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Prolactin (PRL) secretion was studied after i.m. administration of Metoclopramide (alone or with a pretreatment with 5-Br-2alpha-ergo-cryptine) and after i.m. administration of Sulpiride. The results obtained evidenced a considerable hPRL increase after Metoclopramide administration, similar to that observed with Sulpiride, completely abolished by 5-Br-2alpha-ergocryptine. On the basis of these data it seems evident a strong and specific effect of Metoclopramide on hPRL secretion, probably more potent than Sulpiride.
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Twenty-one patients with early dSSc (mean age 41.4 +/- 9.8 yrs., mean disease duration 2.47 +/- 0.75 yrs.) were prospectively evaluated. Six patients with late dSSc (mean age 52.6 +/- 9.1 yrs., mean disease duration 9.5 +/- 2.5 yrs.) were used as control group. All underwent solid-state esophageal manometry at rest and 15 minutes later received 10 mg of metoclopramide in an intravenous single bolus.
Right lower quadrant pain is one of the most common symptoms of the emergency patients. For accurate diagnosis and treatment; the patients must be questioned and examined very well. Also accompanying conditions due to right lower quadrant pain may be noticed. In this case presentation, we discussed a patient who was presented with right lower quadrant pain and cervical dystonia. By limiting the usage of metoclopramide the patient was followed seamlessly. In this case presentation we want to accentuate that a patient who with abdominal pain may be presented with rare symptoms such of dystonia. In such conditions a detailed anamnesis and physical examination are the first steps of the evaluation to prevent potential hazardous outcomes. In particular, a surgeon must be always carefully while taking history and examining the patient.
The potent serotonin receptor (5-HT3) antagonists are new highly selective agents for the prevention and control of chemotherapy-induced nausea and vomiting that have been shown to be comparable to or more effective than traditional metoclopramide regimens. This study was designed to compare the antiemetic efficacy of dolasetron and metoclopramide in chemotherapy-naive and non-naive cancer patients receiving high-dose cisplatin-containing chemotherapy. This multicentre, double-blind, randomized trial compared the efficacy and safety of single i.v. doses of dolasetron mesilate salt (1.2 or 1.8 mg/kg) and metoclopramide (7 mg/kg) in 226 patients for the prevention of acute emesis and nausea associated with the administration of high-dose (> or = 80 mg/m2) cisplatin. Efficacy and safety were evaluated for 24 h. Complete responses were achieved by 57%, 48%, and 35% of patients given dolasetron mesilate 1.8 mg/kg (P = 0.0009 vs metoclopramide), dolasetron mesilate 1.2 mg/kg (P = 0.0058 vs metoclopramide), and metoclopramide, respectively. Overall, dolasetron was significantly more effective than metoclopramide for time to first emetic episode, nausea, patient satisfaction, and investigator global assessment of efficacy. Males, chemotherapy-naive patients, and alcoholics had higher response rates. Dolasetron was well tolerated, with mild-to-moderate headache most commonly reported. Twelve percent of patients receiving metoclopramide reported extrapyramidal symptoms compared with 0% of patients receiving dolasetron. In conclusion, dolasetron mesilate was effective for the prevention of CINV with high-dose cisplatin. Single i.v. doses of dolasetron mesilate were more effective than 7 mg/kg metoclopramide in preventing nausea and vomiting induced by highly emetogenic cisplatin-containing chemotherapy. In addition, 1.8 mg/kg dolasetron mesilate consistently produced the highest response rates and appears to be the most effective dose for further clinical development.
I have discussed the pharmacokinetics, efficacies, and side effects of the various nonnarcotic drugs available for the treatment of patients who have headache. Sumatriptan, the newest one, is expensive but may be cost-effective for those who have failed traditional migraine treatment, who visit the ER frequently, who have potential for drug abuse, or who have to miss time from school or work due to the headache. Studies are in progress to compare sumatriptan with other available drugs such as DHE-45 and to determine its possible role in the prophylaxis of migraine. A new 5-HT1D receptor agonist with more efficacy and fewer side effects may be developed in the future. When sumatriptan and DHE-45 are contraindicated due to hypertension or coronary artery disease, other drugs such as metoclopramide, ketorolac, and butorphanol can be used as alternatives.
