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At least 145 records · Page 8Linked to original sources
PubMed1979

Influence of the emetic reflex on vasopressin release in man.

The mechanisms underlying the frequent association of nausea and vomiting with elevations of plasma vasopressin(PAVP) were studied in man and rat. After oral water loads (N = 16), plasma osmolality fell in all human subjects and was associated with a decline in PAVP in 14 asymptomatic human subjects. In 2 human subjects, nausea occurred and was associated with increases in PAVP, without changes in blood pressure. During ethanol infusion (N = 28), PAVP was suppressed unless nausea supervened. In 4 nauseated human subjects, PAVP escaped from ethanol inhibition and rose to levels 10 times basal, despite the absence of hemodynamic changes. Apomorphine, a potent dopamine agonist and emetic agent, was administered to human volunteers in doses of 7 to 24 microgram/kg. There was no increase in PAVP in 3 human subjects who remained asymptomatic (7 to 16 microgram/kg). Ten human subjects experienced nausea after 16 microgram/kg, which was followed shortly by marked increases in PAVP. Emesis occurred in 5 human subjects given 16 to 24 microgram/kg, and was followed by PAVP levels similar to those seen with nausea alone. In 7 human subjects from the nausea group, the repeat study (16 microgram/kg) after pretreatment with dopamine antagonist (haloperidol, N = 4; fluphenazine, N = 3) resulted in complete blockage of apomorphine-induced AVP release. In rats, which lack an emetic reflex, apomorphine doses of 200 microgram/kg induced only slight increases in PAVP when compared to the response to 16 microgram/kg in man. These studies indicate that stimulation of the emetic reflex results in AVP-release in man. Nausea-mediated AVP release supervenes over concomitant osmolar or pharmacologic (ethanol) inhibition.

Alcohols↗
PubMed1998

Potent inhibition of both the acute and delayed emetic responses to cisplatin in piglets treated with GR205171, a novel highly selective tachykinin NK1 receptor antagonist.

The effects of GR205171, a selective tachykinin NK1 receptor antagonist, were investigated on both the acute and delayed phases of cisplatin-induced nausea-like behaviour and vomiting in the conscious piglet. Animals receiving cisplatin (5.5 mg kg(-1), i.v.) were observed for 60 h. Fifteen min prior to cisplatin infusion (T0(-15 min)), eight piglets acting as controls received an intravenous injection of saline solution (1 ml kg(-1)), whereas experimental animals received a single i.v. administration of GR205171 (1 ml kg(-1)) at a dose of 0.01 (n=8), 0.03 (n=8), 0.1 (n = 8), 0.3 (n = 16) or 1.0 (n = 13) mg kg(-1). In eight additional piglets, GR205171 (1 mg kg(-1)) was administered 15 min before the onset of the delayed phase (T16(-15 min)). A further five piglets received GR205171 (1 mg kg(-1)) every 6 h throughout the experiment. The latencies of the first emetic episode (EE) and nausea-like behavioural episode (NE) increased in all experimental groups treated at T0(-15 min), and the total number of both EE and NE during the 60 h was reduced in a dose-dependent manner. In piglets treated at T0(-15 min) with GR205171 1 mg kg(-1), eight out of 13 (62%) did not vomit throughout the experiment. Animals treated with GR205171 (1 mg kg(-1)) at T16(-15 min) exhibited an acute response to cisplatin but did not vomit during the delayed phase. The greatest inhibition of both nausea-like behaviour and vomiting was observed in piglets receiving multiple injections of GR205171. These results demonstrate the long-lasting anti-emetic effects of GR205171, and confirm the key role of substance P within the emetic reflex.

Animals↗
PubMed2001

The broad-spectrum anti-emetic activity of AS-8112, a novel dopamine D2, D3 and 5-HT3 receptors antagonist.

