Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0027497 (nausea)
 23,468 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Nausea affects from 40% to 70% of cancer patients who received narcotics to manage their pain. This occurs more frequently when they are ambulatory than when they are recumbent and may be the result of narcotic-enhanced labyrinthine sensitivity to motion. Scopolamine has previously been found to be an effective antiemetic for motion sickness. In a prospective pilot study, 9 (69%) of 13 cancer patients experienced rapid relief of their narcotic-induced nausea when they used Scopolamine Transderm-V patches alone. Only two patients experienced side effects with the scopolamine, and in one patient, the side effects may have been dose related. Although tolerance to the increased vestibular sensitivity may occur, this was not universal. Further prospective trials are necessary to establish whether transdermal scopolamine is useful in controlling the narcotic-induced nausea experienced by cancer patients.
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PMID:Transdermal scopolamine use in the control of narcotic-induced nausea. 188 Apr 39

The authors evaluated the effect of transdermal scopolamine on the incidence of postoperative nausea, retching, and vomiting after outpatient laparoscopy in a double-blind, placebo-controlled study. A Band-Aid-like patch containing either scopolamine or placebo was placed behind the ear the night before surgery. Anesthesia was induced with fentanyl (0.5-2 micrograms/kg iv), thiopental (3-5 mg/kg iv), and succinylcholine (1-1.5 mg/kg iv) and maintained with isoflurane (0.2-2%) and nitrous oxide (60%) in oxygen. Scopolamine-treated patients had less nausea, retching, and vomiting compared with placebo-treated patients (P = 0.0029). Severe nausea and/or vomiting was present in 62% of the placebo group but only 37% of those getting the scopolamine patch. Repeated episodes of retching and vomiting were also less frequent in the scopolamine group compared with the placebo group (23% vs. 41%; P = 0.0213) as was the need for additional antiemetic therapy (13% vs. 32%; P = 0.0013). Patients in the scopolamine group were also discharged from the hospital sooner (4 +/- 1.3 vs. 4.5 +/- 1.5 h; P = 0.0487). Side effects were more frequent among those patients treated with the scopolamine patch (91% vs. 45%; P less than 0.05) but were not troublesome. The authors conclude that transdermal scopolamine is a safe and effective antiemetic for outpatients undergoing laparoscopy.
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PMID:Transdermal scopolamine reduces nausea and vomiting after outpatient laparoscopy. 198 53

Strong premedication may prolong recovery and cause side-effects after short surgical procedures in general anaesthesia. To be operated without premedication may be unpleasant for the patient. Midazolam is a water-soluble benzodiazepine with rapid onset and short half-life. In a randomized study with 193 female patients, we compared the effects and side-effects of three different premedicants i.m.: midazolam, morphine-scopolamine (Mo-Scop) and placebo. Midazolam and Mo-Scop had an equal and significantly better effect than placebo on preoperative anxiety and alertness. Side-effects like nausea, dry mouth and prolonged recovery occurred significantly more often in the Mo-Scop than the midazolam or placebo groups. The midazolam-premedicated patients had significantly more amnesia compared with the other two groups. Only 3% of the patients would prefer no medication before anaesthesia, whereas 80% would prefer a combination of an anxiolytic and hypnotic premedication. Sixty-three percent of the patients would prefer a premedicant administered by injection. The results indicate that midazolam i.m. is an effective premedicant, with few side-effects, for short procedures in general anaesthesia.
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PMID:Premedication with midazolam in out-patient general anaesthesia. A comparison with morphine-scopolamine and placebo. 288 53

