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PubMed1986

Droperidol, alizapride and metoclopramide in the prevention and treatment of post-operative emetic sequelae.

Women (182) undergoing elective orthopaedic surgery under general anaesthesia received 100 or 200 mg alizapride, 1.25 mg droperidol, 20 mg metoclopramide or a saline placebo intravenously 5-10 min before the end of anaesthesia in a double-blind random fashion to prevent post-operative nausea and vomiting. Administration of the same anti-emetic was repeated during 24 h post-operatively if the patient complained of nausea or retched or vomited. Significantly fewer patients given any of the anti-emetics prophylactically were nauseated or vomited in comparison with patients given saline. The incidence of nausea and vomiting in the saline group was 83%, while in those patients who received an anti-emetic it was as follows: droperidol 35% (P less than 0.001 vs. saline), alizapride, 100 mg 46% (P less than 0.01), alizapride 200 mg 53% (P less than 0.05) and metoclopramide 58% (P less than 0.05). The number of patients needing an additional dose of the same substance in the post-operative period was significantly higher in the saline group (67%) than in the groups which had received droperidol (32%, P less than 0.01) and alizapride 100 mg (37%, P less than 0.05) or 200 mg (33%, P less than 0.05). The patients who received metoclopramide, however, did not differ statistically from the saline group in the treatment of nausea and vomiting. It is concluded that droperidol was the most effective, and metoclopramide the least effective, anti-emetic in this study.

Adolescent↗
PubMed1983

Levonantradol: a synthetic cannabinoid in the treatment of severe chemotherapy-induced nausea and vomiting resistant to conventional anti-emetic therapy.

Twenty-three patients with severe nausea and vomiting refractory to conventional anti-emetic therapy were entered into an open phase II study of levonantradol. Of 22 patients evaluable for response, three achieved complete relief from nausea and vomiting, seven obtained very good relief from nausea and vomiting, four obtained a partial reduction in nausea and vomiting, and eight obtained no relief. However all patients experienced side effects including, in particular, drowsiness and thought disturbance, and as a result eight patients had to be withdrawn from the study. There was no statistical patient preference for levonantradol over previous anti-emetic treatment. Levonantradol is an effective anti-emetic in approximately 50% of patients resistant to conventional anti-emetics; however, its usefulness is likely to be restricted by side effects which are common and frequently unpleasant.

Adult↗
PubMed1990

Emetic activity of zacopride in ferrets and its antagonism by pharmacological agents.

Zacopride administered orally was more emetic in fed than in fasted ferrets. The emetic activity of zacopride (0.1 mg/kg p.o.) was inhibited (100%) by 0.1 mg/kg i.p. of zacopride and 1 mg/kg i.p. of ICS 205-930. Haloperidol (3.16 mg/kg i.p.) and prochlorperazine (3.16 mg/kg i.p.) were weakly effective. N-acetyl-5-hydroxytryptophyl-5-hydroxytryptophan amide, a 5-HT1P antagonist, was inactive. Thus, the emetic activity of zacopride, like that of cisplatin, is blocked by 5-HT3 receptor antagonists.

Animals↗
PubMed2004

Cereulide, the emetic toxin of Bacillus cereus, is putatively a product of nonribosomal peptide synthesis.

AIMS: To determine if cereulide, the emetic toxin produced by Bacillus cereus, is produced by a nonribosomal peptide synthetase (NRPS). METHODS AND RESULTS: NC Y, an emetic strain of Bacillus cereus, was examined for a NRPS gene using PCR with primers recognizing a fragment of a NRPS gene from the cyanobacterium Microcystis. The amplicon was sequenced and compared with other gene sequences using BLAST analysis, which showed that the amplicon from strain NC Y was similar in sequence to peptide synthetase genes in other micro-organisms, including Bacillus subtilis and B. brevis, while no such sequence was found in the complete genome sequence of a nonemetic strain of B. cereus. Specific PCR primers were then designed and used to screen 40 B. cereus isolates previously implicated in outbreaks of foodborne illness. The isolates were also screened for toxin production using the MTT cell cytotoxicity assay. PCR and MTT assay screening of the B. cereus isolates revealed a high correlation between the presence of the NRPS gene and cereulide production. CONCLUSIONS: The results indicate that cereulide is produced by a NRPS complex. SIGNIFICANCE AND IMPACT OF THE STUDY: This is the first study to provide evidence identifying the mechanism of production of cereulide, the emetic toxin of B. cereus. The PCR primers developed in the study allow determination of the potential for cereulide production among isolates of B. cereus.