The anti-emetic and pharmacological profile of AS-8112 ((R)-5-bromo-N-(1-ethyl-4-methylhexahydro-1H-1,4-diazepin-6-yl)-2-methoxy-6-methylamino-3-pyridinecarboxamide.2 fumarate), a novel and potent dopamine D2, D3 and 5-hydroxytryptamine-3 (5-HT3) receptors ligand, was investigated in the present study. In guinea-pig isolated colon, AS-8112 produced a rightward shift of the concentration-response curves of 2-methyl-5HT, a 5-HT3 receptor agonist (pA2 value of 7.04). Other 5-HT3 receptor antagonists also produced such a shift in the following antagonistic-potency order: granisetron> ondansetron=AS-8112>>metoclopramide. In mice, AS-8112 (1.0 - 3.0 mg kg(-1) s.c.) potently inhibited hypothermia induced by the dopamine D3 receptor agonist; R(+)-7-OH-DPAT (R(+)-7-hydroxy-2-(N,N-di-n-propylamino)tetraline) (0.3 mg kg(-1) s.c.). Domperidone and haloperidol, which have affinity for dopamine D3 receptor, also inhibited R(+)-7-OH-DPAT-induced hypothermia. In ferrets or dogs, AS-8112 dose-dependently inhibited emesis induced by R(+)-7-OH-DPAT, apomorphine, morphine or cisplatin with ID50 values of 2.22 microg kg(-1) s.c., 10.5 microg kg(-1) s.c., 14.2 microg kg(-1) i.v. and 17.6 microg kg(-1) i.v., respectively. Moreover, oral administration of AS-8112 significantly inhibited emesis induced by these emetogens. AS-8112 (0.3 mg kg(-1) i.v.) significantly inhibited emesis induced by cyclophosphamide and doxorubicin. In conclusion, AS-8112 is a potent dopamine D2, D3 and 5-HT3 receptors antagonist, and a novel anti-emetic agent with a broad-spectrum of anti-emetic activity. These results suggest that this compound is worthy of clinical investigation.

Animals↗
PubMed1999

Comparison of anti-emetic effects of ondansetron, metoclopromide or a combination of both in children undergoing surgery for strabismus.

This prospective, randomized and double-blinded study was designed to evaluate the anti-emetic efficacy of a combination of ondansetron and metoclopramide in 100 ASA physical status I and II children of either sex and 1-15 years of age undergoing elective surgery for strabismus. A standardized anaesthetic technique and post-operative analgesia were used for all the children. Children were divided into four groups. They received saline, metoclopromide 250 micrograms kg-1, ondansetron 150 micrograms kg-1 or a combination of metoclopramide 150 micrograms kg-1 and ondansetron 100 micrograms kg-1 intravenously immediately after the insertion of an intravenous cannulae. There were no differences between the groups in their age, gender, weight, duration of surgery, number of muscles subjected to surgery or intravenous fluids received. In the first 24 post-operative hours, 18 (72%) patients in the placebo group, 15 (60%) patients in the metoclopramide group, 10 (40%) patients in the ondansetron group and 11 (44%) patients in the combination group had nausea or vomiting. The overall incidence of post-operative nausea and vomiting was significantly (P < 0.05) lower in the combination group and in the ondansetron group compared with the placebo group. Nine (36%) patients in both the placebo and the metoclopramide groups and one (4%) patient in the ondansetron group required rescue anti-emetic treatment. None of the patients in the combination group required rescue anti-emetic and this was significantly less (P < 0.01) when compared with the placebo and the metoclopramide groups. Recovery and sedation scores were comparable in all the four groups. A combination of metoclopramide 150 micrograms kg-1 and ondansetron 100 micrograms kg-1 administered prior to surgery was not found to be more effective than ondansetron 150 micrograms kg-1 alone for the prophylaxis of nausea and vomiting following surgical repair of strabismus in paediatric patients.

Adolescent↗
PubMed1995

Anti-emetic principles of Poria cocos.

The triterpenes isolated from P. cocos and their derivatives were examined for anti-emetic activity. Some of these triterpenes inhibited emetic action induced by oral administration of copper sulfate pentahydrate to leopard frog. The triterpenes having an exomethylene group at C-24 showed anti-emetic activity to frogs.

Animals↗
PubMed1994

Anti-emetic principles of Magnolia obovata bark and Zingiber officinale rhizome.

Magnolol and honokiol, biphenyl compounds, were isolated as anti-emetic principles from the methanolic extract of Magnolia obovata bark. [6]-, [8]-, and [10]-shogaols and [6]-, [8]-, and [10]-gingerols were isolated from the methanolic extract of Zingiber officinale rhizome as anti-emetic principles. Some phenyl-propanoids with allyl side-chains were found to show the same activity. They inhibited the emetic action induced by the oral administration of copper sulfate pentahydrate to leopard and ranid frogs.

Animals↗
PubMed1999

Novel experimental model using free radical-induced emesis for surveying anti-emetic compounds from natural sources.

