Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: UMLS:C0344307 (analgesia)
 28,200 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Tramadol hydrochloride produced dose-related antinociception in mouse abdominal constriction [ED50 = 1.9 (1.2-2.6) mg/kg i.p.], hot-plate [48 degrees C, ED50 = 21.4 (18.4-25.3) mg/kg s.c.; 55 degrees C, ED50 = 33.1 (28.2-39.1) mg/kg s.c.] and tail-flick [ED50 = 22.8 (19.2-30.1) mg/kg s.c.] tests. Tramadol also displayed antinociceptive activity in the rat air-induced abdominal constriction [ED50 = 1.7 (0.7-3.2) mg/kg p.o.] and hot-plate [51 degrees C, ED50 = 19.5 (10.3-27.5) mg/kg i.p.] tests. The antinociceptive activity of tramadol in the mouse tail-flick test was completely antagonized by naloxone, suggesting an opioid mechanism of action. Consistent with this, tramadol bound with modest affinity to opioid mu receptors and with weak affinity to delta and kappa receptors, with Ki values of 2.1, 57.6 and 42.7 microM, respectively. The pA2 value for naloxone obtained with tramadol in the mouse tail-flick test was 7.76 and was not statistically different from that obtained with morphine (7.94). In CXBK mice, tramadol, like morphine, was devoid of antinociceptive activity after intracerebroventricular administration, suggesting that the opioid component of tramadol-induced antinociception is mediated by the mu-opioid receptor. In contrast to the mouse tail-flick test and unlike morphine or codeine, tramadol-induced antinociception in the mouse abdominal constriction, mouse hot-plate (48 degrees or 55 degrees C) or rat hot-plate tests was only partially antagonized by naloxone, implicating a nonopioid component. Further examination of the neurochemical profile of tramadol revealed that, unlike morphine, it also inhibited the uptake of norepinephrine (Ki = 0.79 microM) and serotonin (0.99 microM). The possibility that this additional activity contributes to the antinociceptive activity of tramadol was supported by the finding that systemically administered yohimbine or ritanserin blocked the antinociception produced by intrathecal administration of tramadol, but not morphine, in the rat tail-flick test. These results suggest that tramadol-induced antinociception is mediated by opioid (mu) and nonopioid (inhibition of monoamine uptake) mechanisms. This hypothesis is consistent with the clinical experience of a wide separation between analgesia and typical opioid side effects.
 ...
PMID:Opioid and nonopioid components independently contribute to the mechanism of action of tramadol, an 'atypical' opioid analgesic. 130 73

Tramadol hydrochloride is a synthetic opiate agonist with a plasma elimination half-life of 5 to 6 hours and peak plasma levels at about 1 1/2 hours. It derives its activity from attachment to the mu-receptor and blockage of norepinephrine reuptake. The purpose of this single-dose, double-blind, placebo-controlled study was to determine the analgesic effectiveness of an oral administration of two dose levels of tramadol hydrochloride (75 or 150 mg) compared with the combination of 650 mg acetaminophen plus 100 mg propoxyphene napsylate in 161 patients with severe postoperative pain after cesarean section. Analgesia was assessed over a 6-hour period. Treatments were compared on the basis of standard scales for pain intensity and relief and a number of derived variables based on these data. A global rating of the study medication was also used to compare treatments. The three active treatments were effective analgesics, statistically superior to placebo for many hourly and summary measures. A dose response was seen between the two tramadol doses, with the 150 mg dose providing significantly greater analgesia over the lower dose. The 75 mg dose of tramadol was generally more effective than the acetaminophen-propoxyphene combination after hour 2, and significantly so for some hourly time points, as well as for the global rating of the medication. The 150 mg dose of tramadol was significantly more effective than the acetaminophen-propoxyphene combination from hour 2 through hour 6 for the sum of pain intensity differences and total pain relief scores, as well as for the global rating of the medication. Tramadol hydrochloride at both dose levels is an effective analgesic agent and at 150 mg is statistically superior to the acetaminophen-propoxyphene combination. No serious adverse effects were observed; however, dizziness was more frequently reported with 150 mg tramadol.
 ...
PMID:Analgesic oral efficacy of tramadol hydrochloride in postoperative pain. 135 4