Bacillus cereus↗
PubMed1992

Surgical and pharmacological dissociation of cardiovascular and emetic responses to intragastric CuSO4.

Under control (intact and laparotomized) conditions, arterial pressure of urethan-anesthetized ferrets rose significantly in response to intragastric copper sulfate (CuSO4; 10 ml of 5 mg/ml). CuSO4 was emetic 75-90% of the time, and a cardiovascular response always immediately preceded and accompanied emetic responses. The cardiovascular response was significantly reduced or abolished by hexamethonium (0.35 mg/kg) pretreatment combined with atropine methyl bromide (1 mg/kg). Addition of the alpha 2-receptor antagonist 2,3-dichloro-alpha-methylbenzylamine HCl (DCMB, 10 mg/kg) and the beta-receptor antagonist propranolol (3 mg/kg) to the hexamethonium and atropine combination prevented its reduction of the cardiovascular response. Given individually, these agents did not alter cardiovascular response, nor did yohimbine (0.30 mg/kg), RS(+/-)-zacopride (0.30 mg/kg), or granisetron (0.50 mg/kg). Only RS(+/-)-zacopride significantly reduced incidence of emesis. Atropine methyl bromide alone, with hexamethonium, or with hexamethonium, propranolol, and DCMB significantly delayed the first emetic episode. Conversely, bilateral abdominal vagotomy significantly reduced the number of vomiting animals without affecting cardiovascular response. These results suggest that the neural pathways mediating the two events are not identical. In another series of experiments, a significantly greater proportion of animals vomited in response to intragastric CuSO4 than to intraduodenal CuSO4, suggesting that the primary site of CuSO4 action in the ferret is the stomach.

Animals↗
PubMed1991

Comparison of cardiorenal and emetic effects of dopamine prodrugs docarpamine (TA-870) and levodopa in dogs.

Positive inotropic and renal vasodilatory effects of a novel dopamine prodrug, docarpamine, [N-(N-acetyl-L-methionyl)-3,4-bis(ethoxycarbonyl)dopamine; TA-870] and those of levodopa were compared in anesthetized dogs, and emetic effects of the two drugs were compared in conscious dogs. Intraduodenal administrations of docarpamine and levodopa at 20 mg/kg produced similar increases in cardiac contractility. The maximal increases in the left ventricular dP/dtmax after docarpamine and levodopa were 36.6 +/- 14.2 and 39.2 +/- 12.1%, respectively. The two drugs also produced similar decreases in renal vascular resistance (21.2 +/- 2.2 and 13.6 +/- 3.4%, respectively) and increases in renal blood flow (27.9 +/- 3.2 and 17.9 +/- 5.2%, respectively), however, the duration of renal vasodilation after docarpamine was longer than that of levodopa. Oral administration of the two drugs in conscious dogs produced vomiting. The ED50 value of the emetic effect for docarpamine was greater than 160 mg/kg, and that for levodopa was 11.0 mg/kg. The emesis was inhibited by pretreatment with a DA2 antagonist, domperidone. In conclusion, docarpamine and levodopa produced similar cardiorenal effects, but the emetic effect of docarpamine was much weaker than that of levodopa. Docarpamine can be used as a selective dopamine prodrug for the peripheral circulation.

Animals↗
PubMed1977

Syrup of ipecacuanha as an emetic in adults.