A novel experimental model of free radical-induced emesis for screening anti-emetic compounds from natural sources was established. 2,2'-Azobis(2-amidinopropane) dihydrochloride (AAPH) dissolved in liposome induced emesis in young chickens, and the emesis was prevented by antioxidants including N-(2-mercaptopropionyl)-glycine (MPG), alpha-tocopherol, and L-ascorbic acid. Tropiseton, a serotonin receptor antagonist, also prevented emesis induced by AAPH. Known anti-emetic drugs and anti-emetic principles from natural sources also showed significant retching inhibition in the experiment using this system.

Amidines↗
PubMed1997

Fulminant liver failure in association with the emetic toxin of Bacillus cereus.

BACKGROUND: A 17-year-old boy and his father had acute gastroenteritis after eating spaghetti and pesto that had been prepared four days earlier. Within two days, fulminant liver failure and rhabdomyolysis developed in the boy and he died. The father had hyperbilirubinemia and rhabdomyolysis but recovered. We investigated the cause of these illnesses. METHODS: Bacteria were isolated and characterized by conventional methods, and bacterial toxins were quantified by immunoassays and cell-culture techniques. The effect of the isolated toxin on the rates of oxidation of various substrates was analyzed in rat-liver mitochondria. RESULTS: Autopsy of the boy's liver revealed diffuse microvesicular steatosis and midzonal necrosis that suggested impaired beta-oxidation of liver mitochondria due to a mitochondrial toxin. There was no evidence of ingestion of heavy metals, halogenated compounds, hepatotoxic drugs, or staphylococcal enterotoxin. However, high concentrations of Bacillus cereus emetic toxin were found in both the residue from the pan used to reheat the food and the boy's liver and bile. B. cereus was cultured from the intestinal contents and the pan residue. The emetic toxin isolated from the B. cereus cultures was found to be a mitochondrial toxin. CONCLUSIONS: Fulminant liver failure developed after the ingestion of food contaminated with the B. cereus emetic toxin. The toxin inhibits hepatic mitochondrial fatty-acid oxidation, indicating that it caused liver failure in this patient.

Adolescent↗
PubMed2005

Quantitative analysis of cereulide, an emetic toxin of Bacillus cereus, by using rat liver mitochondria.

An emetic toxin cereulide, produced by Bacillus cereus, causes emetic food poisonings, but a method for quantitative measurement of cereulide has not been well established. A current detection method is a bioassay method using the HEp-2 cell vacuolation test, but it was unable to measure an accurate concentration. We established a quantitative assay for cereulide based on its mitochondrial respiratory uncoupling activity. The oxygen consumption in a reaction medium containing rat liver mitochondria was rapid in the presence of cereulide. Thus uncoupling effect of cereulide on mitochondrial respiration was similar to those of uncouplers 2,4-dinitrophenol (DNP), carbonylcyanide m-chlorophenylhydrazone (CCCP), and valinomycin. This method gave constant results over a wide range of cereulide concentrations, ranging from 0.05 to 100 microg/ml. The minimum cereulide concentration to detect uncoupled oxygen consumption was 50 ng/ml and increased dose-dependently to the maximum level. Semi-log relationship between the oxygen consumption rate and the cereulide concentration enables this method to quantify cereulide. The results of this method were highly reproducible as compared with the HEp-2 cell vacuolation test and were in good agreement with those of the HEp-2 cell vacuolation test. The enterotoxin of B. cereus or Staphylococcus aureus did not show any effect on the oxygen consumption, indicating this method is specific for the identification of cereulide as a causative agent of emetic food poisonings.

2,4-Dinitrophenol↗
PubMed1981

Emetic action of xylazine on the chemoreceptor trigger zone for vomiting in cats.

Xylazine is an effective sedative analgesic that induces vomiting in the cat. A consistently effective intramuscular emetic dose of xylazine was established in normal cats in this laboratory. Animals in which the area postrema of the medulla oblongata had been chronically destroyed did not exhibit emesis in response to the standard test dose of xylazine but continued to show sedation. By contrast, sham-operated cats responded normally. Refractoriness to deslanoside, a known specific emetic drug, was used as functional proof for successful ablation of area postrema, and the lesions were also validated histologically. We conclude that xylazine exerts its emetic action on the chemoreceptor trigger zone of the area postrema. It is suggested that this action may be mediated by an opiate type of molecular receptors.

Animals↗
PubMed2006

Efficacy and efficiency of gastric electrical stimulation with short pulses in the treatment of vasopressin-induced emetic responses in dogs.

