Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0432222 (SEM)
 47,337 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Plasma ergotamine levels were measured in 33 volunteers (subgroups 11, 12 and 10) after a single dose of ergotamine administered by various routes. Ergotamine tartrate was given in doses normally used in the treatment of acute migraine--2.0 mg orally, 2.0 mg combined with 100 mg caffeine rectally and 0.5 mg i.m. Plasma ergotamine concentrations were determined by radioimmunoassay. The highest and longest lasting levels were found after i.m. administration, the peak concentration being 1.94 +/- 0.34 (SEM) ng/ml at 1/2 h. The corresponding maximum concentrations after oral and rectal administration were 0.36 +/- 0.08 ng/ml at 2 h and 0.42 +/- 0.09 ng/ml at 1 h. In most of the subjects the plasma ergotamine level began to rise again at 24 to 48 h. The cause of the elevation is not known but it might favour possible accumulation of the drug. Absorption from suppositories was at least as good as after oral administration and the former route may therefore be advantageous for migraine patients in whom nausea and vomiting during an attack may prevent efficient oral medication.
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PMID:Systemic availability of ergotamine tartrate after oral, rectal and intramuscular administration. 42 28

We compared the efficacy and safety of ondansetron (GR 38032F), a selective antagonist of serotonin S3 receptors, with that of placebo in controlling the nausea and vomiting induced by cisplatin treatment in 28 patients with cancer. The patients received either three intravenous doses of ondansetron (0.15 mg per kilogram of body weight) or normal saline (placebo) at four-hour intervals, beginning 30 minutes before the administration of cisplatin. Nausea and vomiting were markedly diminished in the group given ondansetron. The median time to the first episode of emesis was 2.8 hours in the placebo group and 11.6 hours in the ondansetron group (P less than 0.001); the median number of episodes in 24 hours was 5.5 in the placebo group and 1.5 in the ondansetron group (P less than 0.001); the mean (+/- SEM) number of regurgitations or dry heaves per episode was 3.2 +/- 0.5 in the placebo group and 1.17 +/- 0.1 in the ondansetron group (P less than 0.001). None of the 14 patients given ondansetron, but 12 of 14 given placebo, required treatment with antiemetic-rescue agents for the control of nausea and vomiting. There were no adverse effects attributable to ondansetron. The urinary excretion of 5-hydroxyindoleacetic acid, the main metabolite of serotonin, was increased in all patients two to six hours after they received cisplatin chemotherapy, and the increases paralleled the episodes of emesis. We conclude that ondansetron is an effective and safe agent for controlling the nausea and vomiting induced by cisplatin treatment. We suggest that cisplatin treatment increases the release of serotonin from enterochromaffin cells, and that ondansetron acts by blocking S3 receptors for serotonin.
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PMID:Efficacy of ondansetron (GR 38032F) and the role of serotonin in cisplatin-induced nausea and vomiting. 214 2

In an effort to determine the incidence of respiratory depression and other side effects of subarachnoid morphine, we conducted the following prospective study in a large number (856) of young female patients undergoing cesarean delivery in one hospital. During the period from July 1987 to January 1989, patients receiving subarachnoid hyperbaric bupivacaine combined with 0.2 mg preservative-free morphine were included. They were continuously monitored for 24 hours using a pulse oximeter. For 24 hours, the vital signs, including respiratory rate every hour, and the side effects, including pruritus, nausea, and vomiting, were recorded. The need for analgesia and the total dose of opioids during the first 24 hours were documented. Our results showed that respiratory depression (SaO2 less than or equal to 85% and/or respiratory rate ten breaths per minute or less) occurred in eight patients, all of whom were markedly obese. Fifty-eight percent of the patients did not require analgesics for 24 hours. In those requiring an added opioid, the dose was (9.1 +/- 0.5 mg morphine, mean +/- SEM). Eighty-five percent of the patients were satisfied with the postoperative analgesia. Six percent were dissatisfied due to the side effects, i.e., pruritus, nausea and/or vomiting. Nine percent were dissatisfied with the pulse oximeter because it caused false alarms and limited their mobility.
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PMID:The addition of 0.2 mg subarachnoid morphine to hyperbaric bupivacaine for cesarean delivery: a prospective study of 856 cases. 188 70

