Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0042963 (vomiting)
 31,883 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Authors, in an open and preliminary study, evaluate the beneficial effects on chemotherapy-induced nausea and vomiting of an association of three antiemetic drugs parenterally administered. Twenty-six patients receiving chemotherapy for Lymphomas (195 cycles) were treated with: Chlorpheniramine maleate 10 mg IM 45' before, Sulpiride 200 mg in normal saline 100 ml, at XXX gtt/m', 20' before, and 6-Methyl-Prednisolone 500 mg IV over 2'-3' immediately before chemotherapy. Patients were evaluated for emesis over 48 hours after chemotherapy: they were interviewed on nausea, vomiting and other possible side-effects. The antiemetic activity observed was: complete response in 73.1% (19/26); partial response 27.9% (7/26). Failure of response was never observed. 166/195 cycles were well tolerated. Our results demonstrate the antiemetic efficacy of this antiemetic regimen. Further studies should investigate its use in randomized trials.
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PMID:[Antiemetic protocol in oncohematologic polychemotherapy]. 337 28

The antiemetic activity, gastric motor activity, and dopamine receptor effects of metoclopramide, dazopride, and sulpiride were assessed to establish if enhancement of gastric motility or antagonism of central dopamine receptors is the predominant action for drug-induced suppression of cisplatin-induced emesis. Emesis produced in dogs by cisplatin is antagonized by metoclopramide and dazopride. The antiemetic actions of metoclopramide and dazopride are associated with their ability to enhance gastric motor activity. Dazopride, unlike metoclopramide, has minimal dopamine receptor antagonist properties. Sulpiride is a potent dopamine receptor antagonist; however, it had no effect on the stomach and was ineffective in suppressing cisplatin-induced emesis.
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PMID:Antagonism of cisplatin-induced emesis by metoclopramide and dazopride through enhancement of gastric motility. 369 69

Sulpiride, which has been utilized as an antipeptic ulcer and antidepressant in Japan, is one of the dopamine antagonists, and is considered to have anti vomiting activity. We designed a comparative controlled study of Sulpiride and Domperidone, against nausea and vomiting during cancer chemotherapy. A total of 69 cases were entered into this study, 34 cases being treated with Sulpiride at a dose of 100 mg i.v. or i.m. (S group), and 35 cases being treated with Domperidone at a dose of 10 mg i.v. (D group), before and after chemotherapy. Three cases from the S group and 4 cases from the D group were excluded from this study because of differences in the administration schedule. There was no difference in patient characteristics between the two groups, such as age, sex, original disease and antitumor agents. According to our criteria 27 of 31 cases in the S group showed effectiveness of the agent against nausea and vomiting (87%), while in the D group, 24 cases showed effectiveness (77%). There was no statistical difference between them, and no side effects were found in either group.
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PMID:[Clinical evaluation of sulpiride against nausea and vomiting during cancer chemotherapy compared with domperidone--envelope method]. 372 95

A new benzamide, cis-N-(1-benzyl-2-methylpyrrolidin - 3 - yl) - 5 - chloro - 2 - methoxy - 4 - methylaminobenzamide (YM-09151-2) exhibited more potent and longer-lasting inhibitory effects on apomorphine-induced behaviours (stereotyped behaviour, emesis and hypothermia), and methamphetamine-induced stereotyped behaviour, conditioned avoidance response and open field behaviour, conditioned avoidance response and open field behaviour than either structurally similar benzamides (YM-0850 and sulpiride) or classical neuroleptics [chlorpromazine (CPZ) and haloperidol(HPD)]. Such inhibitory effects of YM-09151-2 relative to cataleptogenicity were greater than those of CPz and HPD. In contrast, sulpiride elicited few of the neuroleptic effects described above. YM-09151-2, a potent inhibitor for dopamine-sensitive adenylate cyclase (Ki: 3.0 nM) reduced, in a selective manner, the binding of [3H]dopamine to the dopamine D1 receptor (Ki:4.8 nm) associated with adenylate cyclase rather than to the dopamine D2 receptor (Ki: 0.98 microM) independent of adenylate cyclase. Sulpiride, on the contrary, inhibited only the binding to the dopamine D2 receptor, CPZ and HPD antagonized [3H]dopamine nonselectively at the two distinct dopaminergic receptors. These results suggest that YM-09151-2 is a potent and long-lasting neuroleptic with a highly selective blocking action on the dopamine D1 receptor.
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PMID:Neuroleptic properties of cis-N-(1-benzyl-2-methylpyrrolidin-3-yl)-5-chloro-2-methoxy-4-methylaminobenzamide (YM-09151-2) with selective antidopaminergic activity. 611 70