The emetic actions of syrup of ipecacuanha have been evaluated in 105 adult patients presenting at the emergency department of the Royal Perth Hospital with a diagnosis of accidental or intentional poisoning. The australian Pharmaceutical Formulary (APF) and the United States Pharmacopeia (USP) formulations of the syrup were compared and gave similar overall emetic responses of 88% and 89% respectively at a dose level of 15 ml. A 30 ml dose regimen of the APF formulation gave a slightly but not significantly increased overall emetic response of 96%. There were no differences between the three groups of patients in the time taken to vomit, the duration of vomiting or the volume of stomach contents recovered.

Adolescent↗
PubMed1992

Alpha adrenoceptor subtypes involved in the emetic action in dogs.

In order to assess the involvement of alpha-1 and alpha-2 adrenoceptors in emesis, the emetic effect of eight alpha agonists was studied in dogs. The i.m. administration of each agonist elicited dose-dependent emesis. The order of potency in inducing emesis was: clonidine greater than oxymetazoline greater than tramazoline greater than naphazoline greater than xylazine greater than epinephrine greater than methoxamine = phenylephrine. The clonidine-induced emesis was antagonized by adrenoceptor antagonists showing alpha-2 blocking activity, yohimbine, tolazoline and phentolamine. Among these antagonists, yohimbine was the most effective. The alpha-1 and beta adrenergic, cholinergic, dopaminergic, histaminergic, serotonergic and opioid receptor antagonists did not prevent the clonidine-induced emesis. The emesis induced by oxymetazoline, tramazoline, xylazine, naphazoline and epinephrine was also antagonized by a selective alpha-2 adrenoceptor antagonist, yohimbine, but not by a selective alpha-1 adrenoceptor antagonist, prazosin. In contrast, methoxamine and phenylephrine-induced emesis was antagonized by prazosin, but not by yohimbine. Neither yohimbine nor prazosin prevented the morphine- and histamine-induced emesis. These results indicate that alpha-2 adrenoceptors are involved in the mediation of emetic action, and that the alpha adrenoceptor-mediated emesis does not involve beta adrenergic, cholinergic, dopaminergic, histaminergic, serotonergic and opioid receptors in the emetic pathway. This study further suggests that alpha adrenoceptors involved in the emesis are mainly of the alpha-2 type, although the involvement of alpha-1 adrenoceptors cannot be ruled out.

Adrenergic alpha-Agonists↗
PubMed1985

Emetic effect of triazolopyrimidine, a pyrimidine compound, in dogs.

The intention of this study was to determine the minimum required dosage of triazolpyridine (TAP) to consistently induce emesis in canines. We administered single oral doses of TAP to 42 adult beagle dogs. The effect of TAP dosage on emesis was highly significant. The effective emetic dosages were 4.0 mg/10 ml water/animal (p less than 0.05) and 8.0 mg/10 ml water/animal (p less than 0.01). In all the dogs tested, 8.0 mg of TAP successfully induced emesis. The mean latency of emesis in the beagle group studied was 15 min, 54 sec (95% confidence limits = 8 min, 11 sec to 23 min, 38 sec). Intravenous apomorphine HCL was used to demonstrate the effectiveness of anti-emetic pretreatment with subcutaneous chlorpromazine (CPZ). Pretreatment with CPZ appeared to inhibit apomorphine-induced emesis, but did not modify the emetic response elicited by TAP. Emesis following the administration of TAP was considered a result of direct action of TAP upon the gastrointestinal mucosa. Eighty adult mongrel dogs were also given TAP doses of 8.0 mg/10 ml water/animal, with 100% effectiveness in inducing emesis.

Animals↗
PubMed1982

[Mechanism of the species characteristics of the sensitivity of monkeys and dogs to the emetic action of various pharmacological agents].

