Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0030193 (pain)
 261,466 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Forty patients affected by various rheumatic disorders (mainly osteoarthritis) were treated with flurbiprofen (300 mg daily) or diclofenac (200 mg daily) in a two-week, parallel group, randomized trial. Both drugs were clinically effective in all the parameters except for fingertip-to-floor distance and ESR. Flurbiprofen proved to be more effective than diclofenac in reducing pain on movement (p less than 0.01) and number of swollen joints (p less than 0.05). The doctor's overall assessment favoured flurbiprofen (p less than 0.10). The incidence and severity of side-effects were low and similar with the two drugs.
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PMID:Controlled study on flurbiprofen and diclofenac in the treatment of rheumatic disorders. 634 28

Our purpose was to evaluate the analgesic efficacy and safety of single oral doses of flurbiprofen 25, 50 and 100 mg, aspirin 600 mg, and placebo in the relief of moderate to severe post-episiotomy pain. One hundred and fifty-two evaluable patients completed a randomized, double-blind, stratified, parallel groups study. They were observed over a six hour period by one nurse-observer. Based upon each of the summary efficacy measures SPID, TOTAL and PEAK % and most of the hourly direct measures of pain intensity and pain relief, each of the four active treatments were statistically superior to placebo. Flurbiprofen 25 mg appeared to be slightly less effective than aspirin 600 mg, but the differences were not statistically significant. Flurbiprofen 50 and 100 mg were quite similar and were significantly more effective than aspirin 600 mg and flurbiprofen 25 mg. There were no observed or reported adverse effects.
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PMID:Analgesic effect of graded doses of flurbiprofen in post-episiotomy pain. 634 14

Fifty patients suffering from acute soft tissue rheumatism entered an open parallel group study of flurbiprofen 200 mg to 400 mg daily versus piroxicam 20 mg to 40 mg daily for 4 weeks. Both treatments caused statistically significant improvements in pain, pain on active movement, restriction of passive movement and reduction of strength. Global assessments of the patients' progress also improved significantly with both compounds. Flurbiprofen was significantly superior to piroxicam with regard to relief of pain at Day 28, pain on active movement at Days 14 and 28, pain on passive movement at Days 7, 14 and 28 and pain, as measured by a visual analogue scale, at Day 14. Clinically, flurbiprofen showed greater improvements in all the other parameters throughout the study period. Side-effects, mainly gastro-intestinal in nature, occurred in 6 patients receiving flurbiprofen and 8 receiving piroxicam. One patient receiving flurbiprofen was withdrawn due to stomach pain and headache, but no withdrawals due to side-effects were necessary in those receiving piroxicam. One patient receiving piroxicam was withdrawn due to a total remission by Day 14.
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PMID:The efficacy of flurbiprofen versus piroxicam in the treatment of acute soft tissue rheumatism. 639 33

Twenty-five patients suffering from primary dysmenorrhoea took part in a double-blind crossover study which demonstrated flurbiprofen (100 mg three times a day) to be significantly more effective than paracetamol (1 g three times a day) in providing pain relief on Days 1 and 2, and on the worst day of pain. Flurbiprofen also appeared to reduce the incidence of secondary symptoms of nausea and feeling faint, and menstrual blood loss. The study was also analyzed as if a parallel group study and showed flurbiprofen to be significantly more effective than paracetamol.
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PMID:A comparison of flurbiprofen and paracetamol in the treatment of primary dysmenorrhoea. 640 90

This study was designed to evaluate the effectiveness of flurbiprofen when compared to aspirin and placebo. The study medications were administered 30 minutes preoperatively and at fixed intervals four and eight hours later in 107 patients undergoing surgical removal of third molars using a randomized, double-blind design. The treatment consisted of flurbiprofen 25mg, flurbiprofen 50mg, aspirin 650mg, and placebo. Flurbiprofen was significantly more effective than aspirin and placebo with respect to pain severity scores and patient evaluation of the pretreatment dose. Aspirin was significantly more effective than placebo. There were no differences between the two doses of flurbiprofen. Side effects were minor and not significantly different among the groups.
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PMID:The prophylactic use of flurbiprofen to prevent post-extraction dental pain. 659 87

