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)

Efficacy and safety of the antiemetic agent Navoban (5HT3-receptor-antagonist Tropisetron) on cytostatic-induced emesis of breast cancers and gynecological cancers was tested in 28 female patients receiving a total of 127 chemotherapy courses containing high (cisplatin), moderate high (cyclophosphamid) or moderate (for example 5 FU) emetogenic cytostatic drugs. We studied antiemetic response rates of Navoban (5 mg/d) during the first 24 hours after administration of the chemotherapy as well as response rates of the "delayed nausea and emesis" (days 2-9 after chemotherapy). A complete response was observed in 103 chemotherapy courses (= 81.1%) during the first 24 hours after chemotherapy and in 93 courses (= 73.2%) for the "delayed emesis". Treatment failures (more than 5 vomiting episodes) during the first 24 hours were present in four courses and for the "delayed emesis" in 11 courses. The side effects of Navoban such as constipation, headache or tiredness were minimum. Therefore no patient refused to receive the necessary chemotherapy. Navoban is, with its single dose application, an effective therapeutic drug for the prevention of nausea and emesis in patients receiving a chemotherapy.
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PMID:[Effectiveness and tolerance of Navoban (5HT3-receptor antagonist tropisetron) in prevention of cytostatic drug-induced nausea and vomiting in patients with breast carcinomas and gynecological malignancies]. 890 Jun 4

The antiemetic activity of droperidol is attributed to antagonizing the dopaminergic neurons of the chemoreceptor trigger zone. Ondansetron is a serotonin (5HT) receptor antagonist at both peripheral and central 5-HT3 receptor sites with no known action on dopamine-mediated activity. We hypothesized that the combination of these two antiemetics would be more effective than droperidol alone. Women with ASA classified physical status I or II, scheduled for laparoscopic tubal banding, participated in a randomized double-blind clinical trial using a standardized anesthesia regimen. Within 15 min after induction of anesthesia, Group 1 (n = 60) received IV droperidol 1.25 mg and ondansetron 4 mg and Group 2 (n = 60) received IV droperidol 1.25 mg and saline. Before surgery and during recovery at 1, 2, and 24 h, emetic episodes, nausea, pain, drowsiness, medications taken, and adverse events were recorded. The complete response (no emesis, no rescue) for Group 1 was 55 of 60 (91.6%) versus 47 of 60 (78.3%) in Group 2 (P = 0.04). No patient needed rescue antiemetic medication in Group 1, whereas 5 of 60 (8.3%) patients were rescued in Group 2 (P = 0.03). There were seven emetic episodes in five patients in Group 1 and 30 emetic episodes in 12 patients in Group 2 over the 24-h study period (P = 0.03). The time to the first emetic episode was more than twice as long for Group 1 than Group 2 (P = 0.03) and total nausea scores were lower in Group 1 than Group 2 (P = 0.01). The droperidol/ondansetron combination was significantly superior to droperidol in complete response, time to and number of emetic episodes, and the incidence and severity of nausea in women having tubal banding.
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PMID:Droperidol/ondansetron combination controls nausea and vomiting after tubal banding. 917 30

Efficiency of ondansetron, a selective 5-HT3 receptor antagonist, in prevention of postoperative nausea and vomiting in 40 ASA I-II patients who will undergo emergency intraabdominal operations is studied in a randomized double-blind and placebo controlled study. Patients of no premedication are administered 4 mg i.v. ondansetron or placebo (saline) before induction. Thiopental (4 mg/kg) was used for induction, succinylcholine (2 mg/kg) for muscular relaxation, and 50% nitrous oxide in oxygen and isoflurance (0.8-1.5%) for the maintenance of anesthesia, and fentanyl and norcuron were administered when necessary. Vital signs were closely monitored and recorded during anesthesia and early postoperative period. Study is carried out during postoperative 0-1 h, 1-2 h and 2-24 h periods. Nausea scores and emesis were recorded during 0-1 and 1-2 h periods. Ondansetron was found significantly more effective than placebo (p < 0.05 and p < 0.05). Although is was effective during 2-24 h period, the difference was not statistically significant (p > 0.05). No significant difference was observed between the groups in terms of vital findings, laboratory findings and side effects (p > 0.05). Therefore it is concluded that administration of prophylactic i.v. ondansetron to patients undergoing emergency intraabdominal operations is effective in prevention of nausea and vomiting without any significant side effects.
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PMID:Prophylactic administration of ondansetron in emergency intraabdominal operations. 899 79

