Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UNIPROT:P46098 (5-HT3 receptor)
 2,290 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Ondansetron, a selective 5-HT3 receptor antagonist, has recently been shown, in a dose of 8 mg, to be superior to 1.25 mg droperidol in preventing postoperative vomiting. There are indications that a dose of 4 mg of ondansetron may be just as effective in reducing postoperative nausea and vomiting as a dose of 8 mg. The aim of this study was to evaluate the efficacy and the adverse effects of 4 mg ondansetron in the prevention of postoperative nausea and vomiting compared to droperidol in patients undergoing surgery with inhalation anaesthesia supplemented with alfentanil. METHODS. Following institutional approval, 40 ASA physical status I and II women scheduled for minor gynaecological surgery gave informed consent to participate in this randomized, double-blind comparative study. Five minutes before induction of general anaesthesia, 20 patients received a single intravenous (i.v.) dose of 4 mg of ondansetron and the remaining 20 received 1.25 mg droperidol i.v. Anaesthesia was induced with 2.1-4 mg/kg of thiopental and 0.1 mg of alfentanil i.v. and maintained with 65% nitrous oxide and 1.5%-3% enflurane in oxygen. On pain stimuli another 0.2-0.4 mg of alfentanil was given. Total effective antiemetic response was defined as the absence of nausea and vomiting for 24 h postoperatively. The incidence of nausea, vomiting and the number of patients showing total antiemetic response as well as the incidence of adverse effects were compared with the chi 2 test and P < 0.05 was considered significant. RESULTS. Patients were similar with respect to age, height, body weight and total anaesthetic agents received. Duration of anaesthesia and the time until awakening was not significantly different among groups. Postoperatively 7 out of 20 patients given 4 mg of ondansetron and 3 out of 20 patients with droperidol vomited (n.s.). The incidence of nausea was 11 out of 20 in the ondansetron group, and 4 out of 20 in the droperidol group (P < 0.05). Sixteen patients in the droperidol group and 8 patients in the ondansetron group showed a total effective antiemetic response (P < 0.05). Postoperative sedation and well-being scores did not differ significantly among groups. CONCLUSION. Our results show that for the prevention of postoperative nausea and vomiting 4 mg of Ondansetron was inferior to 1.25 mg of droperidol. The drugs were given intravenously prior to general anaesthesia for minor gynaecological surgery with nitrous oxide and enflurane in oxygen supplemented with small boluses of alfentanil.
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PMID:[Ondansetron as prophylaxis for postoperative nausea and vomiting. A prospective randomized double-blind comparative study with droperidol]. 797 72

Considerable progress has been made in the development of means to limit nausea and vomiting arising from cancer chemotherapy. A number of key conceptual advances in the last decade have been critically important. these include recognition of the value of combination antiemetic therapy, identification of important patient- and treatment-related factors predictive of emesis, and appreciation of the importance of serotonin (5-HT) in the pathophysiology of emesis and the value of selective antagonists of the type-3 serotonin receptor. Comparative trials of the 5-HT3 receptor antagonists and classic antiemetic agents have helped define optimal antiemetic approaches in a number of settings. A combination of a 5-HT3 antagonist and dexamethasone is the treatment of choice for patients receiving single- and multiple-day cisplatin. The 5-HT3 antagonists are also effective agents with noncisplatin chemotherapy. Clear-cut superiority to classic antiemetics such as dexamethasone has not been consistently demonstrated, however. Results with the 5-HT3 antagonists in cisplatin-induced delayed emesis have been disappointing to date. The results of ongoing prospective trials should define their role more clearly. At present a combination of metoclopramide and dexamethasone is the treatment of choice in this setting. Results of trials comparing 5-HT3 antagonists are beginning to emerge. Available information suggests no clinically relevant differences in antiemetic efficacy between these agents. Many questions regarding the optimal use of the 5-HT3 antagonists and their integration into clinical practice remain unanswered and are the appropriate focus for additional study.
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PMID:Treatment of chemotherapy-induced emesis in the 1990s: impact of the 5-HT3 receptor antagonists. 800 Jul 24

In ferrets, the highly selective 5-HT3 receptor antagonist, granisetron, abolished or reduced emesis induced by cisplatin (10 mg/kg i.v.) or whole body X-irradiation (50 Gy in 10.4 min) in a dose-dependent manner when administered by a variety of routes (intravenous, per os, subcutaneous, intramuscular). Complete protection from vomiting and retching was achieved with 0.5 mg/kg i.v. or p.o. granisetron. Granisetron (0.5 mg/kg i.v.) was also effective when given 6 h before cisplatin, completely protecting 50% of ferrets for a total of 10 h. Following repeat dosing, for either 4 days i.v. or 10 days p.o. before emetic challenge, granisetron (0.5 mg/kg) still retained its antiemetic activity on the 5th or 11th day. Prior treatment with cyclophosphamide (80 mg/kg i.v.) resulted in a significantly shorter time to the onset of vomiting after exposure to X-irradiation. Granisetron, but not saline, abolished vomiting and nausea when given as intervention after this combined emetic regimen. These results show that granisetron has potential flexibility for administration via a variety of different routes and also a long duration of action when used as an antiemetic against a wide range of cytostatic agents.
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PMID:Further studies of the antiemetic activity of granisetron against whole body X-irradiation or cisplatin-induced emesis in the ferret. 801 89

