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)

The three-step analgesic ladder, originally proposed for cancer pain relief by the World Health Organization (WHO), is now widely employed for all types of pain, including the chronic pain of musculoskeletal disease. Tramadol, an analgesic with weak opioid receptor affinity and possessing monoaminergic activity, has proved suitable for use at Step 2 of the WHO ladder. Owing to its pharmacological properties, tramadol is more appropriate than NSAIDs for patients suffering from gastrointestinal and renal problems. Importantly, the analgesic potency of tramadol is greater than that of NSAIDs and of other weak opioids (codeine, dextropropoxyphene). It also causes fewer opioid-type adverse effects, e.g. nausea, drowsiness, vomiting, dry mouth and constipation. In chronic musculoskeletal pain it is recommended that tramadol should be given by mouth and by the clock; the initial dose should be titrated upward gradually to reach the individual level required for suitable pain control. This dosage strategy will also minimise the usual opioid-type adverse effects encountered with tramadol. Four recent publications are reviewed to illustrate the efficacy of tramadol, alone or in conjunction with an NSAID, in the management of low back pain, osteoarthritis pain and breakthrough pain.
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PMID:Tramadol in musculoskeletal pain--a survey. 1195 1

We compared the antiemetic efficacy of tropisetron versus droperidol in women given tramadol after total hysterectomy. Forty patients were randomly allocated to group 1 (n = 20, tropisetron 0.05 mg/kg intravenously) or group 2 (n = 20, droperidol 15 micrograms/kg intravenously). Tramadol infusion (intravenously), for post-operative analgesia, was started at fascia closure. Incidences of post-operative nausea and vomiting, pain intensity, tramadol use, and the need for a rescue antiemetic (metoclopramide 10 mg) were recorded 0 h, 2 h, 6 h, 12 h, 24 h and 48 h post-operatively. Vomiting and nausea incidences were reported fewer in group 1 than in group 2, but statistical significance was only reached for vomiting incidence 6 h post-operation. Tropisetron seems to have better antiemetic properties than droperidol in patients receiving tramadol because of the length of its duration of action. Further studies, investigating alternative ways of managing post-operative nausea and vomiting, and the use of tramadol for post-operative analgesia, are needed.
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PMID:Comparison of the antiemetic efficacy of tropisetron and droperidol with patient-given tramadol. 1296 1

(1) First-line treatment for both acute and chronic pain is paracetamol or, if necessary, ibuprofen, a nonsteroidal antiinflammatory drug. If relief is inadequate, the best option is a combination of paracetamol with codeine (a weak opiate). (2) A fixed-dose combination of paracetamol (325 mg) and tramadol (37.5 mg), a weak opiate, arrived on the French market in May 2003. (3) In the acute setting, three trials in a total of 1197 patients showed that a single dose of the paracetamol 650 mg + tramadol 75 mg combination after dental surgery was no more effective than ibuprofen 400 mg. Compared with each drug used alone, the paracetamol + tramadol combination prolongs the analgesic effect but does not increase its intensity. (4) A trial after gynaecological surgery and another trial after orthopaedic surgery showed that a single dose of paracetamol 975 mg + tramadol 112.5 mg had similar efficacy to tramadol alone at 112.5 mg. (5) In the chronic setting, we found no trials comparing the paracetamol + tramadol combination with each drug used alone. A comparative double-blind trial in 462 patients with low back pain or osteoarthritic pain showed no difference in efficacy between paracetamol 325 mg + tramadol 37.5 mg and paracetamol 300 mg + codeine 30 mg. (6) The main adverse effects of the paracetamol + tramadol combination are the same as other weak opiates: nausea, vomiting, dizziness, headache, drowsiness and constipation. Tramadol carries a higher risk of drug interactions than codeine. (7) In practice, the paracetamol + tramadol combination offers patients no advantages relative to standard analgesics.
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PMID:Paracetamol + tramadol: new preparation. No advance. 1498 89