A series of 2-piperazinylbenzimidazole derivatives were prepared and evaluated as 5-HT3 receptor antagonists. Their 5-HT3 receptor affinities were evaluated by radioligand binding assays, and their abilities to inhibit the 5-HT-induced Bezold-Jarisch reflex in anesthetized rats were determined. Compound 7e (lerisetron, pKi = 9.2) exhibited higher affinity for the 5-HT3 receptor than did tropisetron and granisetron, while compound 7q (pKi = 7.5) had very low affinity for this receptor, showing that substitution on the N1 atom of the benzimidazole ring is essential for affinity and activity. The effect of substitution on the aromatic ring of benzimidazole by several substituents in different positions is also discussed. A strong correlation between the 5-HT3 antagonistic activity of the studied compounds and the position of substitution on the aromatic ring was established. Thus, while the 4-methoxy derivative 7m showed weak affinity for the 5-HT3 receptor (pKi = 6.7), the 7-methoxy derivative 7n exhibited the highest affinity (pKi = 9.4). Compounds 7e and 7n are now under further investigation as drugs for the treatment of nausea and emesis evoked by cancer chemotherapy and radiation.
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PMID:New 2-piperazinylbenzimidazole derivatives as 5-HT3 antagonists. Synthesis and pharmacological evaluation. 904 49

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 two treatment methods using this drug and compared the antiemetic effect of this method with that of standard bolus intravenous injection on nausea and vomiting associated with anticancer drug including 75 mg/m cisplatin (CDDP). The two-treatment group received an intravenous bolus injection of 5 mg azasetron before and 8 hours after the start of chemotherapy, and a standard group was given an intravenous bolus injection of 10 mg azasetron only once a day. The inhibitory effect on vomiting in the two-treatment group was significantly greater than those of the standard group on day 1 and 2 (p = 0.0458, p = 0.0273), and the inhibitory effect on nausea of the two-treatment group tended to be superior those of the bolus group on day 2 (p = 0.0533). No adverse effects were observed in either group of this study. From these data, the two-treatment approach was considered to be highly effective in prophylaxis of nausea and vomiting induced by anticancer drug.
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PMID:[Clinical effect of two azasetron treatment methods against nausea and vomiting induced by anticancer drugs including CDDP]. 917 May 25

In the past few years important progress in the prevention of chemotherapy-induced nausea and vomiting has been made mainly thanks to the introduction of the 5-HT3 receptor antagonists in clinical practice (ondansetron, granisetron, tropisetron). In the prevention of acute emesis induced by cisplatin, an intravenous combination of a 5-HT3 receptor antagonist plus single dose dexamethasone (20 mg) should be considered the treatment of choice. This is also the case in the prevention of acute emesis induced by moderately emetogenic chemotherapy (intravenous cyclophosphamide, doxorubicin, epirubicin, carboplatin, used alone or in combination), but high and repeated doses of dexamethasone should be used (8 mg intravenously plus 4 mg orally every 6 hours for four doses starting contemporarily to chemotherapy administration). Several-well conducted double-blind comparative studies among intravenously administered 5-HT3 receptor antagonists have been carried out. Almost all showed that they have identical antiemetic activity and tolerability. Therefore, the choice among 5-HT3 receptor antagonists should be based only on their acquisition cost in each country. In the prevention of delayed emesis (from day 2 to day 4) induced by cisplatin oral metoclopramide (0.5 mg/kg or 20 mg every 6 hours for four doses daily) and oral ondansetron (8 mg twice daily), both combined with dexamethasone, showed similar antiemetic efficacy. Metoclopramide plus dexamethasone should be considered the antiemetic regimen of choice due to its lower cost. Ondansetron plus dexamethasone is a valid alternative regimen that should be preferred in patients who not tolerate metoclopramide and in patients who suffer from acute vomiting. In the prevention of delayed emesis induced by moderately emetogenic chemotherapy oral dexamethasone or oral ondansetron showed a good antiemetic efficacy, but the results from a recently published study seem suggest the necessity to treat only patients who present acute vomiting or moderate-severe nausea. In fact, patients obtaining complete protection from vomiting and nausea (or at most mild acute nausea) have a very low incidence of delayed emesis.
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PMID:[Recent improvements in antiemetic therapy]. 923 27

Recently, granisetron (KYT), one of the 5-HT3 receptor antagonists, has been developed and proved to have a strong effect for cisplatin (CDDP)-induced emesis. The combination chemotherapy with CDDP and 5-fluorouracil (5-FU), which has great efficacy for head and neck cancer, induces nausea and vomiting as side effects. We compared the effects of KYT for CDDP plus 5-FU-induced emesis between two administration schedules. Forty patients were randomized to two groups. KYT was administered either on day 1 for twenty patients (Group A), or for consecutive 5 days in another twenty patients (Group B). Additional antiemetics were administered in thirteen patients in Group A and seven patients in Group B for severe nausea and vomiting even after KYT administration. The times of additional antiemetics administration were more frequent in Group B. The nausea score was statistically lower in Group B and the duration of nausea or vomiting was statistically longer in Group A. The frequency of vomiting was the same in the two groups on day 1, but it was controlled faster in Group B. Appetite loss was lower on day 7 in Group B. It was concluded that vomit and nausea were controlled better in Group B after day 4. Additional antiemetics were not effective, and 5 consecutive administrations of KYT for chemotherapy with CDDP plus 5-FU was effective for late emesis.
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PMID:[Comparison of effects between single vs five-day injection of granisetron for combination chemotherapy with cisplatin and 5-fluorouracil for head and neck cancer]. 923 62