Chemotherapy-related nausea and vomiting can today be controlled with available antiemetics in a high percentage of patients but emesis remains a problem for some patients, with certain drugs and with repeated cycles of chemotherapy. The fundamental steps of clinical research in antiemetics towards the improvement of the control of nausea and vomiting with new drugs or combinations are presented. Special emphasis is given to cisplatin-induced nausea and vomiting because of the frequency and relevance of this phenomenon. The use of high-dose metoclopramide, its combination with steroids, and later the addition of lorazepam or diphenhydramine represented the evolving standard of the 1980s, with the level of complete protection from vomiting improving from 30%-40% to 60%-70% with the three-drug combination. The introduction of new agents such as the 5-hydroxytryptamine 3 (5-HT3) receptor antagonists has recently offered new possibilities because of their activity and lack of toxicity. In particular, the combination of ondansetron plus dexamethasone is today the most efficacious and least toxic antiemetic treatment for prevention of emesis in patients treated with a single high dose or low repeated doses of cisplatin. A comparison of different 5-HT3 antagonists, always in combination with steroids, is now considered necessary. For patients treated with moderately emetogenic chemotherapy the use of steroids can still be considered the standard treatment. In this setting, the role of 5-HT3 receptor antagonists, alone or in combination with steroids, has to be better defined through large, well-planned clinical trials, which should have a cost-effectiveness analysis as one of their goals.
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PMID:Antiemetics in cancer chemotherapy: historical perspective and current state of the art. 803 96

Nausea and vomiting are frequent problems in the postoperative period. The introduction of 5-HT3 receptor antagonists has stimulated interest and research in this area. The paper reviews the etiology, physiology, prophylaxis and treatment of postoperative nausea and vomiting. Before using specific antiemetic prophylaxis it is important to evaluate patient risk factors, surgical stimuli and method of anaesthesia. The choice of antiemetic drugs for treatment and prophylaxis should be guided by consideration of effect mechanism, side-effects, clinical documentation and total costs. No single drug is fully effective and combination therapy should be considered in resistant cases.
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PMID:[Postoperative nausea and vomiting]. 807 48

Nausea and vomiting are among the most distressing side-effects of chemoradiotherapy. Conditioning protocols for patients undergoing bone marrow transplantation consist of highly emetogenic high-dose chemotherapy with or without total body irradiation. Marked improvement in controlling emesis and nausea was achieved by the introduction of a new class of antiemetic drugs, the 5HT3 serotonin-receptor antagonists. Tropisetron is a highly potent, selective antagonist of 5HT3 receptors. Previous studies have used a single 5-mg dose i.v. of tropisetron to control nausea and vomiting in cancer patients. The present study was undertaken to evaluate the efficacy and safety of a single daily dose of tropisetron in controlling emesis in patients receiving high-dose chemotherapy (with or without total body irradiation) prior to bone marrow transplantation. The anti-emetic efficacy was investigated in a non-homogeneous cohort in a prospective and open study. Of 11 patients evaluated, 9 (81%) showed complete or major control, 1 (9%) minor control and 1 (9%) failed to respond. The most common adverse events reported during the study included diarrhea (46%) and headache (18%), no patients being withdrawn because of side-effects. Our data suggest that a single 5-mg i.v. dose of tropisetron is safe and effective in preventing chemotherapy-induced emesis in patients receiving bone marrow transplantation conditioning. A larger randomized study is warranted to confirm our preliminary results.
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PMID:The anti-emetic efficacy and tolerability of tropisetron in patients conditioned with high-dose chemotherapy (with and without total body irradiation) prior to bone marrow transplantation. 808 43

