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)

2-Chloro-11-(2-dimethyl-aminoethoxy)dibenzo [b,f]thiepine (zotepine) is a new neuroleptic drug with a chemical structure different from known neuroleptics. The psychopharmacological effects of zotepine in mice, rats and dogs were studied and compared with those of commercially available neuroleptics. Haloperidol and perphenazine were the most active and thioridazine was the least active in hibiting apomorphine-induced gnawing and circling movement, methamphetamine-induced gnawing and circling movement, conditioned avoidance response, motor activity, dopamine-induced pancreatic secretion and apomorphine-induced vomiting. These drugs also had the same order of potency in inducing catalepsy and increasing dopamine turnover and prolactin release. Chlorpromazine, propericiazine and thiothixene were intermediate in potency. Zotepine equalled chlorpromazine in most activities, however, it was clearly less active than chlorpromazine in potentiation of barbiturate sleep and cardiovascular effect.
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PMID:Pharmacological study of [2-chloro-11-(2-dimethylaminoethoxy) dibenzo[b,f]thiepine] (zotepine), a new neuroleptic drug. 4 13

The results of this study demonstrate that prochlorperazine, haloperidol and droperidol are all effective post-operative anti-emetic compounds when compared to saline but vary in onset of activity and duration of action. Haloperidol has the shortest onset of action, being effective within 30 minutes of intravenous administration. Prochlorperazine has an intermediate onset of action and droperidol is the slowest of the three compounds but the only one to provide significant anti-emesis 4-24 hours following administration. Our data suggest that a combination of haloperidol and droperidol may be more effective as an anti-emetic than any one of the compounds used alone.
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PMID:Comparison of droperidol, haloperidol and prochlorperazine as postoperative anti-emetics. 46 47

1 Peruvoside, (a glycoside obtained from the plant, Thevetia neriifolia Juss) and ouabain produce emesis in cats. Vomiting is not produced by these drugs in animals pretreated with catecholamine depleting drugs like reserpine, tetrabenazine or syrosingopine. Chloropromazine hydrochloride, mepyramine maleate, or BOL-148 administered intravenously or intracerebro-ventricularly do not afford protection.2 Phenoxybenzamine produces partial protection against peruvoside-induced emesis.3 Haloperidol (1 mg/kg i.v.) prevents vomiting induced by peruvoside or ouabain. Intracerebroventricularly administered haloperidol is ineffective.4 Cats pretreated with SKF-525-A, are not protected by haloperidol. Animals pretreated with phenobarbitone in a dose of 25 mg/kg for a week were protected by haloperidol, 250 mug/kg i.e. one quarter of the effective antiemetic dose in normal cats.5 It is postulated that catecholamines are involved in the mechanism of vomiting induced by cardiac gycosides. Further, a metabolite of haloperidol seems to be responsible for its effective antiemetic action.
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PMID:Role of catecholamines in the central mechanism of emetic response induced by peruvoside and ouabain in cats. 114 5

In healthy volunteers the emetic effect of apomorphine (5-10 mg, i.m.) was prevented by haloperidol (2 mg), metoclopramide (10 mg) and sulpiride (100 mg), injected intramuscularly. In parkinsonian patients, apomorphine (1 mg) given alone ameliorated the neurological symptoms (30% improvement in the disability score), but the improvement was accompanied by nausea, vomiting, sedation or sleepiness. Haloperidol (2 mg) prevented not only the emetic effect of apomorphine (10 mg), but also its therapeutic efficacy in parkinsonism. Indeed, the disability score was worsened by the drug combination in some patients. Moreover, after haloperidol, apomorphine produced deep sedation and sleep. By contrast, in parkinsonian patients pretreated with metoclopramide (10 mg) or sulpiride (100 mg), apomorphine (10 mg) markedly diminished tremor and rigidity and failed to produce nausea, vomiting and sleepiness.
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PMID:Therapeutical efficacy of a combination of apomorphine with sulpiride or metoclopramide in Parkinsonism. 127 13

