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Query: UMLS:C0184567 (acute pain)
 3,962 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Pain is a common complaint, often occurring in conjunction with inflammation. Nonsteroidal anti-inflammatory drugs (NSAIDs) are the most commonly used analgesic agents in ambulatory patients. In recent studies, the cyclooxygenase-2 (COX-2) inhibitor rofecoxib demonstrated analgesic effects similar to those of NSAIDs in the treatment of acute pain and primary dysmenorrhea. The present randomized, single-dose, double-blind, double-dummy, placebo- and active-comparator-controlled, parallel-group study was undertaken to compare the analgesic efficacy of the COX-2 inhibitors rofecoxib 50 mg and celecoxib 200 mg with that of ibuprofen 400 mg and placebo in patients with postoperative dental pain. Two hundred and seventy-two patients experiencing pain after the removal of > or =2 third molars were randomized according to pain severity (moderate vs severe) to receive a single dose of placebo (n = 45), rofecoxib 50 mg (n = 90), celecoxib 200 mg (n = 91), or ibuprofen 400 mg (n = 46). Using a patient diary, patients recorded pain intensity, pain relief, and global evaluations throughout the 24-hour period after dosing. The overall analgesic effect, onset of action, peak effect, and duration of effect were evaluated, with the primary end point being total pain relief over 8 hours (TOPAR8). The safety profile was assessed on the basis of physical findings, laboratory results, and spontaneous reports of adverse experiences. The results showed that compared with celecoxib, rofecoxib had superior analgesic effects on all measures of analgesic efficacy, including overall analgesic effect (TOPAR8, 18.3 vs. 12.5; P<0.001), time to onset of effect (30 vs. 60 minutes; P = 0.003), peak pain relief (score, 2.8 vs 2.3; P<0.05), and duration of effect (>24 vs. 5.1 hours; P<0.001). In addition, rofecoxib's analgesic efficacy was similar to that of ibuprofen (TOPAR8, 18.3 vs. 17.0; P = 0.460), but the duration was longer (P<0.05); with ibuprofen, the time to on set was 24 minutes, peak pain relief score was 2.9, and duration of analgesic effect was 8.9 hours. The safety profile was similar across all treatment groups. Thus rofecoxib provided analgesic efficacy superior to that of celecoxib and comparable to that of ibuprofen in the treatment of patients with acute postoperative dental pain.
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PMID:Comparison of rofecoxib and celecoxib, two cyclooxygenase-2 inhibitors, in postoperative dental pain: a randomized, placebo- and active-comparator-controlled clinical trial. 1056 62

Conventional nonsteroidal anti-inflammatory drugs (NSAIDs) inhibit both cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2). The clinical efficacy of NSAIDs is primarily related to the inhibition of COX-2 activity, whereas much of the toxicity, particularly gastrointestinal toxicity, is related to COX-1 inhibition. In vitro and in vivo assays indicate that both COX-2-specific inhibitors and conventional NSAIDs are equally effective in inhibiting COX-2, suggesting that the clinical efficacy of COX-2-specific inhibitors should be similar to that of conventional NSAIDs. Multiple studies in patients with osteoarthritis, rheumatoid arthritis, and acute pain have now confirmed that the clinical efficacy of COX-2-specific inhibitors is similar to that of conventional NSAIDs.
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PMID:Efficacy of cyclooxygenase-2-specific inhibitors. 1117 44

Rofecoxib (Vioxx, Merck & Co., Inc.) is a new orally-effective non-steroidal anti-inflammatory drug (NSAID) approved for treatment of acute pain, fever, primary dysmenorrhea and pain and inflammation in osteoarthritis (OA). It is also being evaluated for treatment of rheumatoid arthritis and adenomatous polyps of the colon. Rofecoxib is a specific inhibitor of cyclooxygenase-2 (COX-2), thereby inhibiting prostanoid synthesis in cells that express COX-2, including inflammatory cells. As cells in the gastrointestinal (GI) tract principally express COX-1, a different isoform of cyclooxygenase, it is predicted that rofecoxib will have less GI toxicity than other less selective NSAIDs. In clinical trials, rofecoxib was found to be as effective as other NSAIDs for management of pain and inflammation. In trials that compare rofecoxib with ibuprofen, diclofenac and indomethacin, less GI toxicity has been observed, as assayed by a decrease in lesions visible on endoscopy, by GI blood loss and, in a meta-analysis, by frequency of serious adverse GI events. The presence of COX-2 in cells other than inflammatory cells results in side effects common among NSAIDs, including peripheral oedema and hypertension. These side effects are dose-dependent. Rofecoxib, together with other branded NSAIDs, are relatively expensive, which has led to concern regarding costs versus benefits. There is also concern regarding potential risks associated with the use of rofecoxib by populations that would otherwise not tolerate NSAIDs.
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PMID:Rofecoxib. 1124 95

