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)

Fundamental approaches in selection of new agents for evaluation in prevention of space/motion sickness (SMS) are reviewed. The discussion centers on drugs under investigation at the Johnson Space Center. Methodology that employs the rotating chair for measuring SMS symptomatology and susceptibility is described. The most obvious approach to the development of new agents relies on selection of agents from drug classes that possess pharmacologic properties of established anti-motion sickness agents. A second approach selects drugs that are used to prevent emesis caused by means other than exposure to motion. The third approach relies on basic research that characterizes individual differences in susceptibility. The hypothesis is: detection of individual differences leads to identification of specific drugs, which target physiologic systems that show individual differences. These physiologic systems are targets for therapy and may play a role in the etiology of SMS. Two drugs that reduce susceptibility to SMS include dexamethasone and d(CH2)5Tyr(Me)AVP, a vasopressin (AVP)V1 antagonist. The latter peptide has demonstrated complete blockade of emesis and other significant symptoms in squirrel monkeys. These studies were predicated on observations that subjects who were more resistant to SMS had higher plasma AVP after severe nausea than subjects with lower resistances. Investigations are underway to test a 0.5-mg intravenous dose in humans. Kappa opioid agonists inhibit AVP release and offer new therapeutic possibilities and advantages over AVP peptides. This review details the experimental data collected on AVP and adrenocorticotropin. The literature supports interrelated roles for AVP and opioid peptides in SMS. Experimental testing of kappa agonists is warranted because specific opioid agonists act at neuroanatomical sites causing nausea and vomiting. It is argued opioid receptors in the chemoreceptor trigger zone and vomiting center stimulate and inhibit the emetic response, respectively. The evidence suggests kappa and/or mu receptors at VC are involved in inhibition of emesis, whereas delta opioid receptors at CTZ are involved in stimulation of emesis.
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PMID:New pharmacologic approaches to the prevention of space/motion sickness. 166 31

Despite excellent control of acute-stage emesis, some patients are still bothered by delayed emesis occurring more than 24 hours after cisplatin administration. We report 19 patients with 61 courses of cisplatin-based chemotherapy. They all received high-dose metoclopramide, dexamethasone and lorazepam on the day of cisplatin treatment. After 24 hours, they were treated with intravenous dexamethasone 8 mg once and metoclopramide 50 mg twice on day 2, and oral metoclopramide 10 mg qid on days 3-5. Delayed vomiting and nausea were noted in 27.9% and 39.4% respectively, as compared with 69.8% of delayed emesis and 79.4% of delayed nausea in 63 courses of 15 patients without receiving any antiemetics on days 2-5. The statistics showed significant difference (both P less than 0.001). Side effects were mild and acceptable. Therefore, this regimen is highly effective in preventing delayed vomiting and nausea.
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PMID:[Control of cisplatin-induced delayed emesis]. 166 84

Dronabinol, delta-9-tetrahydrocannabinol in sesame oil, has been used for several years as an antiemetic for patients receiving cancer chemotherapy. In combination studies with prochlorperazine, enhancement of efficacy, as measured by duration of episodes of nausea and vomiting and by severity of nausea, has been found. The incidence of psychotropic effects from dronabinol appears to be decreased by concomitant administration of prochlorperazine. In open pilot studies, dronabinol caused weight gain in seven of ten patients with symptomatic HIV infection. In both HIV and cancer patients, dronabinol improved appetite at a dose which was well tolerated for chronic administration.
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PMID:Recent clinical experience with dronabinol. 166 30

Granisetron (BRL 43694) is a highly selective 5-HT3 receptor antagonist which possesses significant antiemetic activity, likely mediated through antagonism of 5-HT3 receptors on abdominal vagal afferents and possibly in or near the chemoreceptor trigger zone. Clinical trials in cancer patients demonstrate that, compared with placebo, granisetron significantly reduces the incidence of nausea and vomiting for 24 hours after administration of high-dose cisplatin. In large comparative trials, 70% of patients who received granisetron prior to cisplatin or other chemotherapy experienced complete inhibition of vomiting with little or no nausea for 24 hours after antineoplastic administration; these results were similar to those obtained with high-dose metoclopramide plus dexamethasone, and superior to a combination of chlorpromazine plus dexamethasone, or prochlorperazine plus dexamethasone, or methylprednisolone monotherapy. The most frequently reported adverse event associated with granisetron administration is headache which occurs in about 10 to 15% of patients while constipation, somnolence, diarrhoea and minor transient changes in blood pressure have been reported less frequently. Extrapyramidal effects, which can occur with high-dose metoclopramide and may be a limiting factor in its use, have not been noted with granisetron administration. Thus, granisetron is an effective, well tolerated and easily administered agent for the prophylaxis of nausea and vomiting induced by cancer chemotherapy which appears to be devoid of extrapyramidal side effects associated with metoclopramide. As a member of a new class of drugs, the selective 5-HT3 receptor antagonists, granisetron provides the medical oncologist with a new, potentially more acceptable antiemetic therapy.
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PMID:Granisetron. A review of its pharmacological properties and therapeutic use as an antiemetic. 172 76