In the past few years a combination of a 5-HT3 receptor antagonist plus dexamethasone has been shown to be the most efficacious antiemetic prophylaxis of acute emesis induced by cisplatin and moderately emetogenic chemotherapy. In the prevention of cisplatin-induced delayed emesis oral metoclopramide or ondansetron, both combined with dexamethasone, offer similar antiemetic protection. Due to its lower cost the metoclopramide regimen remains the treatment of choice, whereas the ondansetron one is a valid alternative treatment that may be preferred in patients who present acute emesis. In the prevention of delayed emesis induced by moderately emetogenic chemotherapy ondansetron and dexamethasone have been shown superior to placebo. On the other hand, a recent observational study suggested that patients presenting acute vomiting or acute moderate-severe nausea, having a high incidence of delayed emesis, should always receive antiemetic prophylaxis. Instead, patients obtaining complete protection from acute emesis may not require any antiemetic prophylaxis.
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PMID:Antiemetics revisited. 925 81

Paclitaxel (Taxol; Bristol-Myers Squibb Company, Princeton, NJ) and cisplatin are cytotoxic drugs active against non-small cell lung cancer (NSCLC) that possess additive cytotoxicity in animal tumors. Paclitaxel and cisplatin are active in patients with advanced NSCLC when given on a 3-weekly schedule. In an attempt to increase activity, we designed a phase II study with a biweekly schedule. Paclitaxel 110 mg/m2 was given by 3-hour intravenous infusion, followed by cisplatin 60 mg/m2 via intravenous infusion. Treatment was scheduled every 2 weeks. Of the 42 patients treated, 19 were men and 23 were women, with a median age of 54 years (range, 31 to 69 years). Four patients had stage IIIA NSCLC, 18 stage IIIB, and 20 stage IV. Median World Health Organization performance status was 1 (range, 0 to 2), and adenocarcinoma was the most common histology (52%). A median of nine cycles was administered (range, one to 24 cycles), with more than 360 cycles administered. Rates of frequency of World Health Organization grade 3 or 4 toxicities were as follows: neutropenia, 20%; thrombocytopenia, 2%; nausea/vomiting, 7% (despite prophylactic treatment with 5-HT3 receptor antagonists plus prednisolone); neurotoxicity, 2%; and nephrotoxicity, 2%. There were three septicemic episodes, no bleeding episodes, and no toxic deaths. Dose reduction was performed in 15 patients (36%), due to nephrotoxicity in 14 cases. Treatment delay was necessary in 23 patients (55%), most often due to neutropenia (nine cases). Forty patients are currently evaluable for response, with two complete and 15 partial responses (overall response rate, 43%; 95% confidence limits, 27% to 59%). Median response duration was 31 weeks (range, 9 to 85 weeks). The biweekly schedule of paclitaxel plus cisplatin has noteworthy activity in patients with NSCLC. A relatively large fraction of patients required either dose reduction and/or treatment delay, but World Health Organization grade 3 or 4 toxicity was rare, apart from the neutropenia that caused only a few septicemic episodes.
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PMID:Preliminary results of a phase II study of paclitaxel and cisplatin in patients with non-small cell lung cancer. 933 Nov 14

In 1983, Coates conducted a survey that ranked the side-effects perceived by patients receiving chemotherapy in the order of their severity. Vomiting and nausea were found to be the two most distressing side-effects. They have an impact on quality of life and compliance with treatment. The development of 5HT3 antagonists has been a major step forward in the prevention and treatment of chemotherapy-induced nausea and vomiting. Presently, these antiemetics are routinely used as concomitant therapy in emetogenic chemotherapy regimens. The purpose of this study was to evaluate the impact of 5HT3 antagonists on patient perceptions of the side-effects of chemotherapy. Coates' survey was replicated in patients who received 5HT3 antagonists for acute nausea and vomiting resulting from emetogenic chemotherapy. Patients received the survey to identify those physical and non-physical side-effects that they attributed to chemotherapy and were asked to rank the five most distressing side-effects. Of the 197 patients who consented to take part in the study, 181 were evaluable. Nausea, hair loss and vomiting were described as the three most distressing side-effects of chemotherapy. Eighty per cent of all the patients actually experienced nausea and 57% experienced vomiting. Hair loss appeared to be more distressing to women (P < 0.001) but, in other aspects, gender, age and marital status did not influence the ranking of the three most distressing side-effects. Constipation was ranked as 6th and was not identified as a distressing side-effect in 1983. Nausea and vomiting remain to be the first and third most distressing side-effects of chemotherapy, even though the incidence and severity of acute nausea and vomiting are now significantly reduced.
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PMID:Patient perceptions of the side-effects of chemotherapy: the influence of 5HT3 antagonists. 937 66


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