A series of 4-(4-cycloalkyl/aryl-oxazol-5-yl)benzenesulfonamide derivatives were synthesized and evaluated for their abilities to inhibit cyclooxygenase-2 (COX-2) and cyclooxygenase-1 (COX-1) enzymes. In this series, substituent effects at the ortho position to the sulfonamide group on the phenyl ring were examined. Most substituents reduced or lost both COX-2 and COX-1 activities. In contrast, introduction of a fluorine atom preserved COX-2 potency and notably increased COX1/COX-2 selectivity. This work led to the identification of a potent, highly selective, and orally active COX-2 inhibitor JTE-522 [9d, 4-(4-cyclohexyl-2-methyloxazol-5-yl)-2-fluorobenzenesulfonamide], which is currently in phase II clinical trials for the treatment of rheumatoid arthritis, osteoarthritis, and acute pain.
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PMID:4-(4-cycloalkyl/aryl-oxazol-5-yl)benzenesulfonamides as selective cyclooxygenase-2 inhibitors: enhancement of the selectivity by introduction of a fluorine atom and identification of a potent, highly selective, and orally active COX-2 inhibitor JTE-522(1). 1190 92

Celecoxib is a novel cyclooxygenase-2-specific inhibitor for the management of acute pain, primary dysmenorrhea, and the signs and symptoms of arthritis. This double-blind, placebo-controlled study in 16 healthy volunteers evaluated whether celecoxib alters the effect of concomitant aspirin on platelet function. Volunteers received celecoxib (400 mg/day) or placebo for 4 days. On day 5, they also received a single 325 mg dose of aspirin with either 200 mg celecoxib or placebo. Thromboxane and platelet aggregation response to adenosine 5'-diphosphate (ADP), collagen, and arachidonic acid were measured before the first dose of celecoxib or placebo (baseline) and before dosing and 2 and 8 hours post dose on day 5. There was no significant difference in thromboxane inhibition between the two groups (percent inhibition: placebo 99.4%, celecoxib 99.0%; p = 0.555). There was also no significant difference in the effect of aspirin on platelet aggregation due to ADP, collagen, or arachidonic acid between the groups. Therefore, these data indicate that celecoxib does not alter the effects of aspirin on platelet function.
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PMID:Celecoxib does not affect the antiplatelet activity of aspirin in healthy volunteers. 1221 Dec 19

Coxibs are a new group of non-steroidal anti-inflammatory drugs (NSAIDs), which inhibit cyclooxygenase-2 selectively. They can be prescribed for treatment of osteoarthritis, rheumatoid arthritis, primary dysmenorrhea, and acute pain. Their main advantage is a reduction in the frequency of serious gastrointestinal complications compared to NSAIDs, but they have the same tendency to induce oedema and renal side effects. The coxibs do not influence platelet function. Meta-analysis of studies with coxibs suggests that they increase the risk of heart attack, but according to recent information this may have been exaggerated. Coxibs should be used for patients at risk for gastrointestinal complications and bleeding, but perhaps not for patients at risk for arterial thrombotic diseases.
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PMID:[Coxiber and risk of myocardial infarction--the apprehension might have been exaggerated]. 1257

Rofecoxib is a new specific cyclooxygenase-2 inhibitor. The efficacy of rofecoxib has been established in the treatment of osteoarthritis, rheumatoid arthritis and acute pain. Rofecoxib has been approved in the United States for the treatment of osteoarthritis and acute pain. Endoscopically proven gastrointestinal ulceration is much less with rofecoxib than standard nonsteroidal antiinflammatory drugs (NSAIDs) and the ulceration rate with rofecoxib is similar to that seen with placebo. Rofecoxib appears to provide clinical benefit equivalent to standard NSAIDs with less toxicity.
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PMID:Rofecoxib: a specific cyclooxygenase inhibitor. 1287 21

Pain monitoring is often inadequate in the ambulant field to assure therapy results. Today NSAID take the centre in acute pain and inflammation control in dental interventions. Compared to conventional non-selective NSAID modern selective Cyclooxygenase-2 inhibitors (COX-2) provide the potential for improved compatibility and simplified medication with heightened effectiveness in acute postoperative toothaches. The aim of this study was to compare the effect of selective COX-2 inhibitors with NSAID after operative wisdom tooth extraction in 30 ambulant patients. The pain curve under mefenamine acid showed a significant increase during the first 48 hours after extraction. With rofecoxib a continuous pain decrease with the lowest stand 48 hours after intervention was registered. One week after extraction the patient's satisfaction was in favour of rofecoxib, which showed a clearly prolonged analgetic effect over 24 hours. Additionally rofecoxib as a COX-2 selective inhibitor doesn't bear the risk for severe non-anticipatable gastrointestinal side effects or prolonged bleeding after surgical intervention.
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PMID:[Pain management after third molar extraction. Observations of the use of mefenamic acid and rofecoxib in the treatment of postoperative pain in the dental office]. 1450 73