The authors studied the effects of epidural sufentanil (0.75 microgram.kg-1) after urologic surgery in 15 children ranging in age from 4 to 12 yr, and in weight from 14 to 47 kg. The onset and duration of analgesia were 3.0 +/- 0.3 and 198 +/- 19 min, respectively (mean +/- SEM). Side effects included pruritus (3/15), nausea and vomiting (5/15), drowsiness (10/15), and urinary retention (1/11). No apnea was observed. Periosteal analgesia and ventilation were studied in eight of the children (mean age 8.6 +/- 0.8 yr). There was significant periosteal analgesia of the tibia (30, 60, 90, and 120 min after injection) and of the radius (60, 90, and 120 min after injection). Resting respiratory rate and tidal volume did not change during the study. Resting minute-ventilation decreased from 6.3 +/- 0.5 l.min-1 preoperatively to 5.6 +/- 0.6 l.min-1 (P less than 0.05) postoperatively, before epidural sufentanil injection; it did not decrease further after epidural sufentanil. Similarly, end-tidal CO2 tension increased significantly from 37.2 +/- 0.7 mmHg preoperatively to 39.9 +/- 1.2 mmHg (P less than 0.05) postoperatively, before epidural sufentanil; epidural sufentanil did not cause a further significant increase in end-tidal CO2 tension. The slope of the CO2 ventilatory response curve decreased significantly from 1.68 +/- 0.12 l.min-1. mmHg-1 preoperatively to 1.10 +/- 0.13 l.min-1.mmHg-1 (P less than 0.01) postoperatively. There were further significant decreases to 0.68 +/- 0.10 and 0.89 +/- 0.16 l.min-1.mmHg-1 30 and 60 min after epidural sufentanil.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Analgesia and ventilatory response to CO2 following epidural sufentanil in children. 289 31

Acodazole (NSC 305884) was examined in a Phase I trial evaluating a 1-h infusion repeated every 21 days in 37 patients with advanced carcinomas. Cardiac toxicity was dose-limiting at 1370 mg/m2, manifested as multiple premature ventricular contractions, QTc interval prolongation, and decreasing heart rate. Other toxicities included mild to moderate nausea and vomiting and local reaction near the i.v. injection site requiring the use of central venous catheters. Antineoplastic activity was not observed. Acodazole levels assayed by high-performance liquid chromatography disclosed a peak plasma level of 19 +/- 4 (SEM) micrograms/ml for 1370 mg/m2. Acodazole plasma levels decreased in a triphasic manner over a 100-fold range. The volume of distribution at steady state was 238 +/- 18 liter/m2 suggesting extensive tissue binding. The total body clearance was 13.6 +/- 0.9 liter/h/m2; the percentage of urinary excretion was 29 +/- 2% for 48 h. To evaluate cardiac toxicity, acodazole was administered to five dogs at 2262 mg/m2 (1-h infusion) which provided plasma concentrations similar to those achieved at 1370 mg/m2 in humans. Consistent findings in dogs were drug-related prolongation of QTc intervals, and reduction in heart rate, left ventricular dP/dt, and mean blood pressures. Clinical development of acodazole requires studies to further elucidate and alleviate this cardiac toxicity.
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PMID:Acodazole hydrochloride: phase I trial, pharmacokinetics, and evaluation of cardiotoxicity in dogs. 339 Aug 38

The anesthetic effect of 2 ml of 5% lidocaine in 7.5% glucose (LG) or 5% meperidine in water were evaluated and compared in 40 ASA class 1 or 2 patients. Patients were randomly assigned to one of the two groups (20 patients in each) according to the anesthetic agent, which was injected into the lumbar subarachnoid space in the sitting position. The patients remained sitting for 5 min before being placed in the supine position. Times of onset of sensory and complete motor blockade were significantly more rapid with LG. The extent of maximum cephalad spread of analgesia and the time to maximum height of analgesia in the two groups were not different. Duration of analgesia at the T-7 (48.96 +/- 6.64 min with LG, 44.74 +/- 6.14 min with meperidine; means +/- SEM) and L-1 (94.37 +/- 7.42 min with LG, 76.19 +/- 5.64 min with meperidine) dermatomes was not different in the two groups but was statistically longer at the T-10 dermatome with LG (66.83 +/- 6.72 min) than with meperidine (46.66 +/- 6.26 min). The duration of complete motor blockade was also significantly longer with LG (66.44 +/- 7.05 min) than with meperidine (42.67 +/- 4.47 min). Complications in both groups included decrease in blood pressure and nausea and vomiting intraoperatively, and urinary retention, nausea and vomiting, and mild headache postoperatively. Complications that occurred only in the meperidine group were intraoperative drowsiness, respiratory depression, bronchospasm, and itching. The frequency of complications was greater wit meperidine.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Meperidine as a spinal anesthetic agent: a comparison with lidocaine-glucose. 354 85

A double-blind, between-patient comparison of intramuscular pethidine 100 mg and nalbuphine 20 mg for the relief of pain during labour in 80 patients is described. Severity of pain was assessed before and after treatment by subjective pain scores and visual analogue scales. Neither of these methods showed a significant difference between the treatments. Nalbuphine was associated with less maternal nausea and vomiting than pethidine, but this possible advantage was somewhat offset by a tendency of the drug to produce more maternal sedation and dizziness. The mean umbilical vein/maternal vein ratio was significantly higher for nalbuphine (0.78, SEM 0.03) than for pethidine (0.61, SEM 0.02), which suggests easier placental transfer of the former. This finding was reflected in significantly lower 2-4 hour neurobehavioural scores for the infants of mothers given nalbuphine, but there was no significant difference between these scores at 24 hours. On the basis of this study, nalbuphine does not offer a substantial improvement over pethidine for pain relief in labour.
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PMID:A double-blind comparison of intramuscular pethidine and nalbuphine in labour. 381 47

