly emetogenic cytotoxic therapy such as dacarbazine, total body irradiation or hemi-body irradiation, a 5-HT3 receptor antagonist plus a corticosteroid may provide optimal control of emesis and nausea. High-dose single-fraction and fractionated radiotherapy to the upper abdomen induces moderate emesis. Traditional anti-emetics prevent emesis in approximately 50% of patients; 5-HT3 receptor antagonists provide a more effective anti-emetic therapy for these patients. Studies evaluating anti-emetics in specific chemotherapy regimens will give clear guidelines for the management of emesis in different patient populations.
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PMID:Management of other non-cisplatin-induced emesis. 869 52

High-dose cisplatin chemotherapy induces a biphasic pattern of emesis. Following the initial peak of emesis, which occurs during the first 8 h after cisplatin, there is a reduction in the occurrence of symptoms with a further increase in the incidence of nausea and emesis which are most severe 48-72 h following cisplatin administration. This latter phase of emesis is defined as delayed emesis and is distinct from the prolonged emesis which occurs after non-cisplatin chemotherapy such as cyclophosphamide. The incidence and severity of delayed emesis is influenced by the dose of cisplatin, being particularly severe in patients receiving doses > 100 mg/m2. Patients who have good control of acute emesis experience less delayed emesis. For this reason, clinical trials designed to evaluate antiemetics for delayed emesis should be carefully designed; ideally patients should be randomized to different treatments after the first 24 h. Studies which have used this design have shown that metoclopramide plus dexamethasone is an effective treatment. However, approximately 50% of patients may experience delayed emesis despite this treatment. The efficacy of the 5-HT3 receptor antagonists in the control of cisplatin-induced delayed emesis in phase II studies has been equivocal and large well-controlled studies with these agents are needed to establish their role in this setting.
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PMID:Management of cisplatin-induced delayed emesis. 869 55

The serotonin 5-HT3 receptor is unique among the seven serotonin receptor "families" that have been recognized so far. It functions not as a G-protein coupled but as a direct ion channel gated receptor. Because of the varied neural functions linked to this receptor, intensive research interest has developed in recent years about its basic and clinical pharmacology, which are summarized in this review. Some new agonists and many new antagonists have been developed. These agents have a useful role as selective pharmacologic research probes, and some of them can be used therapeutically as potent and selective anti-nausea and antiemetic drugs, particularly in patients undergoing cancer chemotherapy treatment or general anesthesia procedures. Potential applications of these agents include the treatment of some behavioral disorders in mental disease, drug addiction, and certain types of pain syndromes.
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PMID:5-HT3 receptors: pharmacologic and therapeutic aspects. 878 44

While the use of 5-HT3 receptor antagonists is clearly justified in patients receiving cisplatin, their role with less emetic drugs is still not defined. The aim of our randomized study was to verify the efficacy of the single standard dose of three 5-HT3-receptor-antagonists in moderately emetic chemotherapies. Sixty chemotherapy-naive breast cancer patients of 30 to 71 years in age, P.S. = 0-1, receiving 5-fluorouracil-epirubicin-cyclophosphamide (FEC 75) q 21 days or cyclophosphamide-methotrexate-5-fluorouracil (CMF) or 120 mg/m2 epirubicin or high dose mitomycin-methotrexate-mitoxantrone (MMM) q 14 days (+ G-CSF) or 100 mg/m2 epirubicin (+ G-CSF) were randomized to receive, 15 min before chemotherapy, 8 mg i.v. bolus of ondansetron or 3 mg i.v. granisetron or 5 mg i.v. tropisetron and no further antiemetic therapy in the following days. 180 cycles were evaluable. Complete protection, (the absence of vomiting episodes,) was respectively 75%, 70% and 70% in the acute and 70%, 82%, 72% in the delayed phases, and an absence of nausea was 56%, 37% and 20% in the acute phase and 50%, 35% and 27% in the delayed, respectively. Complete response, (absence of vomiting and absence or mild nausea,) was 74%, 58.6% and 50.8% in the acute and 64%, 63.7%, 47.3% in the delayed phases, respectively. At the statistical analysis no significant differences between the three drugs were found regarding acute vomiting while ondansetron was superior to granisetron and tropisetron in acute (p = 0.018; p < 0.05) and delayed nausea (P = 0.104; p < 0.01). This activity is practically the same as that we reported (Ann Oncol 1994; 6, suppl 8: 204) with a loading dose on day 1 and maintenance for the following 2-5 days, but with a significantly favorable cost-benefit ratio.
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PMID:Prevention of delayed emesis by a single intravenous bolus dose of 5-HT3-receptor-antagonist in moderately emetogenic chemotherapy. 880 24