The substituted benzamide sulpiride is considered an "atypical" neuroleptic and antipsychotic in that its pharmacology and clinical effects differ significantly from "classical" dopamine antagonists such as the butyrophenones and phenothiazines. Sulpiride increases dopamine turnover, elevates prolactin release, inhibits emesis, and is an effective antipsychotic. Sulpiride does not affect other transmitters, requires sodium for binding, does not induce catalepsy in rats or strong sedation and extrapyramidal side effects in humans. Compared to the butyrophenone and phenothiazine neuroleptics sulpiride is chemically distinct because it lacks certain properties associated with other dopamine antagonists. Poor blood-brain barrier penetration and preferential receptor affinities in different brain regions are the most probable reasons for sulpiride's effects in vivo. Nevertheless, the atypical conformation of sulpiride merits study of its structure-activity relationships. Experimental determination of specific pharmacophores could provide the data necessary for a computer analysis of structure. Comparison of relative orientation of sulpiride's pharmacophores with similar data on classical neuroleptics is suggested for study of structural requirements for dopamine antagonism.
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PMID:Sulpiride: assessment of a pharmacologically and chemically distinct neuroleptic. 614 15

The domestic pig was used to develop a new model for evaluating the emetogenic potential of anticancer drugs and determining the antiemetic activity of drugs. Emesis was characterized by expulsion of solid or liquid material. In each animal, the number of vomits after infusion of the emetogenic drug (infusion in ketamine and xylazine anesthesia) was recorded in 1-hr periods during the first 4 hr and then in a 4- and a 16-hr period. Intravenous infusion of cisplatin caused a concentration-dependent emetic response. Anti-cancer drugs other than cisplatin such as carboplatin, dactinomycin, cyclophosphamide, and ifosfamide, also induced emesis, indicating that the domestic pig is suitable to detect the emetogenic potential of chemotherapeutic agents. A cisplatin dose of 2 mg/kg i.v. proved to be most suitable for studying the effect of potential antiemetic drugs (applied as i.v. injection), because this cisplatin dose caused consistent emetic responses without other toxic signs in the 24 hr following its infusion. Emesis induced by cisplatin was reduced by high doses of metoclopramide (25 mg/pig; approximately 0.8 mg/kg). The more selective dopamine D2 receptor antagonists, alizapride and domperidone, even at high doses (25-50 mg/pig; approximately 0.8-1.6 mg/kg), did not inhibit cisplatin-induced emesis, nor did haloperidol up to 20 mg/pig (approximately 0.6 mg/kg). Sulpride (50 mg/pig; approximately 1.6 mg/kg) halved the occurrence of vomits in the first 4 hr after cisplatin, but this effect was followed by an increase in the frequency of vomits; thus, no change in the total number of vomits was observed in the 24-hr observation period.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Emesis induced in domestic pigs: a new experimental tool for detection of antiemetic drugs and for evaluation of emetogenic potential of new anticancer agents. 786 62

