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

Antinociception by nonsteroidal antiinflammatory drugs, notably diclofenac and S(+)-ibuprofen, has traditionally been attributed to peripheral tissue cyclooxygenase inhibition. This study investigates the potential role of the nitric oxide system for the central antinociceptive effects of diclofenac, S(+)-, and R(-)-ibuprofen. Diclofenac and S(+)- but not R(-)-ibuprofen inhibited the behavioral response dose dependently, "biting, scratching, and licking (BSL)," induced by the spinal application of N-methyl-D-aspartate, but not that of amino-methylisoxazole-propionic acid or substance P. Diclofenac and S(+)-ibuprofen induced a parallel shift in the number of BSL responses and in the duration of the response in the behavioral model at their approximate median effective doses (diclofenac 1 mumol and S(+)-ibuprofen 5 mumol). Pretreatment with L-arginine, the natural substrate for the nitric oxide synthetase, antagonized diclofenac, and S(+)-ibuprofen-induced suppression of the biting, scratching, and licking response evoked by intrathecal N-methyl-D-aspartate. D-arginine did not antagonize the diclofenac- and S(+)-ibuprofen-induced antinociception. The study results indicate that analgesia after diclofenac and S(+)-ibuprofen involves a central mechanism which may add to the peripheral antinociceptive effect of these agents. The central action of diclofenac and S(+)-ibuprofen is partly mediated by an interaction with the N-methyl-D-aspartate receptor and nitric oxide-generating mechanisms.
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PMID:Nonsteroidal antiinflammatory drug modulation of behavioral responses to intrathecal N-methyl-D-aspartate, but not to substance P and amino-methyl-isoxazole-propionic acid in the rat. 901 80

Diclofenac in hyaluronan is analgesic and angiostatic. The depletion of substance P may be a common mechanism. Mice received diclofenac, diclofenac in hyaluronan, or saline i.v. for 5 days and snout substance P assessed: saline 2.80 +/- 0.23; 0.5 mg/kg diclofenac 2.03 +/- 0.20 (P < 0.05); diclofenac in hyaluronan 1.88 +/- 0.21 (P < 0.02); capsaicin 1.45 +/- 0.26 fmol/mg tissue (P < 0.005). Substance P recovered by 5 days (diclofenac in hyaluronan, capsaicin) and 24 h (diclofenac). Diclofenac may deplete substance P in analgesia, and hyaluronan prolong the depletion.
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PMID:The depletion of substance P by diclofenac in the mouse. 916 75

This study investigated the opioid-sparing effect of diclofenac using patient-controlled analgesia with oral methadone. Fifteen patients with advanced cancer participated. After achieving adequate analgesia with regular dosing of oral methadone (T1), patient-controlled analgesia with methadone was administered for 3 days (T2). Intramuscular diclofenac 75 mg twice daily was then added to this regimen for 3 days (T3). Compared to T2 values, methadone dose was significantly reduced at T2 and T2, and pain report (recorded on a visual analogue scale) was significantly reduced at T3. A reduction in methadone plasma concentration was also observed at T2 and T3, although it did not attain statistical significance. Significant decreases in the intensity of several symptoms other than pain were also found at T2 and T3. Diclofenac appears to have a relevant opioid-sparing effect when using patient-controlled analgesia with oral methadone.
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PMID:Opioid-sparing effect of diclofenac in cancer pain. 922 38

The postoperative pain and stress experienced by tonsillectomy patients are often underestimated. For this reason traditional methods of analgesia are frequently used but with an ineffective result. Our study involved an analysis of pain sensation with regard to postoperative analgesia after adult tonsillectomies. In all, 150 patients following tonsillectomy were treated with different methods of analgesia, which included Diclofenac monotherapy and combined treatment with Tramadol-retard and Naproxen. Postoperative sensations of pain were realized in a visual analogous pain score, with consideration given to individual experiences of subjective pain. In addition, circulatory and hemopoiesis parameters were controlled. Results showed that the postoperative analgesic effect of Diclofenac was significantly less than that of Tramadol-retard and Naproxen. Diclofenac monotherapy after tonsillectomy was only sufficient in cases involving an individual's low pain sensation. In cases with moderate or stronger pain the tonsillectomy patient requires an effective postoperative analgesia, as achieved with combined therapy using Tramadol retard and Naproxen. Aggravating side effects were not found in both schemes of analgesia.
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PMID:[Pain therapy after tonsillectomy in adults]. 953 56