The objective of this study was to compare the analgesic efficacy of tramadol/acetaminophen (APAP) (total dose 75 mg/650 mg) and tramadol (total dose 100 mg) for the control of pain after oral surgery. A total of 456 patients with moderate-to-severe pain within 5 h after extraction of two or more third molars were randomized to receive two identical encapsulated tablets containing tramadol/APAP 37.5 mg/325 mg, tramadol 50 mg, or placebo. Tramadol/APAP was superior to tramadol (P < 0.001) or placebo (P < 0.001) on all efficacy measures: total pain relief (PAR) over 6 h (7.4, 2.5, and 1.5, respectively, on a scale of 0-24); sum of pain intensity differences (PIDs) (3.1, 0.6, and 0.1, respectively, on a scale of -6 to 18); and sum of PAR and PID (10.5, 3.1, and 1.6, respectively, on a scale of -6 to 42). Median times to onset of perceptible and meaningful PAR were 37.6 and 126.5 min, respectively, for the tramadol/APAP group (P < 0.001) for each, compared with tramadol and placebo arms). The most common adverse events with active treatment were nausea, dizziness, and vomiting; these events occurred more frequently in the tramadol group than in the tramadol/APAP group. This study established the superiority of tramadol/APAP 75 mg/650 mg over tramadol 100 mg in the treatment of acute pain following oral surgery.
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PMID:A double-blind placebo-controlled comparison of tramadol/acetaminophen and tramadol in patients with postoperative dental pain. 1515 85

Tramadol is a centrally acting analgesic with weak opioid agonist properties, which also has monoaminergic activity, exerted via inhibition of neuronal uptake of serotonin and norepinephrine. Tramadol is generally well tolerated and the most common adverse events are nausea, dizziness, drowsiness, sweating, vomiting and dry mouth. Currently it was examined by which principal mechanism tramadol induces oral dryness. The effects of intravenous administration (+/-)-tramadol were studied in rats on the flow of saliva in response to a peripheral cholinergic stimulus or to reflex activation involving the relay of impulses in the central nervous system. In pentobarbitone-anaesthetized rats, the salivary secretion to acetylcholine (0.1-10 micromol/kg IV) was increased by up to 110% by tramadol (1-5 mg/kg IV) and the protein concentration therein by up to 400%. The administration alpha- and beta-adrenoceptor antagonists resulted in almost identical acetylcholine-evoked responses as in the absence of tramadol. The secretory response to the application of citric acid on the tongue of the rat was reduced by 38% and by 64%, respectively, at 5 and 10 mg/kg IV of tramadol (p < 0.05-0.01). Thus, tramadol exerts its principal xerogenic effect by activating inhibitory pathways in the central nervous system and has no anticholinergic effect on the salivary glands at dosages that may be clinically relevant. Furthermore, the tramadol-induced increase of the acetylcholine-evoked secretion occurred at a glandular level and depended most likely on a release of noradrenaline from glandular nerve terminals.
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PMID:The xerogenic potency and mechanism of action of tramadol inhibition of salivary secretion in rats. 1548 38

Tramadol is a synthetic opioid that has been available in the Netherlands since 1992 and is usually used as a centrally-acting analgesic when paracetamol or an NSAID provides insufficient relief. In the period 1 January 1992--30 November 2003, the Netherlands Pharmacovigilance Centre Lareb received 299 reports concerning 522 adverse drug reactions associated with the use of tramadol. Some of the frequently reported side effects with a high reporting odds ratio were nausea, constipation and withdrawal symptoms. These side effects are very similar to those of the other opioids due to the affinity of tramadol for the micro-opioid receptor. Because tramadol is often not recognised as an opioid, it is important that such opiate effects be recognised as an adverse drug reaction on time.
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PMID:[Side effects of tramadol: 12 years of experience in the Netherlands]. 1583 26

Anxiolytic drugs are widely used for premedication in oral surgery. Since anxiety is usually associated with the fear of pain, we tested the effects of the analgesic tramadol in premedication before operative extraction of the mandibular third molar under local anesthesia. In a double-blind crossover study, 20 patients were randomized to receive 100 mg oral tramadol or placebo 1 h before operation. Anxiety, nausea, dryness of the mouth, pain and discomfort were recorded before administration of the drug, immediately before and after operation, and 0.5, 1, and 2 h postoperatively using ungraded 0-100 mm VAS scales. Blood pressure and heart rate were measured at the same times; vigilance was tested using the Maddox Wing Test and sensorimotor performance using the Trieger Dot Test; hemoglobin oxygen saturation (SpO2) was measured using a pulse oximeter. In addition, SpO2 and heart rate were recorded continuously in nine patients using a pulse oximeter connected to a computer. The surgeon assessed the quality of operating conditions on the VAS scale. Tramadol delayed and decreased the need of analgesics on the day of operation (p < 0.05). The operating conditions were better in patients on tramadol premedication than in those on placebo during the first operation (p < 0.05), but no differences were seen in patient well-being between treatments. The second operation was less stressful than the first. Tramadol is recommended only with special indications for premedication of patients undergoing third molar extraction under local anesthesia.
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PMID:Tramadol premedication in operative extraction of the mandibular third molar: a placebo-controlled crossover study. 1609 62