The acute effects of an oral preparation of sulmazol, a recently synthesized cardiotonic agent, were assessed by means of a Swan-Ganz catheter in 10 patients who had advanced heart failure that persisted despite treatment with digitalis, diuretics and nitrates. All patients demonstrated a hemodynamic improvement. Pulmonary wedge pressure decreased significantly 1 h after administration from 26 +/- 2 to 16 +/- 3 mm Hg (mean +/- SEM; 32%; p less than 0.01) and this decrease remained significant at least 6 h after intake. The cardiac index increased from 1.8 +/- 0.1 to 2.4 +/- 0.1 1/min/m2 (33%; p less than 0.01) and remained significant up to 6 h later. Total systemic and pulmonary resistances were also significantly decreased (peak changes 28% and 46%, respectively) up to 6 h later. Heart rate and mean blood pressure were unaffected. Once the duration of action was assessed for each patient, a short-term oral therapy was initiated for 48 h. Hemodynamic measurements performed 24 h and 36 h following the commencement of this chronic therapy showed the sustained hemodynamic improvement. 7 patients were continued on sulmazol therapy for 3 weeks to 6 months. Side effects were nausea and vomiting (which were likely to be dose-related), worsening arrhythmias and a possible rebound phenomenon after withdrawal. Although orally administered sulmazol shows promise as a potentially useful agent in the treatment of advanced heart failure, the safety of this drug remains to be established.
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PMID:Clinical and hemodynamic observations on orally administered sulmazol (ARL115BS) in refractory heart failure. 639 55

Sedation is routinely required for successful Magnetic Resonance imaging in infants and children. Five hundred and ninety-six paediatric patients (270 female and 326 male, age (mean +/- SD) 41 +/- 30 months and weight 14.8 +/- 6.5 kg) entered an open, non-comparative, prospective study to assess oral chloral hydrate sedation in a large and homogeneous paediatric population undergoing Magnetic Resonance imaging. Chloral hydrate syrup 70 mg/ml was administered 20-40 min prior to the procedure. Effective sedation was reached in 94.1% with a total dose (mean +/- SEM) of 68 +/- 1 mg/kg (range 20-170 mg/kg). Statistical analysis of sedation failures vs. successful examinations after the total dose showed significant differences for dose (62 +/- 4 vs. 69 +/- 1 mg/kg; P < 0.05), age (64 +/- 7 vs. 40 +/- 1 months; P < 0.001) and weight (19.8 +/- 1.5 vs. 14.5 +/- 0.0 kg; P < 0.001). Effectiveness fell to around 80% in children with encephalic white matter alterations, medullary tumours or syringohydromyela (P = 0.07). The mean time of onset of sedation was 26 +/- 1 min, and the mean time to spontaneous awakening after the completion of the Magnetic Resonance examination was 38 +/- 2 min. Fifty-nine children (9.9%) experienced adverse reactions, with nausea and vomiting being the most common (n = 41), followed by nervousness and unusual excitement (n = 6). Discriminant function analysis identified age and total dose as the quantitative variables helping to differentiate between sedation failures and satisfactory examinations (sensitivity = 0.73, and specificity = 0.61; r = 0.20, P < 0.001).(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Oral chloral hydrate provides effective and safe sedation in paediatric magnetic resonance imaging. 798 2

We have compared the dose requirements and side effects of morphine with those of pethidine when administered by patient-controlled analgesia in 40 patients (ASA I-II, 20-65 yr) after elective total abdominal hysterectomy. Patients were allocated randomly, in a double-blind manner, to receive either morphine (bolus dose 2 mg, lockout time 10 min) or pethidine (bolus dose 20 mg, lockout time 10 min) for postoperative pain relief. Mean 24-h morphine and pethidine consumption was 70 (SEM 6.2) mg and 660 (67.8) mg, respectively (ratio 1:9.4). There were no significant differences in postoperative sedation, nausea, pain relief and patient satisfaction (VAS 0-100 mm), and requirements for antiemetics. Four patients receiving pethidine were withdrawn because of postoperative confusion and one receiving morphine because of intractable nausea and vomiting. The 95% confidence interval for this difference between the groups for VAS scores of sedation, nausea and pain were approximately 30 mm.
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PMID:Dose requirements, efficacy and side effects of morphine and pethidine delivered by patient-controlled analgesia after gynaecological surgery. 865 16


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