Opioid analgesics were used in 282 patients on the first-third day after heart, lung and abdominal surgery. The main indication for their use was pain syndrome. Adequate analgesia with tramal, nubain and moradol was noted in 73, 76 and 81% of cases. In marked pain syndrome after thoracotomy the most effective agents were moradol and morphine. Computer monitoring of the respiratory function in tramal analgesia has shown a decrease in lung ventilation, esophageal pressure, inhalation volume, O2 production. Tramal, nubain and moradol in analgesic doses did not inhibit respiration. In adequate analgesia there was a decrease in lung ventilation which was not accompanied by shifts in acid-base balance of the arterial blood. The above analgesics had no considerable effect on systemic hemodynamics, though the use of tramal decreased systemic blood pressure and the use of moradol decreased systemic blood pressure and total peripheral vascular resistance. Tramal was most effective for synchronization of spontaneous respiration with a lung ventilation device in prolonged ventilation, as well as for the arrest of muscular tremor in the postoperative period. Tramal was effective in 95% of patients in the early post-anesthesia and postoperative period.
 ...
PMID:[Clinical aspects of the use of nubain, tramal and moradol in patients in the early postoperative period]. 141 95

In a multicenter study 153 in- and outpatients suffering from severe pain were treated for three weeks with capsules containing 50 mg 1-(m-methoxyphenyl)-2-(dimethylaminomethyl)-cyclohexan-1-ol (tramadol, Tramal). The daily dosage was limited to 400 mg. At the end of the third week the patients received in a randomized double-blind manner 1.6 mg naloxone or saline (both i.m.) to evaluate the risk of developing dependence during the 3-week tramadol treatment (precipitation test). A total of 109 patients completed the trial. Development of tolerance was not observed as was evident from a constant daily tramadol dose associated with constant analgesia. The median net withdrawal scores for the naloxone treated group (mean = 0, Xmin = 0, Xmax = 13) and for the saline treated group (mean = 0, Xmin = 0, Xmax = 5) indicate absence of dependence. The outcome of the study thus suggests that tramadol under the conditions described does not induce dependence.
 ...
PMID:Clinical investigation on the development of dependence during oral therapy with tramadol. 409 74

Parenteral analgesia with Tramal was performed in 23 normal deliveries. The results were compared with a group of normal deliveries in which analgesia was achieved with pethidine. Both medicaments excerted an identical analgetic efficiency. No adverse side effects were observed with Tramal concerning the follow-up of labour or the newborn. Tramal can be recommended for obstetrical analgesia since it does not excert inhibitory effects upon the respiratory center.
 ...
PMID:[Obstetrical analgesia with tramadol]. 739 Mar 76

Oxygen regimen, hemodynamics, hemocoagulation, vegetative status, and immune status of patients subjected to multiple surgical interventions under anesthesia are analyzed. Three premedication schemes are considered. Routine fluothane anesthesia with nitrogen oxide + oxygen or calypsol after standard premedication is inadequate in children when used repeatedly. Tramal, a new analgesic, used in premedication, is highly effective, causes no side effects, and ensures sufficiently deep and prolonged analgesia. Use of neurovegetative blocking for premedication is a new and most physiological method of analgesia to be used in multiple minor surgical interventions in patients with burns.
 ...
PMID:[Comparative analysis of different premedication methods in minor surgery in children]. 760 33

The problem of postoperative pain remains actual despite the existence of a variety of pharmaceutical and nonpharmaceutical methods of anesthesia. Acute postoperative pain is an essential component of the surgical stress syndrome. Opioid analgetics (Buprenorfin, Nubain, Tramal, Promedol, Morphine) take the leading position among other types of analgetics. Present-day individual approach to administration of analgetics is still imperfect. The use of a standard dose of analgetics appears to be inadequate in a number of patients. The increase of opioids dose may lead to adverse reactions. In view of this it is valid to use nonsteroid antinflammatory medicines (Ketorolac). The choice of a proper dose of an analgetic is critically important in achieving adequate anesthesia. Patient-controlled analgesia (PCA) or "analgesia on demand" is an alternative to administration of analgetics. The major advantage of PCA is the opportunity to achieve the rate of analgesia, according to individual demand of a patient. Besides, PCA allows to reach the desired effect much faster and to maintain the stable plasma level of an analgetic. 2-year experience of the PCA use in more than 200 patients of the National Research Centre for Surgery ICU has been analysed. The authors advocate use of PCA in clinical practice.
 ...
PMID:[The problem of acute pain in postoperative period]. 901 53