Rofecoxib was the first specific inhibitor of cyclooxygenase-2 (COX-2) approved for the treatment of acute pain. It has been shown to provide analgesia that is significantly better than placebo and has an onset of action and efficacy similar to that of traditional nonselective nonsteroidal anti-inflammatory drugs (NSAIDs), such as naproxen and ibuprofen. In addition, the analgesic efficacy of rofecoxib has been demonstrated to be superior to that of the opioid combination of codeine 60 mg/acetaminophen 600 mg in an acute dental pain model. For the treatment of acute pain, the efficacy of rofecoxib was further demonstrated in a study of patients who had undergone orthopedic surgery. Rofecoxib has been found to be as effective as naproxen sodium and more effective than placebo in studies evaluating its use for the treatment of primary dysmenorrhea. In patients with osteoarthritis (OA) of the knee or hip, rofecoxib is superior to placebo and similar to diclofenac and ibuprofen in relieving OA pain and improving physical function. Rofecoxib has also been shown to be superior to acetaminophen and celecoxib after 6 weeks of treatment for OA. The efficacy of rofecoxib has also been demonstrated in patients with rheumatoid arthritis and low back pain. The advantages of using COX-2-specific NSAIDs include convenient once-daily dosing schedule and improved safety compared with traditional NSAIDs. Two large outcomes studies, VIGOR and CLASS, have shown that gastric mucosal ulceration occurs significantly less often in patients taking COX-2-specific inhibitors than in those treated with ibuprofen, diclofenac, or naproxen and occurs with a similar incidence to that of placebo. Absence of any effect on platelet aggregation and bleeding time further distinguishes these agents from traditional NSAIDs. Because COX-2-specific inhibitors do not have an antiplatelet effect, they cannot be used as a substitute for low-dose aspirin for cardiovascular prophylaxis. Rofecoxib is a safe and highly effective alternative to previously available NSAIDs and should be considered for the treatment of acute pain conditions in adult patients, especially those at risk for developing gastrointestinal complications. It is preferred in the perioperative setting because of its analgesic efficacy and lack of platelet effects. Because of its more favorable gastrointestinal toxicity profile compared with nonselective NSAIDs, rofecoxib is safer in patients, especially older patients, for whom chronic anti-inflammatory or analgesic therapy is indicated.
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PMID:The role of rofecoxib, a cyclooxygenase-2-specific inhibitor, for the treatment of non-cancer pain: a review. 1462 51

Lumiracoxib (Prexige; 2-[(2-fluoro-6-chlorophenyl)amino]-5-methyl-benzeneacetic acid) is a novel, chemically distinct cyclooxygenase-2 selective inhibitor, which has been developed for the treatment of osteoarthritis, rheumatoid arthritis, and acute pain. The absorption, metabolism, disposition, and mass balance of [14C]lumiracoxib were investigated in four healthy male subjects after a single 400-mg oral dose. Serial blood and complete urine and feces were collected for 168 h postdose. Lumiracoxib was rapidly absorbed, achieving mean plasma concentrations >1 microg/ml within 1 h of dosing. Unchanged drug in plasma accounted for 81 to 91% of radioactivity up to 2.5 h postdose, suggesting a modest first-pass effect; unchanged drug was the major circulating component in plasma, accounting for approximately 43% of the AUC(0 to 24 h). The terminal half-life of lumiracoxib in plasma was 6.5 h. Major plasma metabolites were the 5-carboxy, 4'-hydroxy, and 4'-hydroxy-5-carboxy derivatives. Excretion involved both renal (54.1%) and fecal (42.7%) routes, and dose recovery was almost complete (96.8%). Lumiracoxib was extensively metabolized before excretion, with little unchanged drug in urine (3.3% of dose) or feces (2.0% of dose). The major metabolic pathways of lumiracoxib were oxidation of the 5-methyl group and hydroxylation of the dihaloaromatic ring. Glucuronic acid conjugates of lumiracoxib metabolites (and to a minor extent lumiracoxib itself) were identified, although there was no evidence of cysteine, mercapturic acid, or glutathione conjugates. In summary, orally administered lumiracoxib is rapidly absorbed and undergoes extensive metabolism before excretion via urine and feces, with no evidence of formation of potentially reactive metabolites.
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PMID:Pharmacokinetics and metabolism of lumiracoxib in healthy male subjects. 1510 Jan 80


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