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)

Oxilorphan (levo-BC-2605) is a new, long-acting, narcotic antagonist that has agonist properties. Twenty-one (21) heroin addicts in Los Angeles were detoxified and given at least one oral dose of oxilorphan. Only three (14.3%) patients took daily doses for 14 days, which was the maximal time allowed for oxilorphan administration in this study. The remainder discontinued oxilorphan because of subjective side effects or for unknown reasons. Side effects most responsible for dropouts were dysphoria, insomnia, weakness, hallucinations, nausea, drowsiness and anorexia. Oxilorphan provided 24-hour protection with a single, oral dose, but subjective side effects encountered during inductiolinical trials with oxilorphan should be attempted with other addict populations to fully determine its potential therapeutic value.
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PMID:Clinical trial in post-addicts with oxilorphan (levo-BC-2605): a new narcotic antagonist. 1 84

In 10 healthy male volunteers breathing 100% oxygen, we determined the effect of four intravenous dose levels of fentanyl (0.0015, 0.003, 0.006 and 0.009 mg/kg) and two of fentanyl plus droperidol (i.e., Innovar, 0.003 and 0.006 mg/kg of fentanyl with 2.5 mg of droperidol for each 0.05 mg of fentanyl) on PECO2 and the slope of the ventilatory response to imposed increases in PECO2. All doses of fentanyl and fentanyl plus droperidol depressed the slope and shifted the curve to the right. Depression was dose related and was maximum 5 minutes after administration. The slope returned to control by 2 hours postinjection even at the highest narcotic dose. However, the rightward shift of the CO2 response curve require 4 hours to return to control. Droperidol added to fentanyl did not increase or prolong the respiratory depression seen with fentanyl alone at equivalent dose levels. Nausea and emesis occurred more frequently with fentanyl alone and orthostatic hypotension occurred more frequently with droperidol plus fentanyl. Dysphoria was a prominent consequence of fentanyl plus droperidol administration.
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PMID:The magnitude and duration of respiratory depression produced by fentanyl and fentanyl plus droperidol in man. 97 96

To determine whether administration of nitrous oxide, 50% and 70%, could provide analgesia and anxiolysis during venous cannulation in pediatric patients, 165 ASA Physical Status 1 patients scheduled for elective surgery were studied. Children, 3 weeks to 18 yr of age, were randomly assigned either to receive nitrous oxide, 50% or 70% in oxygen, or 100% oxygen via mask or to a group breathing room air, for 3 min prior to and during venous cannulation. A blinded observer using a behavioral scale for rating pain in children performed assessments of behavior and pain before and following venous cannulation. Children who received 50% or 70% nitrous oxide were more likely to be relaxed, 59% and 84%, respectively, and had little evidence of pain. Of those given 100% oxygen or no mask, only 30% and 21%, respectively, were considered relaxed, and 16% and 15% had little evidence of pain during venous cannulation. Side effects were seen in 28% of the group given 70% nitrous oxide and included excitement, dysphoria, nausea, restlessness, and opisthotonic movements. Both 50% and 70% nitrous oxide in oxygen administered to pediatric patients are effective at decreasing the pain and anxiety associated with venous cannulation, but use of the latter is associated with side effects.
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PMID:Administration of nitrous oxide to pediatric patients provides analgesia for venous cannulation. 240 40

The opioid agonist-antagonists are a heterogeneous group of compounds capable of providing analgesia sufficient to treat moderate to severe acute pain. Pentazocine, butorphanol and nalbuphine produce subjective effects which are quite different from those of morphine. Lack of mood elevation and occasional dysphoria may contribute to a lower level of patient acceptance, but all of these analgesics are significantly safer than the pure agonists. Doses in the therapeutic range are unlikely to produce dangerous levels of respiratory depression in most patients. Other opioid side-effects such as nausea, constipation and biliary spasm appear to be less frequent as well. The mu partial agonist buprenorphine shares many of the safety advantages of the older drugs, and its subjective effects appear more morphine-like. It is not clear whether mu partial agonists have real clinical advantages over kappa-type analgesics. All of these drugs are opioid antagonists and are able to precipitate abstinence in individuals with significant prior exposure to opiates. Neither absolute potency nor the ratio of agonist to antagonist effect are predictors of therapeutic usefulness. There is now an enormous amount of clinical experience with the agonist-antagonists. In many, but not all, clinical situations they are acceptable alternatives to the morphine-like drugs.
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PMID:The clinical usefulness of agonist-antagonist analgesics in acute pain. 289 87

