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At least 163 records · Page 9Linked to original sources
PubMed1992

[Anti-emetic effect and safety of consecutive use of ondansetron injection in cisplatin-induced nausea and emesis].

Anti-emetic effect, safety and clinical usefulness of Ondansetron injection given in the dose of 4 mg once daily by intravenous administration for 3-5 consecutive days were examined in patients receiving a high single dose (not less than 50 mg/m2 or over 75 mg/body) and lower multiple doses (over 15-20 mg/m2 once daily, for 3-5 consecutive days) of cisplatin. Efficacy rates of inhibitory effects on nausea and emesis in patients receiving the high single dose of cisplatin were 76% on the 1st day, 67% on the 2nd day and 78% on the 3rd day, the average being 71% (86/121 cases) for the 3 days. Those in patients receiving lower multiple doses of cisplatin were 83% on the 1st day, 78% on the 2nd day, 61% on the 3rd day, 65% on the 4th day and 57% on the 5th day, the average being 72% (13/18 cases) for the 3-5 days. Side effects were observed in 15 cases out of 207 (1st course, 182 cases; 2nd course, 21 cases; 3rd course, 4 cases), and major symptoms were headache and fever. Also, abnormalities in clinical laboratory findings attributable to Ondansetron were observed in 13 cases, mainly consisting of elevation of the hepatic function values. From the above, Ondansetron injection which showed sufficient anti-emetic effects on acute emesis and delayed emesis induced by a high single dose or lower multiple doses of cisplatin with its once daily intravenous dose given for 3-5 consecutive days, were considered a safe and clinically useful anti-emetic.

Aged↗
PubMed1991

Nausea and vomiting after termination of pregnancy as day surgery cases: comparison of 3 different doses of droperidol and metoclopramide as anti-emetic prophylaxis.

Frequency of nausea and vomiting following day case termination of pregnancy was found to be rather high (42%) without anti-emetic prophylaxis. Droperidol in doses of 2.5 mg, 1.25 mg and 0.25 mg were found to be equally effective as prophylactic anti-emetic, but not metoclopramide 10 mg. This study confirms that low dose droperidol 0.25 mg is effective as a prophylactic anti-emetic, without any delay in immediate recovery and hence suitable for day surgery cases.

Abortion, Induced↗
PubMed1991

Methodology in anti-emetic trials.

Major progress in the ability to control chemotherapy-induced emesis has been made over the past 10 years. One of the several factors contributing to this improved control has been the development of accurate assessment methodology. The application of proper study methodology fostered the identification of active single agents and led to the formation of effective anti-emetic combinations. In this communication, important areas in anti-emetic study evaluation will be outlined. Proper methodology includes selection of agents or regimens that have a good rationale for study. Patient, chemotherapy, and anti-emetic factors must be controlled or standardised in good trial design, and the evaluation techniques for determining the amount of emesis or of nausea must be performed using reliable and valid methods. The statistical design employed and number of patients entered in the trial should be determined based on achievable and relevant goals.

Adult↗
PubMed1984

Evaluation of anti-emetics in association with intrathecal diamorphine.

Intrathecal diamorphine is associated with a high incidence of emetic symptoms. Six anti-emetic drugs representing various chemical groups were given in random order to patients undergoing total hip replacement and who had received intrathecal diamorphine 0.5-1.0 mg. The phenothiazines, perphenazine and prochlorperazine, were more effective than the others. It is suggested that this might be a useful model for the evaluation of new anti-emetics.

Aged↗
PubMed1983

Another function of the inner ear: facilitation of the emetic response to poisons.

If a foot were surgically removed and it was observed that walking was then impaired, it could be concluded that the foot is part of the normal mechanism for walking and that one of the physiological functions of the foot is to facilitate walking. In seven dogs, the vestibular apparatus of the inner ear was surgically removed and it was observed that the emetic response to certain poisons was impaired. It was concluded that the inner ear is part of the normal mechanism for vomiting in response to poisons, and that one of the physiological functions of the inner ear is to facilitate the emetic response to poisons. It seems likely that the mechanism, whereby the vestibular apparatus facilitates the emetic response to poisons, is the basis of motion sickness. In essence, motion sickness can be considered the result of activation, by motion, of a mechanism that normally functions to facilitate vomiting in response to poisons.