Flurbiprofen is a propionic acid-derived non-steroidal anti-inflammatory drug (NSAID) used widely in the treatment of rheumatism and non-arthritic pain. The pharmacokinetics of topically and orally administered flurbiprofen were compared in a two-part, open study involving healthy adult volunteers. In the first (cross-over) part of the study, 12 Caucasians were randomized to receive either a single oral dose of 50 mg flurbiprofen or a single topical application of a novel 40 mg flurbiprofen-containing patch on the right wrist for 12 h. In the second part of the study, each subject applied a flurbiprofen-containing patch twice daily to the same wrist for 7 days. Plasma concentrations of flurbiprofen and urinary concentrations of the NSAID and its metabolites were measured by high-performance liquid chromatography assay, to enable comparison of the pharmacokinetic parameters for delivery of the drug by both routes. Maximum concentrations of the NSAID in plasma (Cmax) were much lower after a single application of the topical 40 mg flurbiprofen patch than after a single oral dose of 50 mg of the NSAID (mean +/- SD: 43 +/- 16 ng/ml versus 5999 +/- 1300 ng/ml, respectively). After repeated application of the topical patch, Cmax increased only slightly to 103 +/- 57 ng/ml. The mean relative bioavailability of flurbiprofen from the patch was 3.5 +/- 1.7%, calculated from plasma area under the curve data and 4.4 +/- 2.8% from urinary excretion data.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Pharmacokinetic comparison of oral and local action transcutaneous flurbiprofen in healthy volunteers. 765 70

Flurbiprofen is a chiral non-steroidal anti-inflammatory drug used in the treatment of pain or inflammation. The primary routes of biotransformation for (R)- and (S)-flurbiprofen are oxidation (presumably cytochrome P450) and conjugation. To date, the specific cytochrome P450 (P450) involved in the oxidative metabolism of this compound (specifically 4'-hydroxylation) has not been elucidated. Experiments were conducted to characterize the kinetic parameters (Km and Vmax) for the 4'-hydroxylation of (R)- and (S)-flurbiprofen in human liver microsomes, to determine if enantiomeric interactions occur when both enantiomers are present, and to identify the specific P450 form(s) involved in this reaction. In human liver microsomes, the Km and Vmax (mean +/- SD) for (R)-4'-hydroxy-flurbiprofen formation were 3.1 +/- 0.8 microM and 305 +/- 168 pmol.min-1.mg protein)-1, respectively. In comparison, the Km and Vmax (mean +/- SD) for (S)-4'-hydroxy-flurbiprofen formation were 1.9 +/- 0.4 microM and 343 +/- 196 pmol.min-1.mg protein-1, respectively. Enantiomeric interaction studies revealed a decrease in Km and Vmax for both enantiomers and an apparent loss of stereoselectivity. Racemic-warfarin, tolbutamide, alpha-naphthoflavone and erythromycin were studied as potential inhibitors of this process. The estimated Ki values for the inhibition of (R)- and (S)-4'-hydroxy-flurbiprofen formation by racemic-warfarin were 2.2 and 4.7 microM. This reaction was also inhibited by tolbutamide. In contrast, erythromycin and alpha-naphthoflavone had no appreciable effect on 4'-hydroxy-flurbiprofen formation. cDNA-expression of individual forms was used to determine which P450 was involved in 4'-hydroxy-flurbiprofen formation. P450 2C9 and an allelic variant (R144C) readily catalyzed the formation of 4'-hydroxy-flurbiprofen. P450 1A2 was also active albeit with a turnover rate 1/140th that of P450 2C9R144C (P450s 2C8, 2E1 and 3A4 were not active toward either enantiomer). The results of these studies indicate that the enantiomers of flurbiprofen may exhibit stereoselectivity with respect to enzyme affinity but have roughly equal maximum formation velocities. Additionally, these two enantiomers may compete for the enzyme resulting in lower maximum velocities for both enantiomers. Finally, of those P450 forms examined, only P450 2C9 and an allelic variant catalyzed the 4'-hydroxylation of both (R)- and (S)-flurbiprofen.
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PMID:Role of cytochrome P450 2C9 and an allelic variant in the 4'-hydroxylation of (R)- and (S)-flurbiprofen. 776 8