Monkey and dog sensitivity to the emetics that stimulate catecholamino- and serotoninoreactive structures of the chemoreceptor trigger zone (CTZ) of the vomiting center has been studied. It has been found that the monkeys are sensitive to the vomiting effect of serotonin agonists, while the dogs to the stimulants of the dopamino- and adrenoreceptors of the CTZ. At the same time both the monkeys and dogs are equally sensitive to the emetic action of sodium salicylate. The latter's effect has been shown to be realized via the serotoninergic structures of the CTZ in the monkeys, and via the adrenergic structures in the dogs. It is suggested that specific features of the monkey and dog responses to administration of central emetics are determined by the differences in the neurochemical structure of the CTZ, particularly by the prevalence of the serotonin- or catecholamine-containing neurons.

Animals↗
PubMed1994

Emetic reflex arc revealed by expression of the immediate-early gene c-fos in the cat.

The organization of the central neuronal circuitry that produces vomiting was explored by mapping the distribution of c-fos protein (Fos)-like immunoreactivity (FLI) as a monitor of functional activity. The brainstem and spinal cord were examined in cats administered multiple emetic drugs (cisplatin, lobeline, protoveratrine, naloxone, apomorphine) or control saline injections. Some animals were decerebrated, paralyzed, and artificially ventilated to avoid possible Fos expression induced by sensory feedback or fluid depletion during vomiting. Fictive vomiting was identified in these animals by a characteristic pattern of respiratory muscle nerve (phrenic and abdominal) coactivation. Tissues were immunoprocessed using an antibody raised against amino acids 1-131 of Fos and the avidin-biotin peroxidase complex method. Enhanced nuclear FLI was observed in experimental animals along portions of the sensorimotor emetic reflex arc, including the nodose ganglia, area postrema, nuclei of the solitary tract (especially medial and subpostrema subnuclei), intermediate reticular zone of the lateral tegmental field, nucleus retroambiguus, C2 inspiratory propriospinal cell region, and dorsal vagal and phrenic motor nuclei. Enhanced FLI was also detected in the raphe magnus, subretrofacial nucleus, and spinal dorsal horn. Regions showing no recognizable differences in FLI between experimental and control animals included the vestibular, cochlear, spinal trigeminal, subtrigeminal, and lateral reticular nuclei. Only minor differences were observed in the distributions of FLI between intact and decerebrate animals. No unique, well-defined group of labeled neurons that might function as a "vomiting center" could be identified. Instead, the pattern of c-fos expression suggests that neurons involved in coordinating the emetic response may radiate from the area postrema and nucleus of the solitary tract to an arc in the lateral tegmental field implicated in somato-autonomic integration.

Animals↗
PubMed1993

Dose-related antagonism of the emetic effect of morphine by methylnaltrexone in dogs.

Opioids administered to produce analgesia cause unwanted emesis in patients (incidence 20%-30%, depending on situation). Tests in animals show that quaternary narcotic antagonists like methylnaltrexone (MNTX) do not affect the analgesic potency of morphine, but such compounds have not been examined for their potential to antagonize morphine-induced emesis. To determine the effects of MNTX on emetic response, we assigned 85 dogs to one of 11 groups challenged with morphine alone or morphine and various doses of MNTX IM or i.v. Antagonism of the emetic response was dose related: MNTX, 0.25 mg/kg IM or 0.2 mg/kg i.v., completely blocked the emetic effect of morphine in dogs for approximately 60 minutes. If morphine-induced emesis is mediated by receptors available to a quaternary antagonist (perhaps on the peripheral side of the blood-brain barrier), MNTX may prevent opioid-induced emesis. These data indicate that opioid-induced emesis might be prevented without affecting analgesia.

Animals↗
PubMed1990

A phase I/II study of the 5-HT3 antagonist GR38032F in the anti-emetic prophylaxis of patients receiving high-dose cisplatin chemotherapy.