Sumatriptan, a 5-HT1-receptor agonist has been shown to delay gastric emptying of liquids and solids in humans. However, no data are available of the effect of sumatriptan on gastric adaptation after distension with liquids and on symptoms induced by gastric distension. In 23 normal subjects and 30 dyspeptic patients with normal upper gastrointestinal endoscopy and real-time ultrasonography, the transverse gastric proximal and distal area and sagittal axis of the proximal stomach were determined by real-time ultrasonography and computed tomography after 500 ml of water. The area was determined by real-time ultrasonography and computed tomography twice at times 48 hr apart. Thirty minutes before real-time ultrasonography, placebo or sumatriptam were give subcutaneously in a double-blind fashion. Epigastric pain, bloating, heartburn, and nausea were also monitored through an intensity score from zero to 10 performed during the test. In six dyspeptic patients, the gastric distension was performed also with real-time ultrasonography and computed tomography after placebo and hyoscine butyl-bromide, a quaternary anticholinergic agent. Real-time ultrasonography and computed tomography demonstrated that after sumatriptan there is a reduction in proximal and distal transverse area and an increase in the sagittal axis of the proximal stomach. Hyoscine butyl-bromide increased all gastric measurements. Among the symptoms evaluated, only nausea was significantly reduced by sumatriptan (P < 0.01). Sumatriptan modifies gastric size, with a reduction in the transverse section and an increase of the sagittal axis of the proximal stomach and improves the nausea induced by gastric distension in dyspeptic patients.
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PMID:5-HT1-receptor agonist sumatriptan modifies gastric size after 500 ml of water in dyspeptic patients and normal subjects. 1245

Motion sickness is a common and distressing but poorly understood syndrome associated with nausea/vomiting and autonomic nervous system accompaniments that develops in the air or space as well as on sea or land. A bidirectional aetiologic link prevails between migraine and motion-sickness. Motion sickness provokes jerk nystagmus induced by both optokinetic and vestibular stimulation. Fixation of gaze or closure of eyes generally prevents motion sickness while vestibular otolithic function is eliminated in microgravity of space, indicating a predominant pathogenetic role for visuo-sensory input. Scopolamine, dimenhydrinate, and promethazine reduce motion-related nystagmus. Contraction of extraocular muscles generates proprioceptive neural traffic and can provoke an ocular hypertensive response. It is proposed that repetitive contractions of the extraocular muscles during motion-related jerk nystagmus rapidly augment brain stem afferent input by increasing proprioceptive neural traffic through connections of the oculomotor nerves with the ophthalmic nerve in the lateral wall of the cavernous sinus as well as by raising the intraocular pressure thereby stimulating anterior segment ocular trigeminal nerve fibers. This verifiable hypothesis defines the pathophysiological basis of individual susceptibility to motion sickness, elucidates the preventive mechanism of gaze fixation or ocular closure, advances the aetiologic link between MS and migraine, rationalizes the mechanism of known preventive drugs, and explores new therapeutic possibilities.
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PMID:Motion sickness is linked to nystagmus-related trigeminal brain stem input: a new hypothesis. 1582 12

Scopolamine (hyoscine) is commonly used as an anticholinergic drug to relieve nausea, vomiting and dizziness of a motion sickness as well as recovery from anesthesia and surgery. Sucrase as a hydrolytic enzyme breaks down sucrose into its monomers, glucose and fructose. The aim of this study was to evaluate the effect of scopolamine on the activity and the structural changes of yeast sucrase. The results showed that binding of scopolamine to sucrase could inhibit the enzyme activity. A non-competitive inhibition was observed in different concentrations of scopolamine (0.6 to 3.6mM). The study by circular dichroism measurement in far-UV showed that the absolute enzyme exhibited a flat negative trough, indicating the presence of alpha-helices and beta-sheet structures in the enzyme. Binding of the inhibitor on the enzyme made a deeper trough at 218nm, suggesting the increasing of beta-sheet content of the enzyme. Fluorescence measurement showed that binding of scopolamine to free enzyme and enzyme-substrate complex increased the peak intensity at 350nm and also induced red shift. Our findings suggest that scopolamine binds to the location other than the active site of enzyme and that the binding causes structural changes and inhibits the enzyme activity.
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PMID:Structural changes and inhibition of sucrase after binding of scopolamine. 2023 Aug 15