In contrast to the broad experience concerning the therapeutic use of carboplatin, only limited data are available regarding the patterns of carboplatin-induced emesis, one of its most distressing side effects. This study reports frequency, severity and time course of carboplatin-induced vomiting and nausea refractory to 5-HT3 antagonism. A total of 216 patients receiving single-day carboplatin-based chemotherapy regimen were enrolled into an open multicenter study focusing on the safety and efficacy of ondansetron 8 mg t.d.s. Emesis on day 1 occurred in 22% and nausea in 75% of the patients; 44% of patients reported some degree of vomiting within the 5 days observation period. The risk for emesis and nausea over 2-5 days was increased in patients suffering from emesis on day 1 (relative risk 2.25 for vomiting and 2.84 for nausea, respectively). The median cumulative number of emetic episodes was 0 for all patients and 4 for the patients who did vomit at least on 1 day. Vomiting began on average 1.77 days following chemotherapy administration. The mean duration of vomiting was 2 days and 3.1 days for nausea. Carboplatin showed a monophasic prolonged pattern of emesis. The combination with cyclophosphamide led to an earlier onset and a higher frequency of vomiting. The analysis of the pattern of emesis refractory to 5-HT3 receptor blockade should help to describe the course of emesis, which is probably triggered through a 5-HT3 receptor-independent mechanisms.
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PMID:Pattern of carboplatin-induced emesis. The German Ondansetron Study Group. 884 74

Nausea and vomiting are the most frequently reported adverse effects of cancer chemotherapy and have a significant impact on patients' daily functioning, quality of life and compliance with chemotherapy. Summarized in this article are the recommendations for the optimal management of nausea and vomiting developed by a multidisciplinary group of health care professionals. Issues relating to chemotherapy-induced nausea and vomiting are discussed; general principles of treatment are reviewed; treatment algorithms based on emetogenicity and types of chemotherapy are presented; and the importance of issues including non-pharmacological approaches, patient education and pharmacoeconomic perspectives are considered. The goal of antiemetic therapy should be no episodes of vomiting or retching and minimal or no nausea. Data from clinical trials support the clear superiority of 5-HT3 receptor antagonists in a variety of clinical situations. Their cost must be considered not only as an isolated item from the institutional perspective, but also from the perspective of the impact of successful therapy on the patient.
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PMID:Guidelines for the optimal management of chemotherapy-induced nausea and vomiting: a consensus. 885 13

The effects of delta 9-tetrahydrocannabinol on single-unit activity in the subpostremal division of the nucleus tractus solitarii were investigated by extracellular recording in rat brain slices. The spontaneous firing rate of 54.8% of the recorded neurons was significantly changed after bath applications of delta 9-tetrahydrocannabinol. Putative nutrition-related neurons responding to a moderate increase in glucose concentration were selectively sensitive to delta 9-tetrahydrocannabinol. The delta 9-tetrahydrocannabinol-sensitive neurons were depressed by clonidine and are therefore likely to be adrenergic or noradrenergic. These observations suggest that some catecholaminergic, glucose-responsive neurons in the subpostremal nucleus tractus solitarii might mediate the influence of cannabinoids on feeding behaviour. Furthermore, most delta 9-tetrahydrocannabinol-sensitive neurons in the nucleus tractus solitarii showed opposite responses to delta 9-tetrahydrocannabinol and the 5-HT3 receptor agonist 1-phenylbiguanide, and might therefore be involved in the nausea-reducing effects of cannabinoids.
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PMID:Neuronal responses to delta 9-tetrahydrocannabinol in the solitary tract nucleus. 889 9

The involvement of 5-hydroxytryptamine3 (5-HT3) receptors in gastric motor and sensory responses to distension and duodenal lipid was investigated. Subjects were studied on four occasions during which isotonic saline or 20% Intralipid (2 kcal/ml) was infused intraduodenally (1 ml/min) while the proximal stomach was distended with air (100 ml/min). Subjects received either 8 mg ondansetron (5-HT3 antagonist) or placebo orally in random order. Intragastric pressure was recorded continuously, and subjects reported gastric sensations. Gastric motor and sensory responses to distension during duodenal saline were similar with placebo and ondansetron. Intraduodenal lipid decreased gastric tonic and phasic pressure activity, and this was not influenced by ondansetron. Lipid also induced meal-like fullness followed by nausea during distensions. Ondansetron reduced nausea and did not affect meal-like fullness but increased volumes and pressures at which sensations were reported. Intestinal 5-HT3 receptors are involved in induction of nausea but not of meal-like fullness by intraduodenal lipid and gastric distension. 5-HT3 receptor antagonism reduces gastric sensitivity to distension during intraduodenal lipid infusion.
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PMID:Ondansetron reduces nausea induced by gastroduodenal stimulation without changing gastric motility. 889 77


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