Animals↗
PubMed1993

[Combined use of ondansetron and other anti-emetics to control cisplatin-induced nausea and vomiting].

While ondansetron is effective in the control of nausea and vomiting induced by high dose cisplatin, it has to be given in multiple doses and is very expensive. We designed a regimen of combined use of a single dose of ondansetron and dexamethasone to control acute emesis and combined use of metoclopramide, diphenhydramine and valium to control delayed emesis. The results of this regimen was compared with that of the routine treatment regimen using metoclopramide plus diphenhydramine plus valium. A total of 43 patients were rolled in the cross-over study. Effective control of acute emesis was achieved in 93.6% of the patients with an average of 0.7 emetic episodes. In contrast, effective control of acute emesis was observed in only 18.2% of the patients with an average of 8.1 emetic episodes in those treated with the routine regimen. The regimen increased the emesis control rate by 7.6% and 42.7% on day 1 and 2, respectively as compared to that of repeated administrations of ondansetron alone. The regimen, though not as good as expected, was still better than the routine one for the control of delayed emesis. It deserves recommendation for its better anti-emetic efficacy and lower medical expenses.

Adult↗
PubMed1996

Production of an emetic toxin, cereulide, is associated with a specific class of Bacillus cereus.

The emetic toxin (cereulide) of Bacillus cereus was quantified in several isolates of B. cereus and in various food sources. When the emetic toxin was produced, vomiting-type food poisoning was observed in humans. We also found that the H-1 serovar phenotype was strongly associated with the production of cereulide and that none of the isolates that hydrolyzed starch or expressed diarrheal enterotoxin activity produced cereulide.

Bacillus cereus↗
PubMed1989

Development of a murine gastric distension model for testing the emetic potential of new drugs and efficacy of antiemetics.

A small animal model for emesis would allow preclinical testing of antiemetics and new drugs. Mice treated with cisplatinum develop stomachs distended with food. This effect is reduced by metoclopramide and parallels the gastric nausea experienced by patients receiving cisplatinum. To assess gastric distension as a more general model for paralleling the human emetic response, groups of five BALB/c mice were given intravenous nitrogen mustard, adriamycin, cyclophosphamide, 5-fluoruracil (5FU), vincristine and intraperitoneal DTIC at doses equivalent to those used clinically (mg/kg mouse = 12 X mg/kg per man). The mice were allowed free access to food pellets and water. At 48 h they were sacrificed and gastric distension quantitated as a ratio of average stomach to body weight. Significant gastric distension occurred with nitrogen mustard, DTIC, adriamycin and cyclophosphamide but not 5FU or vincristine. This parallels the emetic potential of these drugs in humans. Similarly cisplatinum was compared to its analogues, carboplatin and JM40 and produced gastric distension at lower doses than carboplatin. The model was then used to test the antiemetic efficacy of escalating doses of prochlorperazine against cisplatinum induced gastric distension in groups of 10 BALB/c mice. Doses ranged from 2.5 mg/kg. Only a high dose (19.2 mg/kg) significantly reduced the gastric distension. This parallels a clinical dose response relationship recently reported for prochlorperazine and suggests the further potential use of this model.

Animals↗
PubMed1985

Emetic effects of centrally administered angiotensin II, arginine vasopressin and neurotensin in the dog.

Short-latency emetic responses were induced in dogs by injecting angiotensin II (AII), arginine vasopressin (AVP), and neurotensin (NTN) into cerebroventricular (ICV) and cisternal (ICT) sites also responsive to the emetic effects of apomorphine (APO). Angiotensin III, bradykinin, bombesin, oxytocin, adrenocorticotropic hormone, substance P, gastrin-related peptide and cholecystokinin were ineffective. The results suggest a possible dopaminergic mediation of peptide-induced emesis by receptors in the area postrema (AP).