A total of 24 patients who were receiving combination chemotherapy (POMB) including cisplatin at a dose of 100-120 mg/m2 were treated with the 5HT3 antagonist GR38032F (GR) as an anti-emetic prophylaxis. GR was given as a 15-min loading infusion followed by a 24-h infusion at three escalating dose levels of 1, 2 and 4 mg/h. In the first 24 h after commencing treatment, six patients had complete control of nausea and vomiting (CR), two had 1-2 emetic episodes (MR) and five had 3-5 emetic episodes (mR). The major response rate (CR + MR) was thus 35%. Eight responding patients (CR or MR) went on to receive oral GR at 8 or 12 mg t.i.d. for 5 days. In this group there was one CR, one MR, two mRs and four failures (F). There was no evidence of an improved therapeutic effect with increasing dose in either the infusion or the oral section of the study, although numbers were limited in the latter part of the trial. Toxicity was mild, with low-grade headache affecting 25% of patients being the most frequent side effect. Pharmacokinetic data was obtained in six patients at each dose level. There was a progressive rise in clearance with increasing dose, indicating that the kinetics are non-linear. However, there was no evidence of an association between high plasma levels and therapeutic efficacy. GR38032F is well tolerated and has promising single-agent activity in preventing vomiting induced by high-dose cisplatin.

Adult↗
PubMed2004

Emesis induced by low or minimal emetic risk chemotherapy.

For patients treated with low or minimally emetogenic chemotherapy there is little evidence from clinical trials supporting the choice of a given antiemetic therapy or of any treatment at all. The panel recognized the necessity of considering the introduction into clinical practice of new agents in these categories, particularly oral cytotoxic agents and targeted biological agents and also the possibility of over-treatment with antiemetics. There was consensus among panel members regarding the recommended treatment for patients receiving chemotherapy agents with low and minimal emetic risk. Patients without a history of nausea and vomiting for whom minimally emetic risk chemotherapy is prescribed should not routinely receive antiemetic prophylaxis. A single agent such as a low-dose corticosteroid is suggested for patients receiving agents of low emetic risk. If nausea and vomiting occurs during subsequent cycles of chemotherapy, prophylaxis with a single agent such as a substituted benzamide, a corticosteroid, or a phenothiazine should be administered. Only patients with persistent nausea and vomiting despite treatment with these recommended agents should receive a 5-HT3 receptor antagonist in the following cycles.

Antiemetics↗
PubMed2006

Emetic potential of daily oral etoposide.

BACKGROUND: Chemotherapeutic agents are classified by their degree of emetogenicity. Highly and moderately emetogenic agents require antiemetic prophylaxis for chemotherapy-induced nausea and vomiting. Intravenous etoposide is listed as having low emetic potential. However, oral etoposide is categorized as having moderate emetogenicity. Daily oral etoposide is used in refractory germ cell cancer patients. We prospectively evaluated the emetic potential of oral etoposide in this patient population. MATERIALS AND METHODS: Between August 2003 and February 2006, 16 patients with refractory germ cell cancer received single-agent, daily oral etoposide 50 mg/M(2) for 21 consecutive days every 4 weeks. All patients had progressed after cisplatin combination chemotherapy and had received high-dose chemotherapy with carboplatin plus etoposide (intravenously) with peripheral blood stem cell transplant. No patient received prophylactic antiemetics. Patients completed a six-question Multinational Association of Supportive Care in Cancer (MASCC) antiemetic tool during each day of etoposide during the first 21-day course. Nausea intensity and duration were recorded. Number of emetic episodes and any antiemetic medications were recorded. RESULTS: All 16 patients completed the six-question MASCC form. Eleven of 16 had no nausea or vomiting and two other patients had only minimal nausea, despite absence of any prophylactic antiemetics. Only two patients required antiemetic support. Two patients experienced emesis for a single episode. One patient had nausea on days 9-20 with a MASCC rating of 3-6, and one patient had continued mild nausea (MASCC rating 1-3) for all 21 days. CONCLUSIONS: Daily oral etoposide has a low probability of producing chemotherapy-induced nausea and/or vomiting and, in our opinion, does not require prophylactic antiemetics.

Administration, Oral↗
PubMed1995

Emetic, central nervous system, and pulmonary activities of rolipram in the dog.