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The administered BL bacteria were easily imaged and localized in the stomach and subsequently followed in the duodenum and upper intestine allowing to accurately calculate GE. Gastric emptying after the test meal was significantly slower (T(1/2) 16 ± 3 min) than that obtained in fasting conditions (T(1/2) 2 ± 1 min); administration of HY (1 mg kg(-1) b.w.) significantly (P < 0.05) increased T(1/2) that was delayed up to 25 ± 4 min; MET (1 mg kg(-1) b.w.) significantly (P < 0.05) accelerated T(1/2), that was achieved within 8 ± 2 min.
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Cisapride, but not metoclopramide or erythromycin, is able to improve postoperative ileus in the rat. The results suggest that a combination of 5-HT(3) receptor antagonist and 5-HT(4) receptor agonist properties may be required to obtain a beneficial effect on surgery induced ileus in the rat. Furthermore, they indirectly indicate that stimulation of the excitatory mechanisms is not able to overcome the inhibitory influence of the neural reflex pathways activated during abdominal surgery.
Uterine smooth muscle strips from rats were suspended in organ baths containing Krebs solution, and then isometric tension was measured. The response to erythromycin and the effect of hexamethonium, indomethacin, phentolamine, diphenhydramine, atropine, metoclopramide and verapamil on erythromycin-induced contraction were also assessed.
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Baseline serum prolactin (PRL) was found to be similar in 35 men with untreated essential hypertension (149 +/- 2/98 +/- 1 mmHg; means +/- s.e.) and 44 healthy normotensive men (126 +/- 1/80 +/- 1 mmHg), all 40 years old. A correlation between baseline PRL and aldosterone was found in the normotensive (r = 0.534, P less than 0.001), but not in the hypertensive group (r = -0.011, NS). Ten subjects from each group received intravenous metoclopramide, a competitive dopamine antagonist, while another 12 normotensive subjects were given saline only, and the effect on PRL, vasopressin (AVP) and catecholamines was followed. An exaggerated PRL response to metoclopramide was observed in the hypertensive group compared with the normotensive (P less than 0.05), and the mean normotensive peak value never exceeded the hypertensive. Plasma noradrenaline increased significantly compared with baseline (P less than 0.05) and the control group (P less than 0.001), concomitant with increased heart rate (P less than 0.05), after the administration of metoclopramide both in the hypertensive and normotensive group. After intravenous injection of metoclopramide, forearm blood flow increased significantly by 50% in the hypertensive (P less than 0.001), and 80% in the normotensive group (P less than 0.001) compared with the control group. Mean blood pressure remained unchanged as did plasma AVP, dopamine and adrenaline. The present study indicates an altered central dopaminergic activity in essential hypertension. Even at rest, endogenous dopamine exerts a modulating effect on noradrenaline release in both hypertensive and normotensive men.
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Children were assigned randomly to one of three groups (each contained 50 children) to receive dolasetron 1.8 mg kg(-1) or ondansetron 0.15 mg kg(-1) orally, or a placebo. All children received methylene blue capsules (10 mg) orally as an indicator before the induction of anaesthesia. Postoperatively, contamination of the mouth and the endotracheal tube by methylene blue was recorded, and postoperative nausea and vomiting was recorded for 0-1, 1-24 and 0-24 h. Metoclopramide (0.1 mg kg(-1)) intravenously was used as the rescue antiemetic.
The effects of oral metoclopramide, 10 and 20 mg, bethanechol, 25 mg, and placebo on lower esophageal sphincter pressure (LESP) were studied in 15 men with symptoms of gastroesophageal reflux and basal LESP less than 11 mm Hg. Each drug produced a significant increase in LESP when compared to placebo. Metoclopramide, 20 mg, produced a greater increase than either metoclopramide, 10 mg, or bethanechol, 25 mg. Serum gastrin concentrations were not altered by any of the drugs. Side effects were unremarkable. The LESP increasing effect of metoclopramide might be useful in treatment of gastro-esophageal reflux.