Nausea and vomiting is a common and troublesome symptom in advanced cancer. There have been different approaches described for the management of nausea and vomiting, specifically empirical and etiological. Scopolamine is listed in textbooks as a useful medication in management of nausea and vomiting in this setting, although there is no published data to support this recommendation. We present three cases that support the use of scopolamine in an etiologically based approach for management of nausea in advanced cancer.
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PMID:Scopolamine for cancer-related nausea and vomiting. 2061 16

Transdermal scopolamine, a patch system that delivers 1.5 mg of scopolamine gradually over 72 hours following an initial bolus, was approved in the United States in 2001 for the prevention of postoperative nausea and vomiting (PONV) in adults. Scopolamine (hyoscine) is a selective competitive anatagonist of muscarinic cholinergic receptors. Low serum concentrations of scopolamine produce an antiemetic effect. Transdermal scopolamine is effective in preventing PONV versus placebo [relative risk (RR)=0.77, 95% confidence interval (CI), 0.61-0.98, P = 0.03] and a significantly reduced risk for postoperative nausea (RR=0.59, 95% CI, 0.48-0.73, P < 0.001), postoperative vomiting (RR=0.68, 95% CI, 0.61-0.76, P < 0.001), and PONV (RR 0.73, 95% CI, 0.60-0.88, P = 001) in the first 24 hours after the start of anesthesia.
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PMID:Perspectives on transdermal scopolamine for the treatment of postoperative nausea and vomiting. 2260 91

Major depressive disorder is a common, but serious, psychiatric dysfunction that affects 21% of the population worldwide. Rolipram, a first-generation phosphodiesterase-4 (PDE4) inhibitor, has been shown to have significant antidepressant and cognitive enhancement effects; however, it was unsuccessful in clinic trials because of PDE4-dependent side effects such as nausea and emesis. In this study, we investigated the neuropharmacology of the novel PDE4 inhibitor chlorbipram and the classical PDE4 inhibitor rolipram. Using antidepressant-sensitive behavioral tests, we demonstrated that the acute single administration of chlorbipram (0.075-0.6 mg/kg) produced antidepressant-like effects, as evidenced by decreases in the duration of immobility in Kunming mice in the forced swim and tail suspension tests, and no significant changes in locomotor activity. Scopolamine-induced cognitive dysfunction was also significantly attenuated in the Morris water maze test after the treatment of Sprague Dawley rats with different doses of chlorbipram (0.5-1.5mg/kg). Furthermore, we evaluated the emetic potential of chlorbipram in beagle dogs. After oral administration, 0.5mg/kg rolipram showed emetic profiles in all dogs within 20 minutes, whereas chlorbipram did not induce any emesis during the 120-min observation period, even at the 1.0mg/kg dose. Together, our data suggest that chlorbipram is a novel antidepressant and cognitive enhancer with little or no emetic potency.
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PMID:Chlorbipram: a novel PDE4 inhibitor with improved safety as a potential antidepressant and cognitive enhancer. 2411 23

Motion sickness is a common syndrome that occurs upon exposure to certain types of motion. It is thought to be caused by conflict between the vestibular, visual, and other proprioceptive systems. Although nausea is the hallmark symptom, it is often preceded by stomach awareness, malaise, drowsiness, and irritability. Early self-diagnosis should be emphasized, and patients should be counseled about behavioral and pharmacologic strategies to prevent motion sickness before traveling. Patients should learn to identify situations that will lead to motion sickness and minimize the amount of unpleasant motion they are exposed to by avoiding difficult conditions while traveling or by positioning themselves in the most stable part of the vehicle. Slow, intermittent exposure to the motion can reduce symptoms. Other behavioral strategies include watching the true visual horizon, steering the vehicle, tilting their head into turns, or lying down with their eyes closed. Patients should also attempt to reduce other sources of physical, mental, and emotional discomfort. Scopolamine is a first-line medication for prevention of motion sickness and should be administered transdermally several hours before the anticipated motion exposure. First-generation antihistamines, although sedating, are also effective. Nonsedating antihistamines, ondansetron, and ginger root are not effective in the prevention and treatment of motion sickness.
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PMID:Prevention and treatment of motion sickness. 2507 1


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