Metoclopramide, a benzamide substitute, is used frequently as an antiemetic drug. Sulpiride, another benzamide substitute, was investigated and found to be safe and effective in a handful of studies involving only oncologic or other severely symptomatic patients. In this investigation the authors compared prospectively the antiemetic efficacy of sulpiride versus metoclopramide in a double-blind, randomized study involving 36 nononcologic patients with transient vomiting or nausea of various etiologies. Each group of 18 patients received oral metoclopramide or sulpiride (10 mg or 50 mg respectively) every 8 hours for a total of three doses each (24 hours of treatment). A 5-point score was used to evaluate symptomatic relief. Efficacy of the two drugs proved similar, and at the end of the study, 14 and 13 of 18 patients on sulpiride or metoclopramide respectively were asymptomatic. Only transient, minor side effects were reported in one patient in each group. The authors conclude that sulpiride is an effective and safe antiemetic drug that can be adopted legitimately in such cases as a first choice, or serve as an equipotent alternative to metoclopramide in patients sensitive to the latter.
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PMID:Sulpiride versus metoclopramide in nononcologic patients with vomiting or nausea. 1040 34

This study introduces Cryptotis parva (the least shrew) as a new dopaminergic animal model of emesis. The potential emetogenic effects of a nonselective dopamine agonist [apomorphine], two D1 agonists [SKF-38393 and SKF-82958], a D2 preferring agonist [quinpirole], and two D3-preferring agonists [7-(OH) DPAT and PD 128, 907] were investigated. Intraperitoneal administration of D1 agonists failed to induce emesis. However, other agonists caused a dose-dependent increase in the percentage of animals vomiting as well as potentiating the mean frequency of emesis with the following ED50, potency order: 7-(OH) DPAT < apomorphine < quinpirole < PD 128, 907. For antagonist studies a 2 mg/kg dose of these agonists were used to induce emesis. Thus, the inhibitory dose-response effects of a D2-preferring [sulpride], a D3-preferring [U 99194A] and combination of varying doses of these antagonists [sulpride + U 99194A] were evaluated on the ability of the cited agonists to produce vomiting. Sulpride decreased the number of shrews vomiting and the mean vomiting frequency produced by the cited agonists in a dose-dependent fashion with the following ID50 order [apomorphine < PD 128, 907 < 7-(OH) DPAT < quinpirole]. By itself, U 99194A failed to significantly alter the emesis produced by any of the cited agonists, however, it potentiated (3-8 times) the antiemetic effects of sulpride both in reducing the number of shrews vomiting as well as decreasing the mean vomiting frequency with the following ID50 order: PD 128, 907 < 7-(OH) DPAT < quinpirole. However, U 99194A attenuated the potent antiemetic effect of sulpride on the apomorphine-induced emesis. The results suggest that the tested agonists primarily activate dopamine D2 receptors to induce emesis in the least shrew whereas activation of D3 sites potentiate the vomiting action of D2 dopamine receptors.
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PMID:The role of D2 and D3 dopamine receptors in the mediation of emesis in Cryptotis parva (the least shrew). 1065 Nov 2

Levosulpiride is a substituted benzamide that is widely used for the management of dyspepsia and emesis. However, little is known about levosulpiride-induced movement disorders (LIM). The aim of this study was to investigate the clinical characteristics of patients with LIM. Among 132 consecutive patients who were diagnosed with drug-induced movement disorders between January 2002 and March 2008, 91 patients with LIM were identified and their medical records reviewed. Seventy-eight (85.7%) patients were aged more than 60 years. The most common LIM was parkinsonism (LIP) (n = 85, 93.4%), followed by tardive dyskinesia (n = 9, 9.9%) and isolated tremor (n = 3, 3.3%). Twenty-one (24.7%) of the 85 patients with LIP were rated as Hoehn and Yahr stage III-V. The oro-lingual area was the only body part that was involved by tardive dyskinesia. LIM persisted after withdrawal of levosulpiride in 48.1% of patients with LIP, 66.7% with dyskinesia, and none with isolated tremor. None of clinical and MRI features predicted the reversibility of LIP. Levosulpiride frequently causes drug-induced movement disorders, presenting mainly with LIP followed by lower face dyskinesia. The symptoms are often severe, and irreversible even after the withdrawal of levosulpiride. Physicians should be cautious in using levosulpiride, especially in elderly patients.
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PMID:Levosulpiride-induced movement disorders. 1979 76