Rolipram was characterized for its emetic, behavioral, cardiovascular and pulmonary activities in dogs, to assess its systemic pharmacology and potential bronchodilatory selectivity. At doses > or = 0.1 mg/kg i.v., rolipram induced emesis, anxiety, and stepping behaviors in conscious dogs, and increased heart rate and cardiac contractility in anesthetized instrumented dogs not treated with a beta-adrenoceptor antagonist. Cardiovascular effects in anesthetized dogs were apparently related to rolipram's central nervous system activities, in that they were associated with a reversal pentobarbital-induced anesthesia and could be ablated by pentobarbital supplementation. Rolipram's reversal of anesthesia was confirmed in uninstrumented dogs, where rolipram shortened pentobarbital sleep time while increasing heart and respiratory rates. After intragastric administration, rolipram exhibited greater emetic potency (100% emesis at 0.1 mg/kg p.o.) and lesser bronchodilatory potency (ED50 = 0.04 mg/kg i.d.) than after i.v. administration. The data demonstrate that rolipram is a potent bronchodilator that produces central nervous system effects only at higher doses when administered i.v. to the dog. Administered intragastrically, however, the bronchodilatory selectivity of rolipram is reduced presumably as a result of the activation of emetic reflexes at sites within the gastrointestinal tract.

Animals↗
PubMed1996

The pharmacology of the emetic response to upper gastrointestinal tract stimulation in Suncus murinus.

This paper is the first to describe aspects of the mechanics of retching in the insectivore Suncus murinus (house musk shrew) and in an animal of such a small size (approximately 50 g). In anaesthetised animals using the novel stimulus of mechanical stimulation of the upper gastrointestinal tract as the provocative stimulus the frequency of retching was found to be about 4 retches/s, a much higher frequency than in other species (dog, cat, ferret). These studies show that quantification of retching in Suncus cannot be undertaken using direct observation. The temporal pattern of the emetic response was characterised in conscious Suncus using motion (1 Hz, 5 min) and nicotine (20 mg/kg s.c.). The ultrapotent capsaicin analogue resiniferatoxin (100 micrograms/kg s.c.) was discovered to be highly emetic and comparative studies showed that nicotine and resiniferatoxin induced the most intense responses with episodes (retches and a vomit) occurring every 10-15 s. The retching response to mechanical stimulation in the anaesthetised Suncus was not blocked by a 5-HT3 receptor antagonist (granisetron, 1-5 mg/kg s.c.), a tachykinin NK1 receptor antagonist (CP-99,994 20 mg/kg s.c. dihydrochloride salt (9+) -(2S,3S)-3-(2-methoxybenzylamino)-2-phenylpiperidine) or morphine (2 mg/kg s.c.) but was blocked by the 5-HT1A receptor agonist 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT 100 micrograms/kg s.c.). Suncus appears to be a suitable animal in which to study the pharmacology of the emetic response to mechanical stimulation of the gut. The results are discussed in the light of studies of the pharmacology of emesis in other species.

8-Hydroxy-2-(di-n-propylamino)tetralin↗
PubMed1990

Mechanism for the emetic side effect of xanthine bronchodilators.

The usefulness of xanthine bronchodilators in the treatment of asthma is often limited by the side effects of nausea and vomiting. We investigated the mechanism of emesis induced by xanthines, by examining the roles of phosphodiesterase (PDE) inhibition and adenosine antagonism. Theophylline, enprofylline, 8-phenyltheophylline and isobutylmethylxanthine (IBMX), as well as vehicle, were given to ferrets at doses ranging from 0.1 to 150 mg/kg i.p. The potencies of these compounds in producing emetic responses were ranked IBMX greater than enprofylline greater than theophylline greater than 8-phenyltheophylline. These results correlate well with the relative potencies of the compounds as nonselective PDE inhibitors but do not correlate with their relative potencies as adenosine A1 or A2 receptor antagonists. The emetic responses also correlate well with the previously reported potencies of these xanthines as bronchodilators in guinea pigs. We conclude that the emetic side effect of xanthine bronchodilators results from the inhibition of one or more forms of PDE rather than from adenosine antagonism.

1-Methyl-3-isobutylxanthine↗