Angiotensin II↗
PubMedDate not supplied

Identification and characterization of the emetic effects of peptide YY.

Emesis was noted following intravenous bolus injections into dogs of a chromatographic subfraction derived from porcine small intestinal tissue extracts. The active agent was isolated from this subfraction using sequential ion-exchange and reverse-phase HPLC and demonstrated to be the recently identified regulatory peptide PYY. The threshold dose for PYY-induced emesis in the dog is less than 120 pmol/kg. Emesis was sometimes seen following large IV bolus doses of neuropeptide Y (NPY), but none was seen following IV injection of pancreatic polypeptide (PP). Dogs prepared with discrete, bilateral lesions of the area postrema were refractory to a suprathreshold emetic dose of PYY. PYY is the most potent, circulating emetic peptide identified to date.

Animals↗
PubMed1995

A novel dodecadepsipeptide, cereulide, is an emetic toxin of Bacillus cereus.

A vacuole-formation substance, cereulide of Bacillus cereus, is an emetic toxin in animals. Both oral administration and intraperitoneal injection of cereulide caused dose-dependent emesis in Suncus murinus, a new animal model of emesis. Vagotomy or a 5-HT3 receptor antagonist completely abolished this emetic effect. Therefore, cereulide causes emesis through the 5-HT3 receptor and stimulation of the vagus afferent. We also found that our purified cereulide caused swelling of mitochondria of HEp-2 cells.

Animals↗
PubMed1991

Interspecific variation in the emetic response of anurans.

1. The emetic response of seven species (four genera) of frogs to apomorphine hydrochloride, copper sulfate, antimonyl potassium tartrate and mechanical stimulation at the esophageal orifice was surveyed. Xenopus laevis and Rhacophorus schlegelii were more sensitive to systemically administered apomorphine than were the other species tested. 2. The sensitivity of Rana rugosa to apomorphine varied with the season. 3. All of the species showed vigorous vomiting behavior after the oral administration of either copper sulfate or antimonyl potassium tartrate. 4. Mechanical stimulation also induced vomiting in all species. Although the species differed in sensitivity to the different emetic stimulants, the adaptive significance of this interspecific variation is not known. 5. From the stand point of the mechanics for ejecting gastric contents, there is little difference between frogs and mammals. 6. Frogs, particularly Xenopus laevis, may be a useful non-mammalian model for studying emesis.

Animals↗
PubMed1998

Anti-emetic effects of a novel NK-1 receptor antagonist HSP-117 in ferrets.

We have developed a non-peptide compound, HSP-117, antagonist of the tachykinin NK-1 receptor. Binding of 3H-substance P (SP) to the membranes of IM-9 cells was inhibited by the antagonists HSP-117 and CP-99,994, the inhibitory activity of HSP-117 being about 50-fold that of CP-99,994. The SP-induced firing responses of single neuron activity in slices of the nucleus tractus solitarius of ferrets were inhibited by 10 microM HSP-117. Intracerebroventricular injection of HSP-117 significantly inhibited retching and vomiting induced by copper sulphate and morphine and the inhibitory effect of HSP-117 on emesis was greater than that of CP-99,994. These results indicate that (1) HSP-117 is a potent anti-emetic agent, blocking NK-1 receptors in the nucleus tractus solitarius and (2) NK-1 receptors in the nucleus tractus solitarius play an important role in emesis induced by broad-spectrum emetic stimuli.

Animals↗
PubMed1976

Nature of histamine receptors in the emetic chemoreceptor trigger zone.