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Counselling or prescribing drugs during pregnancy requires health professionals to assess risk/benefit ratio for women and their baby. A misperception of the risk may lead to inappropriate decisions for pregnancy outcomes. The aim of the present study was to assess teratogenic and/or foetotoxic risk perception of common medications by general practitioners (GPs) and community pharmacists (CPs) from the Midi-Pyrenees area.
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Discussion of the presentations of three children at the Middlemore Hospital emergency department with neurological symptoms after exposure to prochlorperazine or metoclopramide and one child with a possible phenothiazine ingestion.
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Functional hyperprolactinemia and relative hyperestrogenism are risk factors of the development concerning fibrocystic changes in the breast.
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The aim of this review was to determine the level of evidence for the treatment of nausea and vomiting with prokinetics and neuroleptics in palliative care patients suffering from far advanced cancer and no longer being treated with chemotherapy or radiation therapy, AIDS, COPD, progressive heart failure, ALS or MS.
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To evaluate the humoral and hemodynamic (both systemic and renal) effects of celiprolol and to assess whether these effects are at least partially due to the activation of dopamine (DA) receptors, 9 out-patients with mild to moderate uncomplicated essential hypertension, without any therapy for at least 3 weeks, received celiprolol (400 mg once daily) and placebo, each for 1 month, according to a double-blind randomized trial pattern. At the end of each treatment period, blood pressure, heart rate, renal plasma flow, glomerular filtration rate, plasma renin activity, plasma aldosterone and plasma norepinephrine were measured after administration of saline solution and intravenous metoclopramide. Compared with placebo, celiprolol significantly reduced mean blood pressure, heart rate and plasma norepinephrine. Plasma renin activity showed a tendency toward a reduction during celiprolol treatment, which was not associated with changes in plasma aldosterone. Despite the decrease in mean blood pressure, renal plasma flow did not change, so that renovascular resistances were significantly reduced. Glomerular filtration rate was unchanged and the filtration fraction showed a trend toward a reduction during celiprolol treatment. Percent decrements of renovascular resistances and of mean blood pressure induced by celiprolol tended to correlate with changes in plasma norepinephrine. Metoclopramide did not influence the hemodynamic (systemic and renal) effects of celiprolol nor plasma renin activity and plasma norepinephrine, and it increased aldosterone levels to a similar extent before and after administration of celiprolol.(ABSTRACT TRUNCATED AT 250 WORDS)
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Postoperative nausea and vomiting (PONV) is still a common perioperative complication and ondansetron has proved to be an effective antiemetic substance in its prevention. The antiemetic effect of single and repetitive application was evaluated in this study. Fifty-one female patients who underwent gynaecological surgical procedures took part in a random double-blind study. Before the start of anaesthesia, 21 patients (group 1) received either a placebo (six patients), 8 mg ondansetron orally (seven patients) or 16 mg orally (eight patients). The remaining 30 patients (group 2), split into subgroups of ten, were given the same preoperative medication as group 1 plus further doses of the same strength 8 and 16 hours after the first intake of the study medication. Metoclopramide was given intravenously if patients had more than one emetic episode or if they asked for it. Nausea and vomiting were documented up to 24 hours after finishing anaesthesia. Metoclopramide had only to be given to patients who had received a placebo. Nausea was felt by 57% (4/7) of the patients after a single dose of 8 mg ondansetron and by 40% (4/10) of the patients after three doses of 8 mg. One patient (14%, 1/7) with a single dose and two patients (20%, 2/10) with a repetitive dose of 8 mg ondansetron vomited. Following a single dose of 16 mg ondansetron, no patient (0/8) had to vomit and 25% (2/8) of the patients had nausea. There were no complications reported by the patients. Ondansetron was shown to be a well-tolerated antiemetic and seems to have a higher reductive effect on PONV when given in a single dose and not repetitively. The prophylaxis of vomiting seems to be more effective than the reduction of nausea. Follow-up studies will have to clarify our findings.