Nonsteroidal anti-inflammatory drugs (NSAIDs) produce potent analgesic, antipyretic, and anti-inflammatory effects. We studied postoperative pain in 97 consecutive patients having photorefractive keratectomy (PRK) by an excimer laser with different topical NSAID protocols. Treatment with topical homatropine hydrobromide, either diclofenac sodium (Voltaren Ophthalmic) or ketorolac tromethamine (Acular), and a soft contact lens was most effective in achieving post-PRK analgesia. We also studied post-PRK myopic regression in 68 consecutive patients and found that flurbiprofen sodium (Ocufen), when added to topical steroid protocols, significantly reduced myopic regression for one year postoperatively more than steroids alone or steroids and diclofenac sodium. Diclofenac, used with topical steroids, had less of an additive effect on myopic regression than did flurbiprofen. Topical NSAIDs are useful adjuncts to PRK therapy, both to eliminate postoperative pain and to control post-PRK myopic regression.
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PMID:Use of topical nonsteroidal anti-inflammatory drugs in excimer laser photorefractive keratectomy. 800 90

After light touch to its nose, the nematode Caenorhabditis elegans halts forward locomotion and initiates backing. Here we show that three classes of neurons (ASH, FLP, and OLQ) sense touch to the nose and hence are required for this avoidance response. ASH, FLP, and OLQ have sensory endings that contain axonemal cilia. Mutant animals that have defective ciliated sensory endings as well as laser-operated animals that lack ASH, FLP, and OLQ fail to respond to touch to the nose. Together with the previous work of others, these results demonstrate that C. elegans has at least five morphologically distinct classes of mechanosensory neurons. Interestingly, the ASH neuron also acts as a chemosensory neuron; it mediates the avoidance of noxious chemicals. Since ASH possesses both chemosensory and mechanosensory modalities, this neuron might be functionally analogous to vertebrate nociceptors, which mediate the sensation of pain.
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PMID:A dual mechanosensory and chemosensory neuron in Caenorhabditis elegans. 846 Jan 26

The efficacy and safety of local action transcutaneous flurbiprofen 40 mg [flurbiprofen LAT] patches and diclofenac sodium tablets, 50 mg b.d., were compared in an open, multicentre, randomized, parallel-group study in patients with soft-tissue rheumatism. Patches were replaced at 12-hourly intervals. Clinical assessments were performed after 7 and 14 days of treatment. Fifty-six patients were treated with flurbiprofen LAT and 53 with diclofenac. Six withdrawals (three from each group) occurred during the treatment period. A statistically significant difference was observed in favour of flurbiprofen LAT for the principal measure, namely the investigator's opinion of overall change in clinical condition: 49/53 (92%) patients treated with flurbiprofen LAT had improved by day 14 compared with 36/49 (73%) patients receiving diclofenac sodium (p = 0.03; eligible dataset). There were also statistically significant differences in favour of flurbiprofen LAT for the investigator's assessments of the overall severity of the clinical condition (p = 0.03; eligible dataset), for the severity of pain at the region treated (p = 0.04; intent-to-treat), and for the severity of tenderness (p < 0.001; intent-to-treat). Supplementary analgesia (paracetamol) was required by two patients in the flurbiprofen LAT group and by eight diclofenac-treated patients. The difference in favour of flurbiprofen LAT in the average daily consumption of paracetamol was significant (p = 0.04). The patients' assessment of severity of pain on movement also favoured flurbiprofen LAT (p = 0.049; eligible dataset), but there were no statistically significant differences in day or night pain or quality of sleep. For the patients' opinion of treatment there was, however, a statistically significant difference in favour of flurbiprofen LAT (p = 0.02). Of the patients receiving flurbiprofen LAT, 94% regarded it as a convenient form of treatment. With respect to tolerability 8/56 (14%) patients applying flurbiprofen patches reported a total of nine adverse effects (AEs) (mainly local, mild skin irritations), vs 9/52 (17%) patients receiving diclofenac, who reported 12 AEs. Most AEs in the enteric-coated diclofenac group were of a gastrointestinal nature (one of which was severe). In terms of the proportion of patients reporting AEs related to the digestive system, there was a statistically significant difference in favour of flurbiprofen LAT (p = 0.011). In conclusion, local treatment of soft-tissue rheumatism with flurbiprofen LAT was demonstrably superior to benchmark oral therapy with diclofenac sodium over a 2-week period in terms of both efficacy and gastrointestinal tolerability. Flurbiprofen LAT provided both an effective and convenient form of topical SAID treatment.
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PMID:Efficacy and tolerability of a topical NSAID patch (local action transcutaneous flurbiprofen) and oral diclofenac in the treatment of soft-tissue rheumatism. 913 22


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