In a randomized double-blind study, 120 patients with moderate to strong pain after surgical removal of wisdom teeth were given the following in single oral doses: 100-mg enteric-coated diclofenac tablets; 1 g acetaminophen (INN, paracetamol); 1 g acetaminophen plus 60 mg codeine; 100-mg enteric-coated diclofenac tablets plus 1 g acetaminophen; or 100-mg enteric-coated diclofenac tablets plus 1 g acetaminophen plus 60 mg codeine. Patients recorded pain intensity and pain relief for 8 hours. Upside assay sensitivity was confirmed because acetaminophen plus codeine was superior to acetaminophen. Diclofenac plus acetaminophen with and without codeine had superior analgesic effect compared with diclofenac, acetaminophen, or acetaminophen plus codeine. Addition of 60 mg codeine increased the degree of side effects. These results support the clinical practice of combining diclofenac with acetaminophen for acute pain. Of clinical importance are superior and prolonged analgesia and fewer side effects after enteric-coated diclofenac tablets plus acetaminophen compared with acetaminophen plus codeine.
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PMID:Combining diclofenac with acetaminophen or acetaminophen-codeine after oral surgery: a randomized, double-blind single-dose study. 1061 19

Diclofenac sodium (100 mg) has been introduced in the Caribbean as a suppository formulation. In a randomized single-blind (observer-blind) clinical trial, the postoperative analgesic efficacy of diclofenac administered either as a conventional intramuscular injection (75 mg) or as the available suppository formulation (100 mg) was studied in 44 adult male patients undergoing herniorrhaphy in same day surgery. Diclofenac was administered preoperatively at induction of anesthesia to patients (grades ASA I and II) after they had given informed consent. Evaluation of analgesia on the visual analog scale (VAS) did not differ significantly between the two treated groups at three assessment times: on admission to the recovery room, the postoperative ward and at discharge. The times for requests for additional analgesia and the number of patients requesting further analgesia did not differ. Patients who received the suppository were discharged earlier than those who received the injection (40 min vs. 65 min p = 0.02). This preliminary study of the two marketed formulations of diclofenac demonstrated that both preparations provided equivalent analgesia but patients who received the suppository preparation were discharged earlier.
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PMID:Analgesic effects of diclofenac suppository and injection after preoperative administration. 1066 98

The purpose of this project was to evaluate the analgesic efficacy of misoprostol when combined with ibuprofen or diclofenac Na. Animal experiments using the inflamed rat paw formalin model suggested that misoprostol potentiates the analgesic effect of some NSAIDs (nonsteroidal anti-inflammatory drugs) including diclofenac Na but not propionic acid derivatives or opiates. The dental pain model was used to evaluate the clinical relevance of this interaction. Patients received a single oral dose of study medication following surgical removal of impacted teeth. Patients were medicated for moderate to severe postsurgical pain and then filled in an analgesic diary for a 6-h observation period. Several blood samples were taken over the observation period. In addition, microdialysis samples were taken directly from the extraction socket and were analyzed for immunoreactive prostaglandin E(2) levels. The studies were single-dose, parallel group and double-blind assays. In the first study, 70 patients received an oral dose of either placebo (n = 13), misoprostol 200 &mgr;g (n = 18), ibuprofen 200 mg (n = 19), or the combination of misoprostol + ibuprofen (n = 20). Misoprostol alone demonstrated a small analgesic effect compared to placebo. Both the ibuprofen and combination groups were substantially more effective than placebo but not different from each other. The combination group had higher ibuprofen blood levels during the first 45 min but had a lower C(max) and longer time to T(max). The second study evaluated oral doses of placebo (n = 11), misoprostol 200 &mgr;g (n = 21), diclofenac Na 50 mg (n = 18), and the combination of misoprostol + diclofenac Na (n = 20). Relative to placebo, misoprostol performance was similar to the first study. When the results of the two studies were combined, there was a small, but statistically significant, analgesic effect for misoprostol. Diclofenac Na was superior to both placebo and to misoprostol alone. The combination was the most effective treatment, and for hours 4--6 it was significantly better than diclofenac Na alone. Analysis of the blood samples showed an earlier and higher peak effect for the diclofenac Na group compared to the combination, and the combination again had a lower C(max). The microdialysis probe assays demonstrated that misoprostol depressed PGE(2) levels at the peripheral site of trauma over the first 2 h after surgery. These pilot studies used small samples, and the results only suggest trend effects. Both studies demonstrated that misoprostol 200 &mgr;g, a prostaglandin analog, does have an analgesic effect. When combined with ibuprofen, there was no potentiation of analgesia. In contrast, the combination of misoprostol + diclofenac Na demonstrated an enhanced peak effect, total effect for pain intensity difference and pain relief (sum pain intensity difference [SPID] and total pain relief [TOTPAR]), and
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PMID:The Analgesic Interaction of Misoprostol with Nonsteroidal Anti-Inflammatory Drugs. 1186 59