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Granisetron injection used as the primary prophylaxis in LEC demonstrated limited roles in CINV control. Optimization of the guideline-recommended antiemetic regimens may serve as a less costly alternative to protect patients from uncontrolled acute emesis.
Oculogyric crisis is a neurologic reaction characterized by bilateral dystonic elevation of visual gaze as well as hyperextension of the neck. This reaction is most commonly explained as an adverse effect of numerous medications, such as dopamine receptor blocking agents or neuroleptic medications and traditional antipsychotic or antiemetic drugs, such as prochlorperazine or metoclopramide. A case of oculogyric crisis induced by metoclopramide is described in this paper.
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High serum prolactin (PRL) levels and even hyperprolactinemia are a common finding in human immunodeficiency virus (HIV) infection. However, little is known regarding the mechanisms that may contribute to the rise of PRL. We measured serum PRL levels in 54 HIV-infected and 85 healthy age-matched men. The association between PRL levels among anti-PRL autoantibodies and other clinical variables in HIV-infected men was studied. We also evaluated the changes in serum PRL levels by chromatographic separation (affinity with protein G and gel filtration) after a 10-mg iv bolus of metoclopramide. HIV-infected men had higher serum PRL levels compared with healthy men. Sera from 9 of the 54 (16.7%)HIV-infected men were found to have hyperprolactinemia. Moreover, the anti-PRL autoantibody was present in four of nine (44.4%)HIV-infected men with hyperprolactinemia; it was also associated with hyperprolactinemic status. Serum total PRL levels were higher in HIV-infected men with anti-PRL autoantibodies than hyperprolactinemic HIV-infected men without anti-PRL autoantibodies; by contrast, free PRL levels were lower. In HIV-infected men with anti-PRL autoantibodies, gel filtration showed that big big PRL isoform was present as the predominant circulating form of PRL throughout each measurement after iv metoclopramide. By contrast, the predominant isoform of PRL in serum from healthy men and HIV-infected men who were anti-PRL autoantibody negative was little PRL. On the other hand, high serum total PRL levels were observed at each measurement throughout the metoclopramide test in HIV-infected men with anti-PRL autoantibodies; however, the serum free PRL levels were similar to those found in subjects without anti-PRL autoantibodies. These data demonstrated that anti-PRL autoantibodies are associated with hyperprolactinemic status in HIV-infected subjects, particularly in those with high serum PRL levels.
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Drugs that enhance gastrointestinal motility include the benzamide drugs metoclopramide, cisapride and renzapride (BRL-24924). Because these agents also are serotonin-3 (5-HT3) receptor antagonists, which can promote gastric emptying in some species, the motor-stimulating properties of benzamide agents may be due to this mechanism. Metoclopramide (0.3-3.0 mg/kg i.v.), cisapride (0.03-1.0 mg/kg i.v.) and BRL-24924 (0.01-0.1 mg/kg i.v.) were evaluated for their relative motility-stimulating and 5-HT3 receptor antagonist activities in conscious dogs and were compared with selective 5-HT3 antagonist antiemetic compounds ICS-205-930, (3 alpha-tropanyl)1-H-indole-3-carboxylic acid ester and granisetron (BRL-43694). Gastric antral contractions and intestinal myoelectric motility were determined in response to drugs, as were their effects on solid and liquid emptying in a gamma scintigraphic model of gastroparesis. 5-HT3 receptor antagonist potency was examined by deriving ED50 values for inhibition of cisplatin emesis. All drugs were 5-HT3 antagonists as they blocked cisplatin emesis with relative potencies of BRL-43694 = ICS-205-930 greater than BRL-24924 greater than cisapride = metoclopramide. The order of potency for stimulating fasted dog antral contractile activity, however, was BRL-24924 = cisapride greater than metoclopramide greater than ICS-205-930 = BRL-43694. Maximally effective doses of BRL-24924 (0.1 mg/kg i.v.) and cisapride (0.67 mg/kg i.v.) in the antrum also stimulated intestinal myoelectrical activity, whereas ICS-205-930 (0.5 and 2.0 mg/kg i.v.) was not active.(ABSTRACT TRUNCATED AT 250 WORDS)