Metoclopramide is an effective antiemetic for cisplatin-induced vomiting when given in parenteral high-dose regimens but not oral low-dose regimens. Metoclopramide was compared to haloperidol, also given in a high-dose parenteral regimen. Patients received two cycles of cisplatin at a dose greater than or equal to 70 mg/m2. Metoclopramide (2 mg/kg intravenous) was given every two hours for five doses beginning one half hour before cisplatin. Haloperidol (3 mg intravenous) was given on the same schedule. A randomized double-blind crossover design was used to control subjective bias and to compare the same patient's experiences. Twenty-eight patients completed both study arms. Excellent control of vomiting was achieved with both drugs. Metoclopramide resulted in 1.92 vomiting episodes (range, 0-5) with 36% having no vomiting. Haloperidol resulted in 3.04 vomiting episodes (range, 0-8) with 20% having no vomiting. Significantly fewer vomiting episodes were noted with metoclopramide rho = .006, paired sign test). However, responses to the two drugs were well correlated (Spearman's rho = .39, P = .03). Metoclopramide and haloperidol are both excellent antiemetics when given in sufficient dosage by an effective route. Metoclopramide does show a mild advantage. However, the positive correlation in response to these agents suggests a common mechanism of action. The ability to identify related antiemetics will be useful in the design of rational combination antiemetic therapy.
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PMID:Comparison of the antiemetic effect of high-dose intravenous metoclopramide and high-dose intravenous haloperidol in a randomized double-blind crossover study. 653 12

Sixty-four patients receiving cancer chemotherapy known to induce severe emesis entered a randomized double-blind study of the antiemetic efficacy of haloperidol (Haldol) and benzquinamide (Emetecon). Patients preferred haloperidol for control of emesis induced by cis-platinum (78 vs. 22%) or nitrogen mustard (67 vs. 16%). Patients receiving Doxorubicin preferred benzquinamide by a small margin (46 to 38%). Individual patients who experienced no relief with their first antiemetic (13 of 15) usually got some relief with the other after crossover. Haloperidol was more effective than benzquinamide (54 vs. 29%) in patients previously unrelieved by prochlorperazine (Compazine). Complete relief of vomiting was obtained in 14 of 45 patients receiving haloperidol but only five of 41 patients receiving benzquinamide experienced no vomiting, again dependent on the anticancer agent used. Although haloperidol is a more effective antiemetic agent overall, efficacy is related to the anticancer treatment and probably to individual patient characteristics.
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PMID:Specific antiemetics for specific cancer chemotherapeutic agents: haloperidol versus benzquinamide. 701 68

In order to more fully characterize sigma ligand-induced emesis in the pigeon, the effects of a number of compounds were tested alone or in combination with ditolyguanidine (DTG). The drugs tested could be categorized into three types: agonists, which produced the emetic response (DTG > amitriptyline > BD 737 > thioridazine), antagonists, which effectively antagonized the effects of DTG (haloperidol > BMY 14802 > BD 1139 > chlorpromazine), and agents which did not produce the emetic response on their own, but potently enhanced the emetic effect of DTG (BD-1008 > or = phencyclidine > (+)-n-allylnormetazocine > or = propranolol). Chronic haloperidol resulted in a markedly diminished emetic response to DTG, which returned to control levels by 24.5 days. Haloperidol, but not BMY 14802, was effective in antagonizing the lethal effects of DTG. These data suggest further in vivo evidence for a functional mediation by sigma sites of the emetic response to DTG in the pigeon, and may provide in vivo evidence for potential allosteric modification of sigma ligands.
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PMID:Sigma receptor-mediated emetic response in pigeons: agonists, antagonists and modifiers. 810 May 32