Postoperative nausea and vomiting is a major concern for patients undergoing outpatient surgery under general anaesthesia, and may complicate and delay discharge from hospital. This paper evaluates the safety and efficacy of ondansetron, a 5-HT3 receptor antagonist, in the treatment of postoperative nausea and vomiting. One thousand patients in 30 centres in the United States who received general anaesthesia and developed postoperative nausea and vomiting were studied. In a randomised, double-blind, stratified and parallel designed protocol, patients received either ondansetron 1, 4, 8 mg or placebo for nausea or vomiting occurring within 2 h of entry into the Post Anaesthesia Care Unit. Subsequent episodes of vomiting, nausea scores, laboratory and clinical safety data and adverse events were evaluated during the 24-h study period. In a separate study, pharmacokinetic data were compared for intramuscularly and intravenously administered ondansetron. Each dose of ondansetron was significantly better than placebo in reducing nausea from control values during the initial 2-h study period, and in preventing further emesis over 24 h. There were no significant differences in the incidence of adverse events, changes in laboratory values or measures of vital signs in the ondansetron groups compared to the placebo group. Dose comparisons between the three treatment groups showed that ondansetron 4 mg is the optimal dose to treat postoperative nausea and vomiting. Ondansetron is a well tolerated, efficacious antiemetic which has a similar side effect profile to placebo. Intramuscular administration has the same systemic availability as intravenous administration.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Single dose intravenous ondansetron for the 24-hour treatment of postoperative nausea and vomiting. 812 59

One-hundred and forty-five chemotherapy patients receiving cisplatin- and non-cisplatin-containing regimens participated in an open evaluation of ondansetron, a 5-HT3 receptor antagonist, in the prophylaxis of acute and delayed nausea and vomiting. The study had two groups of patients, one receiving cisplatin-containing regimens (Group A) and the other, non-cisplatin-containing regimens (Group B). There were 51 patients recruited to Group A. Ondansetron was given to these patients at a dose of 8 mg intravenously 15 min before chemotherapy, followed by an intravenous infusion for 24 h (1 mg/h), or 8 mg intravenously 4 and 8 h after the start of cisplatin, followed by 8 mg orally three times/day for 5 days. Ninety-four patients were recruited to Group B: these patients received ondansetron at a dose of 8 mg intravenously immediately before chemotherapy or 8 mg orally 1-2 h prior to it, and 8 mg orally three times/day for 3-5 days. For acute emesis (first 24 h), complete control was achieved in 79.5% of Group A patients and in 78.1% of Group B. For delayed emesis (days 2-5), 79.7% of Group A patients and 84.6% of Group B were completely protected during the entire study period. Nausea was also well controlled with ondansetron; 83.2% (Group A) and 86.5% (Group B) reported only mild nausea or no nausea at all. Ondansetron was effective in the control of both cisplatin- and non-cisplatin-induced emesis and well tolerated without any serious drug-related adverse events.
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PMID:Ondansetron in the treatment of nausea and vomiting induced by chemotherapy. Portuguese Ondansetron Study Group. 813 12

This paper reviews recent anti-emetic developments, with particular reference to the 5-HT3 receptor antagonists. These drugs are at least as effective as conventional regimens for controlling acute nausea and vomiting in patients receiving highly or moderately emetogenic chemotherapy and abdominal radiotherapy. They have less side effects than do alternative drugs. Improved control of acute nausea and vomiting by 5-HT3 receptor antagonists seems to reduce anticipatory symptoms in subsequent cycles. Dexamethasone enhances activity of 5-HT3 receptor antagonists in highly emetogenic chemotherapy. Improved control of acute nausea and vomiting by 5-HT3 receptor antagonists may remove one obstacle to offering palliative chemotherapy.
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PMID:Assessing the benefits of anti-emetic innovation. 813 17

There is interest in the development of antiemetics other than dopamine receptor antagonists for the treatment of postoperative nausea and vomiting. A ferret model of morphine-induced emesis may have wider application in evaluating newer agents than the apomorphine dog model. This study describes the conditions for morphine-induced emesis in ferrets and evaluates five antiemetics that are prototypical of three different mechanisms. The average numbers of vomiting and retching episodes induced by morphine (0.1-2.5 mg/kg s.c.) were distributed as a bell-shaped curve. Maximum number of vomits occurred at 0.3 mg/kg (11.8 +/- 2.1 vomits; 45 +/- 12.5 retches). Antiemetics or vehicle were given i.v. 5 min prior to morphine while each ferret was maintained under isoflurane-O2 anesthesia. Ondansetron, a 5-HT3 receptor antagonist, reduced vomiting episodes by 47% and 70% (3 and 10 mg/kg). Granisetron, a 5-HT3 receptor antagonist was inactive at doses of 0.1, 1.0, 3.0 and 10 mg/kg. Metoclopramide reduced vomiting episodes by 48% and 82% (3 and 10 mg/kg). Droperidol reduced vomiting episodes by 84% at 3 mg/kg. Naloxone reduced vomiting episodes by 91% and 43% at doses of 0.1 and 1.0 mg/kg. In most cases, prolonged latency times to the first episodes accompanied the reduction in total numbers of episodes. The significant reduction of morphine-induced emesis in the ferret by ondansetron, metoclopramide and droperidol is consistent with the reduction of postoperative emesis in man by these compounds when morphine was a component of the anesthetic regimen. These results suggested that the morphine ferret model may be useful for evaluating compounds having the potential for preventing and treating postoperative vomiting.
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PMID:The effects of different antiemetic agents on morphine-induced emesis in ferrets. 822 24


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