Terminally ill cancer patients commonly suffer from several symptoms at the same time, such as pain, nausea, anxiety, cognitive failure, bowel obstruction, and fatigue. To obtain optimal symptom control, the simultaneous administration of more than one drug by continuous subcutaneous (SC) infusion is often required. Tramadol is considered an effective step II agent of the World Health Organization's analgesic ladder for the control of chronic pain conditions, including neuropathic pain, and also exhibits a good safety profile. Haloperidol has been found to be very efficient in controlling agitation with or without pain, nausea and/or vomiting of central origin, intestinal obstruction, and delirium. Although the combination of tramadol and haloperidol in the same solution for SC infusion may be desirable, the physicochemical stability of this combination has not yet been documented. Therefore, our aim was to study the physicochemical stability of drug admixtures composed of tramadol hydrochloride and haloperidol lactate, which have been stored in polypropylene syringes at 4 degrees C and 25 degrees C, and assayed at 0, 5, 7, and 15 days after preparation.
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PMID:Stability of tramadol and haloperidol for continuous subcutaneous infusion at home. 1612 35

Tramadol is a synthetic, centrally acting analgesic. A sustained-release (SR) capsule formulation of tramadol gradually releases active drug, allowing for twice-daily dosing. Compared with tramadol SR tablets, tramadol SR capsules produced a smoother plasma concentration profile, with more gradual absorption and lower peak concentrations. There was less intra- and intersubject variability in tramadol plasma concentrations with SR capsules versus SR. Tramadol SR capsules had identical bioavailability to tramadol immediate-release (IR) capsules with lower peak concentrations and less fluctuation in plasma concentrations. Tramadol SR 100 mg capsules administered twice daily had equivalent efficacy to tramadol IR 50 mg capsules administered four times daily in the treatment of moderate to severe chronic low back pain in a well designed study. Patients receiving tramadol SR capsules were significantly less likely than those receiving tramadol IR capsules to report nausea. Starting treatment with tramadol SR capsules at a dosage of 50 mg twice daily with subsequent dose escalation resulted in improved tolerability in patients with moderate to severe chronic pain. The lowest tramadol SR capsule dosage of 50 mg twice daily (administered to 35% of patients with moderate to severe non-oncological pain) significantly improved pain intensity and frequency in 83.4% and 70.4% of patients, respectively, in a postmarketing observational study evaluating tramadol SR capsules 50-200 mg twice daily (n = 3888).
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PMID:Tramadol sustained-release capsules. 1645 Oct 97

Tramadol, a centrally acting analgesic, consists of two enantiomers, both of which contribute to analgesic activity via different mechanisms. (+) Tramadol and the metabolite (+) -O- desmethyl-tramadol (M1) are agonists of the mu opioid receptor. (+) Tramadol also stimulates presinaptic release of serotonin and inhibits serotonin reuptake whereas (-) tramadol inhibits norepinephrine reuptake. Thus tramadol enhances inhibitory effects on pain transmission both by opioid and monoaminergic mechanisms. The complementary and synergistic actions of the two enantiomers improve the analgesic efficacy and tolerability profile of the racemate. Following oral administration the bioavailability of tramadol is high and with new slow release preparations twice daily administration enables effective pain control. The recommended maximum daily dose of tramadol is 400 mg/day. Tramadol is characterised by low plasma protein binding and quite extensive tissue distribution. Elimination is primarily by the hepatic route (metabolism by CYP2D6) and partly by the renal route. It is effective in different types of moderate-to-severe acute and chronic pain, including neuropathic pain, low back pain, osteoarthritis pain and breakthrough pain. It also causes fewer opioid-type adverse effects, e.g. nausea, drowsiness, vomiting, dry mouth and constipation. Although trials in literature demonstrate immune-stimulating effects of tramadol, there are also trials suggesting immunesuppressive effects that are lesser than morphine. Owing to its pharmacological properties, tramadol is more appropriate than NSAIDs for patients suffering from gastrointestinal and renal problems. Besides its proven clinical efficacy tramadol is a safe drug as respiratory depression, cardiovascular side effects, drug abuse and dependence are of minor clinical relevance, unlike some other opioids.
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PMID:[An atypical opioid analgesic: tramadol]. 1678 63


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