The present study was designed to examine withdrawal from a therapeutic, non abused drug, haloperidol. Rats were trained to discriminate the anxiogenic compound pentylenetetrazol (PTZ) from water in a two lever, food reinforced, drug discrimination procedure. Dose effect curves were then determined for PTZ and the antipsychotic drug, haloperidol (0.1-1 mg/kg). Haloperidol did not substitute for PTZ, even at a dose that decreased rates of responding to approximately 15% of control values. Rats were then treated chronically with either 1 or 2 mg/kg/day haloperidol while training was suspended. After 5 days of chronic haloperidol 4/6 animals in the 1 mg/kg/day group and 5/7 in the 2 mg/kg/day group chose the PTZ lever when tested 24-48 hours after the last haloperidol injection. Haloperidol, 1 or 2 mg/kg, did not reverse PTZ-lever responding. After an additional 5 days of chronic haloperidol, 3/6 rats in the 1 mg/kg/day group and 5/7 rats in the 2 mg/kg/day group responded on the PTZ lever 24 hours after the last injection, and this was reversed with the anxiolytic, chlordiazepoxide (3.2-5.6 mg/kg). The current findings indicate that there is an anxiogenic component to withdrawal from haloperidol. In psychotic patients, abrupt discontinuation of haloperidol results in nausea, vomiting and sweating, as well as a "relapse into psychosis" characterized by anxiety, depression and internal chaos (1). Interestingly, the authors caution that the so-called relapse into psychosis may simply be a sign of withdrawal. The current findings support their view and suggest that abrupt discontinuation of psychoactive therapeutic agents may result in anxiety.
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PMID:Withdrawal from chronic haloperidol substitutes for the pentylenetetrazol discriminative stimulus. 846 31

Intestinal pseudo-obstruction (Ogilvie's syndrome) has previously been reported in 2 patients with theophylline toxicity treated with activated charcoal (AC), mechanical ventilation and opioid induced sedation. We report a case of Ogilvie's syndrome in a theophylline toxic patient treated with AC. A 45-y-old male with severe chronic obstructive pulmonary disease presented with vomiting and multifocal atrial tachycardia after an intentional theophylline overdose. His initial potassium concentration was 2.7 mEq/L and his theophylline was 191 mg/L (1060 mumol/L). The patient was hemodialyzed and given a total of 1,000 g of AC without cathartics during the first hospital day. He also received iv potassium replacement. On the second hospital day he required mechanical ventilation for respiratory acidosis. Clindamycin was given for purulent sputum and fever. Haloperidol was given to treat agitation. No other anticholinergic agents or opioids were given. The patient's potassium rose to 6.5 mEq/L and he was given kayexalate. During the third hospital day the patient developed abdominal distention, tenderness and leukocytosis. Abdominal radiographs revealed a distended cecum. In the operating room the cecum was found dilated to 16 cm with no distal obstruction. A cecostomy tube drained AC and pill fragments. A 6 cm charcoal bezoar was found in the stomach. The patient recovered uneventfully.
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PMID:Intestinal pseudo-obstruction (Ogilvie's syndrome) in theophylline overdose. 888 46

Haloperidol is a butyrophenone neuroleptic agent characterized as a high-affinity dopamine antagonist, originally used for the treatment of schizophrenia. Awareness of the role dopamine plays in many symptoms in palliative care, such as nausea, vomiting, and delirium, has led to the use of dopamine antagonists such as haloperidol for the treatment of these symptoms in the palliative care setting. Listed as 1 of the 25 important drugs in palliative care, haloperidol can be administered by multiple routes and can be given without dose alteration in the setting of both renal and hepatic insufficiency. Haloperidol is extensively metabolized in the liver, with CYP3A4 the chief cytochrome oxidase responsible for metabolism. This article will review the pharmacology, pharmacokinetics, and current uses of haloperidol in palliative medicine. There will be an examination of the evidence base for the use of haloperidol in palliative medicine.
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PMID:Role of haloperidol in palliative medicine: an update. 2199 45


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