1 The protective effects of the intracerebroventicular (i.c.v.) administration of the H1-receptor antagonist, mepyramine and the H2-receptor antagonists, burimamide and metiamide on centrally induced histamine-emesis were studied in unanaesthetized dogs. 2 The PD50 values of intraventricular mepyramine, burimamide and metiamide against the 100% emetic dose of histamine (3.0 mg i.c.v.) were found to be approximately 200 mug, 20 mug and 20 mug respectively. 3 Although burimamide (i.c.v. or i.v.) afforded protection against histamine-induced emesis, there was no protection against intravenous apomorphine-or oral copper sulphate-induced emesis. 4 The results suggest that both H1- and H2-histamine receptors in the emetic chemoreceptor trigger zone of the area postrema are concerned in histamine-induced emesis.

Animals↗
PubMed1991

5-HT3 receptor agonism may be responsible for the emetic effects of zacopride in the ferret.

The racemic 5-HT3 receptor antagonist, zacopride (10-100 micrograms kg-1, i.m.) evoked an emetic response in ferrets. This property appeared to reside totally in the S-enantiomer which also produced emesis over the same dose range. This emesis could be prevented by pretreatment with ondansetron (1 mg kg-1, i.m.) or by R-zacopride (100 micrograms kg-1, i.m.). In urethane-anaesthetized ferrets, S-zacopride (0.3 micrograms kg-1, i.v.) evoked a profound Bezold-Jarisch reflex which was blocked by both ondansetron (30 micrograms kg-1, i.v.) and by R-zacopride (100 micrograms kg-1, i.v.). These results suggest that, in the ferret, S-zacopride possesses 5-HT3 receptor agonist properties which may be responsible for the emetic effect. In contrast R-zacopride does not appear to possess 5-HT3 receptor agonist properties in this species.

Anesthesia↗
PubMed1992

Morphine 6-glucuronide: a metabolite of morphine with greater emetic potency than morphine in the ferret.

1. The emetic potencies of morphine and its metabolite morphine 6-glucuronide have been determined in the ferret by constructing dose-response curves for mean total retches and vomits for subcutaneous doses of 0.05 mg kg-1 to 5 mg kg-1. Morphine 6-glucuronide induced retching and vomiting at lower doses than morphine and at a maximal dose induced more retching and vomiting than morphine. 2. The emesis induced by both morphine and morphine 6-glucuronide was abolished by the preadministration of naloxone (0.5 mg kg-1 s.c.). 3. The 5-HT3 receptor antagonists granisetron and ondansetron (1 mg kg-1, s.c.) failed to abolish or reduce emesis induced by either compound. 4. At a high-dose (5 mg kg-1), morphine but not morphine 6-glucuronide failed to induce emesis and abolished the emesis induced by the cytotoxic drug, cyclophosphamide (200 mg kg-1, i.p.). 5. Preliminary pharmacokinetic studies of intravenous and subcutaneous morphine and morphine 6-glucuronide revealed that morphine 6-glucuronide accounts for less than 1% of the metabolic product of morphine in the ferret. Peak plasma levels of the two compounds after their subcutaneous administration were obtained within 10 min. The metabolic profile of morphine was not dose-dependent. There was no relationship between plasma level and emetic response for either compound.

Animals↗
PubMed1999

Semiautomated metabolic staining assay for Bacillus cereus emetic toxin.

This paper describes a specific, sensitive, semiautomated, and quantitative Hep-2 cell culture-based 3-(4,5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide assay for Bacillus cereus emetic toxin. Of nine Bacillus, Brevibacillus, and Paenibacillus species assessed for emetic toxin production, only B. cereus was cytotoxic.

Bacillus cereus↗
PubMed1976

[Intoxication after use of salt as an emetic (author's transl)].

Salt is generally contraindicated as an emetic in toxicological emergency situations. It can only be recommended when its rapid disappearance from the stomach can be guaranteed in the case of lack of vomiting. Less than 1 g salt per kg body weight may be lethal. The danger of sodium chloride becomes apparent from two severe cases of intoxication in children one of which was fatal. One of the two children was given salt as an emetic.

Child, Preschool↗