Tramadol hydrochloride is a novel, centrally acting analgesic with two complementary mechanisms of action: opioid and aminergic. Relative to codeine, tramadol has similar analgesic properties but may have fewer constipating, euphoric, and respiratory depressant effects. A two-center randomized double-blind controlled clinical trial was performed to assess the analgesic efficacy and reported side effects of tramadol 100 mg, tramadol 50 mg, codeine 60 mg, aspirin (ASA) 650 mg with codeine 60 mg, and placebo. Using a third molar extraction pain model, 200 healthy subjects were enrolled in a 6-hour evaluation after a single dose of drug. Of the 200 patients enrolled, seven provided incomplete efficacy data or discontinued prematurely and one was lost to follow-up. Using standard measures of analgesia, including total pain relief score (TOTPAR), maximum pain relief score (MaxPAR), sum of pain intensity difference scores (SPID), peak pain intensity difference (Peak PID), remedication, and global evaluations, all active treatments were found to be numerically superior to placebo. ASA/codeine was found to be statistically superior to placebo for all measures of efficacy. Tramadol 100 mg was statistically superior to placebo for TOTPAR, SPID, and time of remedication, whereas tramadol 50 mg was statistically superior to placebo onlyfor remedication time. Codeine was not found to be statistically superior to placebo for any efficacy measure. A greater TOTPAR response compared with all other active measures was seen for ASA/codeine during the first 3 hours of study. The 6-hour TOTPAR scores for the tramadol groups and ASA/ codeine group were not significantly different. Gastrointestinal side effects (nausea, dysphagia, vomiting) were reported more frequently with tramadol 100 mg, ASA/ codeine, and codeine 60 mg than with placebo.
 ...
PMID:Tramadol hydrochloride: analgesic efficacy compared with codeine, aspirin with codeine, and placebo after dental extraction. 965 May 46

Tramadol hydrochloride is an analgesic with mu receptor activity suitable for administration to children as oral drops. As the serum concentration profile and pharmacokinetic parameters in young children are not known via this route, we studied 24 healthy ASA 1 children to determine those parameters. The children's mean age was 5.3 +/- 1.1 years and their mean weight was 17.8 +/- 3.1 kg. They underwent general anesthesia with sevoflurane for dental surgery. The mean duration of anesthesia was 27.9 +/- 10.1 minutes. Tramadol 1.5 mg/kg (this dose was chosen because we have previously shown it to be effective in providing analgesia following pediatric dental surgery) was administered as oral drops 30 minutes before anesthesia. Venous blood samples were taken following the tramadol at 30-minute intervals for 4 hours, every 2 hours for 6 hours, and every 4 hours for 12 hours. The samples were centrifuged and the serum stored at -20 degrees C, and nonstereoselective gas chromatography was used to determine the concentration of (+) and (-) tramadol enantiomers plus their o-demethyltramadol (M1) metabolite concentrations. The tramadol absorption was rapid, the maximum measured serum concentration present occurring before the first sample at 30 minutes. That first sample had a concentration of 352 +/- 83.4 ng/mL. The concentration remained above the 100 ng/mL analgesic level until 6.8 +/- 0.9 hours. The elimination half-life was 3.6 +/- 1.1 hours, the serum clearance 5.6 +/- 2.7 mL/kg/min, and the volume of distribution 4.1 +/- 1.2 L/kg. The (+) enantiomer concentration was 14.2 +/- 4.9% greater than that of the (-) enantiomer. The M1 metabolites had a (-) enantiomer concentration 92.3 +/- 75.1% greater than the (+) enantiomer. From the peak concentration at 4.5 +/- 1.5 hours, the concentration of the metabolite was approximately one third that of the parent drug. The M1 elimination half-life was 5.8 +/- 1.7 hours. Apart from the rapid rise in the serum concentration, these kinetic parameters are similar to those seen in healthy young adults. The concentration profile supports an effective clinical duration in the region of 7 hours.
 ...
PMID:Pharmacokinetics of oral tramadol drops for postoperative pain relief in children aged 4 to 7 years--a pilot study. 1277 11

Patients taking celecoxib (Celebrex) because they cannot tolerate the GI effects of nonspecific NSAIDs could continue to do so, but should not exceed recommended dosage. For analgesia and osteoarthritis, acetaminophen (Tylenol, and others) or tramadol (Ultram, and others) are reasonable alternatives to NSAIDS. For rheumatoid arthritis, disease-modifying drugs (DMARDs) can be used.
 ...
PMID:NSAID alternatives. 1564 6


1 2 Next >>