Analgesia plays a major role in the therapy of fractures. This raises the question whether frequently used analgetics as Tramadol and Diclofenac have negative effects on the healing of fractures. Human osteoblasts were isolated from human spongiosa and incubated with Diclofenac, Tramadol and without analgetic substance in an in vitro experiment. After 9 days the absolute number of cells as a marker for proliferation and their mitochondrial activity were quantified. The mitochondrial activity was measured using the metabolisation of XTT (sodium-3'-(1-[phenylamino-carbonyl]-3,4-tetrazolium)-bis(4- methoxy-6-nitro) benzene-sulfonic acid hydrate). Both drugs led to a concentration-dependent decrease of cell proliferation. Tramadol showed a significant effect at a concentration of 20 micrograms/ml, which is much higher than the therapeutical concentration of 0.25 microgram/ml in serum. Diclofenac decreased cell proliferation at a concentration of 6 micrograms/ml, having a therapeutical concentration of 1.5 micrograms/ml in serum. Vitality of cells had constant correlation to absolute number of cells (R = 0.95). Our results don't suggest any negative effects of Tramadol on the osteoblast activities in vitro. Diclofenac significantly decreased the proliferation of human osteoblasts at concentrations probably reachable in vivo. A prolonged healing of fractures under treatment with Diclofenac may be possible in critical situations (pseudarthrosis revision, callus distraction).
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PMID:[Modification of human osteoblasts by various analgesics]. 1213 92

The purpose of the case-study was to evaluate the efficiency of non-steroid antiinflammatory drugs (NAD) for postoperative analgesia in children after small-scope surgical interventions. Diclofenac, 1 mg/kg per day administered as rectal suppositories or intramuscular injections after initial narcosis, was used for postoperative analgesia in children of the main group; postoperative analgesia made by analgin and promedol in the control group was compared with the former. Forty-seven children and 10 children with identical diseases like groin hernia, varicocele and dropsy of testicular membranes, were respectively in the main and control groups. Clinical examinations and registration of functional parameters were made in patients during certain time periods, i.e. before surgery (in the standing and lying postures) and after surgery (in 20 minutes, as well as in 1, 2, and 3 hours after surgical interventions). The efficiency of postoperative analgesia was evaluated by means of cardiointervalography according to Bayevsky method as well as by a state of central hemodynamics and by clinical examinations, including the visual-analogue 10-point scale and the 0-4 point verbal pain assessment scale. The postoperatively obtained data revealed a pronounced misbalance between the main and control groups, which is indicative of that the application of NAD for preventive and postoperative analgesia in children improves essentially the postoperative course and contributes to a fast rehabilitation of patients. A comparative analysis of the efficiency of postoperative analgesia by the discussed drugs showed that diclofenac possesses a sufficient analgetic activity and is free of any side-effects inherent in narcotic analgetics.
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PMID:[Postoperative analgesia with nonsteroid anti-inflammatory drugs in children]. 1520 15

The present study evaluates the possible role of dihydropyridine calcium channel antagonist nimodipine on diclofenac analgesia in formalin-induced facial pain model in rats. Adult Wistar rats of either sex received an injection of 50 microl of 5% v/v subcutaneous formalin into one vibrissal pad and consequent facial grooming behaviour was monitored. Animals exhibited two distinct periods of nocifensive grooming: i) an acute phase lasting 0-6 min; and ii) a tonic phase lasting 6-45 min. The individual analgesic response of nimodipine and diclofenac was noted at doses of 5, 10 and 20 mg/kg i.p. and 1, 2 and 4 mg/kg i.p., respectively, administered 5 min prior to formalin injection. Diclofenac 1, 2 and 4 mg/kg i.p. produced dose-dependent inhibition of facial grooming in both acute and tonic phases. Nimodipine per se had antihyperalgesic effect, but to a very small extent. Nimodipine 10 and 20 mg/kg significantly potentiated the subanalgesic dose of diclofenac, i.e., 0.2 mg/kg. Results of the study showed that low dose nimodipine per se has insignificant antihyperalgesic effect. However, it potentiated the subanalgesic dose of diclofenac showing a synergistic response. These results imply that nimodipine can be used as an adjunct to the treatment of various neuropathic pains, postherpetic and diabetic neuropathies but the clinical efficacy needs to be evaluated in patients.
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PMID:Potentiation of antihyperalgesic activity of diclofenac by nimodipine in a formalin model of facial pain in rats. 1531 2


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