The aim of this study was to determine the most effective and efficient anti-emetic parameters of short-pulse gastric electrical stimulation (GES) in dogs. Seven female beagle dogs implanted with four pairs of gastric electrodes were studied in eight randomized sessions (saline, vasopressin, and six GES sessions with different parameters). Each session consisted of four 20-min recordings of gastric slow waves and symptoms. In sessions 1 and 2, saline and vasopressin, respectively, were infused during the second 20-min period. The protocol of the other six sessions was the same as session 2 except that GES was continuously applied. It was found that: (1) vasopressin induced gastric dysrhythmia and emetic response (P < 0.01, anova); (2) short-pulse GES with a frequency of 14 or 40 Hz and pulse width of 0.1 or 0.3 ms, but not 0.6 ms was able to reduce symptoms induced by vasopressin; (3) short-pulse GES with a pulse width of 0.3 ms was the most effective in preventing vasopressin-induced symptoms; (4) none of the tested GES methods improved vasopressin-induced gastric dysrhythmia. We conclude that vasopressin induces gastric dysrhythmia and symptoms. Short-pulse GES with a pulse width of 0.3 ms and frequency of 14 Hz is most effective and efficient in preventing vasopressin-induced emetic responses in dogs.

Animals↗
PubMed2007

Patients' willingness to pay for anti-emetic treatment.

BACKGROUND: Post-operative nausea and vomiting (PONV) is a common complication of anaesthesia. This study was conducted in 100 German and 100 Turkish patients scheduled for elective surgery under general anaesthesia to assess the amount patients were willing to pay for an anti-emetic that completely prevented PONV. METHODS: Post-operatively, using Dixon's up and down method, patients completed an interactive computer questionnaire with a random starting point to determine how much of their own money they were willing to pay for a totally effective anti-emetic treatment. RESULTS: On average, participants were willing to pay 65 euro in Germany and 68 euro in Turkey to avoid PONV. However, patients who actually experienced PONV were willing to pay larger amounts: 96 euro in Germany and 99 euro in Turkey. The amount patients were willing to pay was related to female sex, history of motion sickness, non-smoking status and better education. CONCLUSIONS: Despite differences in political and cultural origin, health care system and financial background, the amount patients were willing to pay for an effective anti-emetic was similar in both Germany and Turkey to that reported previously for the USA.

Adult↗
PubMed1994

An improved method for detecting cytostatic toxin (emetic toxin) of Bacillus cereus and its application to food samples.

We developed an improved HEp-2 cell assay method for the detection of Bacillus cereus toxin, which affects the proliferation of HEp-2 cells. The cytostatic toxin was stable upon exposure to heat, pH 2, pH 11 and trypsin, which suggests it is an emetic. Using the HEp-2 cell assay, we examined the distribution and contamination of B. cereus strains that produced an emetic toxin in various foods. Although there were 228 enterotoxin producers among 310 B. cereus strains obtained from foods, 16 of them produced the cytostatic type (emetic toxin). All of the strains that produced the cytostatic toxin were of the H.1 serotype.

Bacillus cereus↗
PubMed1993

Postoperative nausea and vomiting: a comparison of anti-emetic drugs used alone or in combination.

Drugs with anti-emetic properties can exert their actions at more than one receptor site, histamine H1, muscarinic cholinergic or dopaminergic D2 receptors. This study was designed to test the hypothesis that a combination of drugs acting at different receptor sites in lower than standard doses would be at least as effective as a standard therapeutic dose of a single anti-emetic agent. A combination of droperidol, hyoscine and metoclopramide in subtherapeutic doses has been shown to be at least as effective as droperidol (1.25 mg) alone. In both groups there was a low incidence of emetic sequelae in the first 3 hours postoperatively.

Adult↗
PubMed1994

Propofol for ambulatory gynecologic laparoscopy: does omission of nitrous oxide alter postoperative emetic sequelae and recovery?

The role of nitrous oxide in postoperative emesis is controversial. This prospective randomized study was performed to compare the emetic sequelae and quality of recovery between a group of patients anesthetized with propofol alone and a group anesthetized with propofol plus nitrous oxide. Seventy patients, ASA grade I or II, scheduled for ambulatory gynecologic laparoscopy under general anesthesia were included. Most factors which could influence the incidence of postoperative emesis were controlled. The overall incidence of emetic sequelae during the first 24 h postoperatively was 25% in the group anesthetized with propofol alone versus 29% for the group anesthetized with propofol and nitrous oxide. The incidence of emetic sequelae requiring therapeutic intervention was 13% and 6%, respectively. This difference was not statistically significant. The group of patients who received propofol alone required an average propofol dose of 221.5 +/- 71.9 micrograms.kg-1.min-1 to maintain anesthesia compared with 162.5 +/- 43.9 micrograms.kg-1.min-1 for the group receiving propofol plus nitrous oxide (P < 0.001). The time from discontinuation of propofol to eye-opening and orientation was significantly longer in patients anesthetized with propofol alone. Otherwise, the recovery variables were comparable between the two groups. We conclude that supplementing propofol with nitrous oxide in patients undergoing ambulatory laparoscopy reduces the requirements of propofol, expedites immediate recovery (emergence), and does not increase the incidence of postoperative emesis. This tends to confirm that there is no clinical advantage to omitting nitrous oxide.