he safety and efficacy of oral transmucosal fentanyl citrate (OTFC) as a preanesthetic medication and the efficacy of droperidol as a prophylactic anti-emetic were evaluated in 100 children aged 2-8 yr undergoing general anesthesia for outpatient surgery. Patients were randomly assigned to one of four groups and managed in a double-blinded manner: 1) placebo lozenge 45 min preoperatively and placebo (normal saline) injected intravenously after induction of anesthesia; 2) placebo lozenge 45 min preoperatively and 50 micrograms/kg droperidol intravenously after induction; 3) 15-20 micrograms/kg OTFC lozenge 45 min preoperatively and placebo intravenously after induction; and 4) 15-20 micrograms/kg OTFC lozenge 45 min preoperatively and droperidol 50 micrograms/kg intravenously after induction. Anesthesia was induced and maintained with halothane and nitrous oxide in oxygen. Heart rate, respiratory rate, blood pressure, and hemoglobin oxygen saturation (SpO2) were monitored throughout the study. Scoring systems were used to evaluate sedation, anxiety, cooperation, and ease and quality of anesthetic induction. Emergence, recovery, and discharge times were recorded. Nausea, vomiting, and adverse effects were noted. Preoperatively, children receiving OTFC had significantly greater sedation, slower respiratory rates, lower SpO2, and less excitement during induction. Postoperative nausea and vomiting occurred significantly more frequently after OTFC than after placebo. Prophylactic droperidol did not significantly reduce the incidence of nausea and vomiting. The authors conclude that, in pediatric surgical outpatients, OTFC reliably induces preoperative sedation and facilitates inhalation induction of anesthesia, but it is associated with significant decreases in respiratory rate and SpO2 and a high incidence of postoperative nausea and vomiting that is not significantly reduced by prophylactic droperidol.
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PMID:Oral transmucosal fentanyl citrate for preanesthetic medication of pediatric day surgery patients with and without droperidol as a prophylactic anti-emetic. 172 35

Cytotoxic chemotherapy can induce acute, delayed and anticipatory nausea and vomiting. The efficacy and toxicity data of the available anti-emetics and their role in chemotherapy-induced emesis are reviewed. Moreover, some pitfalls in the methodology of anti-emetic trials as well as factors known to affect the individual sensitivity of patients for the emetic challenge are illustrated. So far, high-dose metoclopramide (3-6 mg.kg-1.d-1) was the most effective single agent in the control of acute emesis. However, extrapyramidal reactions caused by its dopamine antagonism remained a major drawback. The addition of dexamethasone and/or lorazepam decreases the incidence of extrapyramidal reactions, and further improves anti-emetic control. In animals, serotonin type 3 receptor antagonists have demonstrated promising anti-emetic results against chemotherapy-induced and radiotherapy-induced emesis; the results of clinical studies are awaited. Delayed nausea and vomiting have not been studied as extensively. At present, the combination of metoclopramide and dexamethasone offers an optimal protection in approximately 50% of patients on cisplatin chemotherapy. Anticipatory nausea and emesis remain major problems, and an effective pharmacological treatment is lacking. Attempts to control this type of emesis focus on drugs with amnesic properties and on behaviour therapy.
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PMID:Controlling cancer chemotherapy-induced emesis. An update. 174 7