In a randomized, prospective, double-blind trial we investigated the efficacy and safety of the benzodiazepine antagonist RO 15-1788 in 57 patients undergoing general surgery. Anesthesia was induced and maintained by a combination of Flunitrazepam-Fentanyl-Pancuronium. Inhalation anesthetics were excluded from the study. After reversal of any residual relaxant effect we titrated RO 15-1788 or placebo by repeated i.v. administration of 0.1 mg (= 1.0 ml) up to a maximum dosage of 1.0 mg or to a definite arousal reaction. Before as well as 5, 10, 15, 30, 60, and 120 min after injection of the trial substance we evaluated efficacy (sedation, comprehension and collaboration, orientation in time and space), presence of anterograde amnesia, side-effects, hemodynamics, and subjective patient assessment by a point scale. RO 15-1788 significantly improved the level of consciousness (P less than 0.005) at a dosage of 0.59 +/- 0.29 mg at 5, 15, 30, and 60 min after administration as well as orientation in time and space (P less than 0.005) after 30 min. There was significantly less anterograde amnesia (P less than 0.005) after 15, 30, and 60 min. Symptoms of a benzodiazepine rebound effect after 120 min indicate a short half-life time of RO 15-1788. We did not observe any hemodynamic side effects. Local tolerance was good. Side effects in terms of nausea (1 case), vomiting (4), euphoria or dysphoria (2), benign cardiac arrhythmias (1) or a state of excitation (1) occurred several times after RO 15-1788 as well as after placebo (nausea 2, vomiting 6, muscular tremor 1). Our results indicate the efficacy and safety of RO 15-1788.
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PMID:[Efficacy and safety of the benzodiazepine antagonist RO 15-1788]. 313 35

1. This double-blind, random-order study was designed to compare the clinical effects and the plasma catecholamine responses after i.v. administration of meptazinol at doses 0.7 and 1.4 mg kg-1, pentazocine at doses 0.3 and 0.6 mg kg-1 and saline placebo to six healthy volunteers. 2. Mean arterial pressure was not affected by either drug. Heart rate showed slight drug-related changes. Respiratory rate fell slightly with both drugs, but independently of dose. 3. The critical flicker fusion threshold-test and Maddox wing readings could both clearly differentiate active drugs from placebo. Meptazinol caused more nausea and dysphoria as expressed with visual analogue scales. Both analgesics caused short-lived feelings of euphoria. 4. After pentazocine plasma noradrenaline increased almost two-fold in 10-20 min. The effect of meptazinol was slightly smaller, whereas meptazinol caused a pronounced increase in plasma adrenaline concentrations in two of six subjects. Pentazocine had a smaller, but significant effect on plasma adrenaline. 5. We conclude that the effects of meptazinol in healthy volunteers do not differ markedly from those of pentazocine, although it may cause more nausea and dysphoria. The pronounced increase in plasma adrenaline concentrations in two of six subjects calls for caution in its use in patients with cardiac diseases.
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PMID:Meptazinol and pentazocine: plasma catecholamines and other effects in healthy volunteers. 344 93

An oral formulation of meptazinol has been developed and marketed in the United Kingdom. The 200 mg tablet has a potency similar to dextropropoxyphene 32.5 mg/paracetamol 325 mg or pentazocine 50 mg. Nausea is the major side effect and constipation and dysphoria are virtually absent. Though a variable first pass metabolism restricts its potential for use in severe pain, oral meptazinol provides effective analgesia in mild or moderate pain.
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PMID:Oral meptazinol--United Kingdom experience. 390 33

In a randomized cross-over study on sedation in outpatient oral surgery, subcutaneous administration of morphine-scopolamine was compared with rectal administration of diazepam. The mean dose of morphine was 0.13 mg kg-1 (range 0.13-0.24) and of diazepam 0.57 mg kg-1 (range 0.50-0.71). Apprehension, the determining factor for patients' preference for sedation method, the recovery from sedation and the postoperative course were studied. Both methods produced the desired effects. For diazepam, the effect was scored higher by the patient than the nurse observer and for morphine-scopolamine the opposite was found. Postoperative pain and patients' preference for sedation did not differ between the methods and the determining factor for the patients' preference for sedation method was the experience of stronger tranquilization. Side-effects such as prolonged recovery, nausea, dizziness, and dysphoria were frequent during the postoperative course after the morphine-scopolamine sedation but were not seen during diazepam sedation. Thus, rectal administration of diazepam should be preferred to morphine and scopolamine for sedation in minor oral surgery performed under local anesthesia.
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PMID:Comparison of rectal diazepam and subcutaneous morphine-scopolamine administration for outpatient sedation in minor oral surgery. 407 91

Opioid analgesics continue to be the most important drugs in modifying the response to pain. Their versatility is attested by their frequent use in both postoperative and intraoperative management of pain. Recent findings regarding the mechanism of action of opioids may signal the introduction of newer, more effective, and less addictive agents. So far, this has not occurred. However, opioids with mixed agonist-antagonist properties have offered some utility. The adverse effects of nausea and dysphoria and the more serious effects of respiratory depression continue to be a problem, as does the possibility of abuse. Nonetheless, the clinical experience with opioids in control of pain is uncontested. Until better drugs are developed, opioids will form the basis for the control of acute pain by the dental practitioner.
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PMID:Clinical pharmacology of opioid analgesics. 614 39

The space adaptation syndrome is one of the more vexing problems confronted by our nation's astronauts during their journeys. This syndrome may be a variant of motion sickness, although this possibility has been questioned. Physostigmine, a centrally active cholinesterase inhibitor which increases brain acetylcholine, was found to cause a motion sickness-like syndrome--in psychiatric patients and normals--including nausea, emesis, malaise, dysphoria, increases in serum ACTH, beta-endorphin, cortisol, and prolactin, Neostigmine, a non-centrally acting cholinesterase inhibitor, and saline placebo caused no such effects. The above effects closely parallel those of motion sickness. Thus, the effects of physostigmine may be a convenient model for screening for treatments for motion sickness or space adaptation syndrome, or for predicting who will develop these syndromes.
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PMID:A cholinomimetic model of motion sickness and space adaptation syndrome. 648 3


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