Adult↗
PubMed2005

Comparative clinical study of the anti-emetic effects of oral ramosetron and injected granisetron in patients with malignant glioma undergoing ACNU chemotherapy.

The effectiveness of ramosetron tablets and granisetron injection was compared for reducing the frequency of nausea, vomiting, and anorexia in patients with malignant glioma undergoing ACNU chemotherapy. Patients with malignant glioma to be treated with ACNU chemotherapy were randomly assigned to receive oral ramosetron (20 patients) or intravenous granisetron (19 patients) prior to ACNU injection. Gastrointestinal toxicity within 48 hours of ACNU injection was compared to that in patients who had received ACNU chemotherapy with dopamine D2 receptor-blocker as a historical control group. Within 24 hours of the administration of ACNU, 15 of the 20 patients treated with ramosetron and 16 of the 19 treated with granisetron were nausea-free, and 14 of the former and 14 of the latter regained their normal appetite. There was no significant difference in the anti-emetic effects. Ten of the 17 controls experienced no vomiting within 6 hours of the injection of ACNU, five were nausea-free within 24 hours, and two retained their normal appetite within 24 hours. Oral ramosetron has the same anti-anorectic and anti-emetic effects as intravenous granisetron. Ramosetron tablets are less expensive and are easy to take, so should be on the list of first-choice anti-emetic drugs for patients treated with ACNU chemotherapy.

Adult↗
PubMed1978

Mechanism of action of bilharcid and tartar-emetic.

An investigation on the mechanism of action of bilharcid and tartar-emetic produced the following results. Deoxyribonucleic acid (DNA) synthesis by cell of E. coli B from either the maximum stationary phase or the exponential phase are inhibited by 3.62 mM of bilharcid or 16.81 mM of tartar-emetic immediately upon addition of the inhibitor. These drugs cause a downshift of the Tm of native DNA. They displace MG from the DNA-MG complex. They increase the specific viscosity of DNA solution. Also the synthesis of constitutive enzyme (alkaline phosphatase) was stopped, as was the induction of the synthesis of new enzyme (beta-galactosidase). Bilharcid and tartar-emetic act primarily on cell membrane and cause the release of 260 mM absorbing substances from E. coli B. Moreover, they lyse not only protoplasts of B. subtilis, but also spheroplasts of E. coli B.

Alkaline Phosphatase↗
PubMed2002

[Anti-emetic effects of ondansetron hydrochloride throughout courses of cytotoxic chemotherapy].

Since the emesis induced by cytotoxic drugs is intractable, and is a possible determinant of a patient's QOL during chemotherapy, the control of this adverse event is essential to complete a course of cancer chemotherapy. The anti-emetic effects of a 5-HT3 antagonist, ondansetron hydrochloride (OND), was evaluated during a course of CDDP-containing chemotherapy. Forty-eight patients with gynecologic carcinoma, respiratory malignancy, or urological cancer were followed throughout their treatment courses. For acute emesis, prophylactic OND was given intravenously before CDDP administration, and OND tablets were used for 4 days from the day following CDDP administration as a measure against delayed emesis. The efficacy of OND gradually decreased for the acute emesis (1st course: 73.8%, 2nd course: 62.8% and 3rd course: 56.7%). The efficacy, however, did not decrease against the delayed emesis. Of patients with a good response, "effective" or "highly effective", in the previous treatment course, over 80% could again obtain a good response in the next treatment course. Adverse events of this anti-emetic treatment were not observed except for mild leukocytosis in one case, and this unexplainable effect abated without any specific treatments. In conclusion, the anti-emetic effects of OND sufficiently prevented the emetogenic action of CDDP throughout the treatment course, with a special importance for successful control in the first treatment course. The additional use of corticosteroid might enhance the effects of OND for female patients.

Administration, Oral↗