Cefprozil is a new oral semi-synthetic cephalosporin with broad antibacterial spectrum and prolonged serum elimination half-life. In vitro, cefprozil demonstrates excellent activity against common urinary tract pathogens such as Escherichia coli and Klebsiella pneumoniae. Cefprozil, 500 mg once a day, was compared to cefaclor, 250 mg three times a day, in an open, randomized, comparative, clinical trial for the treatment of acute, uncomplicated, urinary tract infection. One hundred and two adult patients were eligible for safety evaluation; four patients were excluded due to side-effects (abdominal discomfort, nausea and vomiting). Ninety-eight patients were eligible for evaluation of efficacy. Clinical and bacteriological responses were comparable for both antibiotics. Leucopenia, nausea, and vaginal yeast infections were slightly more common in the cefprozil group. Cefprozil, 500 mg once daily, appears to be an appropriate alternative for the treatment of acute, uncomplicated urinary tract infections.
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PMID:Comparative efficacy and safety of cefprozil and cefaclor in the treatment of acute uncomplicated urinary tract infections. 176 53

Nausea and vomiting are frequent side-effects of intravenous cancer chemotherapy. How these complications were related to the gastric mucosal function was investigated by measuring the gastric mucosal potential difference (PD). Eight patients with metastatic breast cancer receiving chemotherapy were investigated. The liquid junction-corrected gastric PD and pH were measured with a newly developed microelectrode. The measurements started half an hour before chemotherapy and continued for 4-5 hours. Nausea, vomiting, psychological stress and sleeping episodes were registered. The initial PD values were -34 mV +/- 8 mV (mean +/- SD). During the observation period 6 of 8 patients had one or more episodes of nausea and vomiting. All episodes were preceded by a significant decline in PD. The magnitude of the decline in PD was unrelated to the time-lag between administration of chemotherapy and the occurrence of nausea and vomiting, and there was no correlation between the time for these episodes and the time for the administration of the chemotherapy. One patient had three episodes of severe psychological stress causing a marked decline in PD. The last patient experienced no nausea, vomiting or stress and had no changes in PD. During sleeping periods PD increased significantly.
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PMID:Changes in the gastric potential difference during chemotherapy in patients with metastatic breast cancer. 176 71

The efficacy of methylprednisolone (MP) (500 or 250 mg) or droperidol 2.5 mg administered i.v., was studied in 200 women undergoing major gynaecological surgery. Following a standardised general anaesthesia technique with intrathecal morphine, the incidence of nausea and vomiting was assessed. The frequency of postoperative nausea and vomiting in the non-treated group was 59% and 35%; the group of MP 500 mg has a significant reduction of nausea and vomiting to 21% and 13%. Droperidol 2.5 mg decreased the incidence of postoperative nausea alone (nausea: 36%, vomiting: 19%). MP 250 mg was not effective in reducing either nausea or vomiting (nausea: 44%, vomiting: 38%). It was concluded that, of the drugs studied, MP 500 mg was most effective in preventing nausea and vomiting after major gynaecological surgery.
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PMID:[Comparison of methylprednisolone and droperidol in the prevention of nausea and vomiting following major gynaecological surgery]. 176 10

Fifty-four patients with advanced malignancies were treated on this phase I trial of coumarin and cimetidine. The dose of coumarin was escalated, with three patients treated at each dose level, while the cimetidine dose was held constant at 300 mg four times daily. Patients received coumarin alone as a single daily oral dose for 14 days; on day 15, cimetidine was added and both drugs were continued until progression of disease. This trial was initiated with patients receiving coumarin at 400 mg daily and closed at 7 g daily with four of five patients on this dose experiencing nausea and vomiting. Treatment was generally well tolerated over a wide range of coumarin doses. Symptomatic side effects were few, mild, and usually self limited. Side effects included insomnia, nausea, vomiting, diarrhea, and dizziness. Two patients withdrew from therapy because of daily nausea and vomiting. Typically, nausea, vomiting, and dizziness occurred 2.5-3 hours after a dose of coumarin. In most patients, these side effects abated spontaneously with continuation of therapy. There was no significant hematologic or renal toxicity. Hepatotoxicity occurred in only one patient and was manifested by asymptomatic abnormal elevations of serum hepatic transaminases. This toxicity was reversible upon interruption of therapy. Objective tumor regressions were observed in six patients with renal cell carcinoma. Responses occurred at coumarin doses ranging from 600 mg to 5 g daily. Coumarin is a relatively nontoxic, oral, outpatient therapy that warrants further investigations for the treatment of human malignancies. Because of its low toxicity, there is potential for combining coumarin with chemotherapeutic and/or biological agents in an attempt to improve on efficacy.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Phase I evaluation of coumarin (1,2-benzopyrone) and cimetidine in patients with advanced malignancies. 176 68


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