Prasugrel, a potent thienopyridine, achieves stronger inhibition of platelet activation than clopidogrel. However, onset of inhibition is significantly delayed in patients with acute ST-elevation myocardial infarction (STEMI), as haemodynamic instability and morphine application seem to exhibit significant influence. Since rapid onset of effect was demonstrated in non-STEMI patients when prasugrel was administered only after percutaneous coronary intervention (PCI) without increasing cardiovascular event rates we assessed the efficacy of prasugrel loading immediately after PCI for STEMI instead of pre-loading before revascularisation. We investigated 50 consecutive patients with acute STEMI (mean age 56 ± 10 years) admitted for primary PCI. Prasugrel efficacy was assessed by platelet reactivity index (PRI; VASP assay) before, 1, 2, 4, 6, 12, and 24 hours following an oral loading dose of 60 mg immediately after PCI. High on-treatment platelet reactivity (HTPR) was defined as PRI>50 %. Prasugrel significantly and rapidly reduced platelet reactivity in acute STEMI patients (p<0.0001 at each time point vs control). Morphine application resulted in a significantly higher HTPR rate among patients having received morphine less than 1 hour before prasugrel loading (p<0.001) while concomitant metoclopramide (MCP) treatment did not significantly affect prasugrel efficacy. In conclusion, in contrast to previous reports describing a significant delay in onset of prasugrel-mediated P2Y12 inhibition in acute STEMI, we observed a rapid onset with low HTPR rates comparable to those observed in stable non-STEMI patients. Prasugrel administered directly after primary PCI might therefore be a useful therapeutic strategy in patients with STEMI to provide strong and effective P2Y12 inhibition.
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Preoperative sedation was higher with pregabalin with no significant change in heart rate. The mean arterial pressure was attenuated with oral pregabalin to statistically significant value (P<0.007). The requirement of analgesic drug was reduced with no postoperative respiratory depression, nausea, or vomiting and hemodynamic parameters remained stabilized perioperatively.
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Drugs involved in the most RCTs were: ondansetron 131 RCTs; propofol 118; droperidol 74; metoclopramide 67; granisetron 52; scopolamine 22; tropisetron 16. Drugs involved in the fewest RCTs: two drugs with 2 RCTs; twelve drugs with one; three with none. Probability that this distribution occurred by chance: P < 0.00001; that the distribution of dose-ranging RCTs occurred by chance: P < 0.001. Regression of RCT numbers on cost: R = 0.86, P < 0.0001; on year of drug introduction: R = 0.14. Of 1600 possible comparisons of drugs for PONV, (including dose-ranging) 97.8% have never been published.
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In females undergoing endonasal surgery under propofol-desflurane-remifentanil anaesthesia the incidence of PONV is about 40%. In this setting, both metoclopramide and dimenhydrinate were ineffective to reduce the incidence and the severity of PONV. The combination of both drugs revealed no additional synergistic effect.
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Brains were obtained from 7 drug-induced parkinsonism patients with parkinsonian symptom onset coinciding with use of drugs known to produce parkinsonism. Six were on antipsychotics and 1 was on metoclopramide. Three cases were treated with levodopa for parkinsonism. In two cases, parkinsonian features reversed after stopping the offending agent. Both had autopsy evidence of preclinical PD. In 4 of the remaining 5, dopamine-blocking drugs were continued until death. In 4 of those 5, brain histology revealed no cause for the parkinsonism, but 1 had mild SN neuronal loss without Lewy bodies.