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)

Fenoprofen, a new antirheumatic agent, was evaluated in 45 patients with rheumatoid arthritis in an open study design to simulate the conditions under which the drug will be used. No control agents were used. The effectiveness of fenoprofen was demonstrated by the per cent of patients who improved during fenoprofen therapy. Duration of therapy varied from one to 629 days. Pain was the first parameter to respond, followed by an anti-inflammatory effect, which was observed after four to six weeks of therapy. Side effects consisted mainly of minor gastro-intestinal symptoms.
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PMID:Longterm fenoprofen therapy in patients with rheumatoid arthritis. 78 Dec 30

This study, designed to evaluate fenoprofen in patients with osteoarthritis, consisted of two phases: I. A double-blind crossover comparison of fenoprofen, 200 to 600 mg every six hours, to aspirin, 325 to 975 mg every six hours; II. Longterm use of fenoprofen in an open study design. During the first part of the study, both fenoprofen and aspirin were significantly better than placebo in relieving the severity and duration of pain, and in reducing stiffness. In most of the variables fenoprofen was also slightly better than aspirin. The most frequently observed side effects were abdominal discomfort, headache, pruritus, nervousness, and tinnitus. Longterm administration demonstrated the safety of fenoprofen or periods exceeding two years. Fenoprofen did not precipitate or aggravate chronic disorders, nor did it mask the symptoms of any developing disease. No interaction with concomitant drug therapy was observed.
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PMID:Fenoprofen therapy in large-joint osteoarthritis: double-blind comparison with aspirin and longterm experience. 78 Dec 34

Fenoprofen, a compound with analgesic, anti-inflammatory, and antipyretic properties in animals, has been compared with placebo in a double-blind cross-over trial in 60 patients with rheumatoid arthritis. There was a statistically highly significant reduction in pain, duration of morning stiffness, analgesic requirements, and articular index, with increase in grip strength. There was no significant reduction in joint size or temperature. In a subsequent double-blind group-comparative study fenoprofen proved to be as effective as aspirin in relieving the symptoms of rheumatoid arthritis, with strikingly fewer side effects. Almost half of the patients taking aspirin were unable to tolerate the drug in adequate dosage for six months. The remainder were able to take on average only 4 g daily, and at this dose almost half still complained of tinnitus and deafness.Fenoprofen is likely to be useful for patients who cannot tolerate aspirin and other more toxic anti-inflammatory drugs or whose disease is not of sufficient severity to justify their use.
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PMID:Treatment of rheumatoid arthritis with fenoprofen: comparison with aspirin. 459 Jun 69

Fenoprofen, 600 mg, three times daily, was compared with phenylbutazone, 100 mg, three times daily, in 30 patients suffering from ankylosing spondylitis in a double-blind cross-over study. Assessments were made after an initial washout period and after each month-long treatment period. Phenylbutazone significantly improved morning stiffness, finger-to-floor distance, chest expansion, overall joint pain, spinal pain, the physician's assessment of disease activity and ESR. Only chest expansion was significantly improved by fenoprofen, and phenylbutazone was significantly better than fenoprofen in its effects on finger-to-floor distance, morning stiffness, overall joint pain, spinal pain and the physician's assessment of disease activity. Side-effects were of a minor nature apart from one patient who developed rectal bleeding on phenylbutazone which recurred on rechallenging.
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PMID:A double-blind cross-over trial of fenoprofen and phenylbutazone in ankylosing spondylitis. 701 May 12

Cyclooxygenase (COX) is a critical enzyme in prostaglandin biosynthesis that modulates a wide range of biological functions, such as pain, fever, and so on. To perform in vivo COX imaging by positron emission tomography (PET), we developed a method to incorporate (11)C radionuclide into various 2-arylpropionic acids that have a common methylated structure, particularly among nonsteroidal anti-inflammatory drugs (NSAIDs). Thus, we developed a novel (11)C-radiolabeling methodology based on rapid C-[(11)C]methylation by the reaction of [(11)C]CH(3)I with enolate intermediates generated from the corresponding esters under basic conditions. One-pot hydrolysis of the above [(11)C]methylation products also allows the synthesis of desired (11)C-incorporated acids. We demonstrated the utility of this method in the syntheses of six PET tracers, [(11)C]Ibuprofen, [(11)C]Naproxen, [(11)C]Flurbiprofen, [(11)C]Fenoprofen, [(11)C]Ketoprofen, and [(11)C]Loxoprofen. Notably, we found that their methyl esters were particularly useful as proradiotracers for a study of neuroinflammation. The microPET studies of rats with lipopolysaccharide (LPS)-induced brain inflammation clearly showed that the radioactivity of PET tracers accumulated in the inflamed region. Among these PET tracers, the specificity of [(11)C]Ketoprofen methyl ester was demonstrated by a blocking study. Metabolite analysis in the rat brain revealed that the methyl esters were initially taken up in the brain and then underwent hydrolysis to form pharmacologically active forms of the corresponding acids. Thus, we succeeded in general (11)C-labeling of 2-arylpropionic acids and their methyl esters as PET tracers of NSAIDs to construct a potentially useful PET tracer library for in vivo imaging of inflammation involved in COXs expression.
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PMID:General method for the (11)C-labeling of 2-arylpropionic acids and their esters: construction of a PET tracer library for a study of biological events involved in COXs expression. 2022 90

Analgesic and ulcerogenic properties have been studied for the copper(II) coordination complex of the nonsteroidal anti-inflammatory drug Fenoprofen and imidazole [Cu(fen)2(im)2] (Cu: copper(II) ion; fen: fenoprofenate anion from Fenoprofen, im: imidazole). A therapeutic dose of 28 mg/kg was tested for [Cu(fen)2(im)2] and 21 mg/kg was employed for Fenoprofen calcium, administered by oral gavage in female mice to compare the therapeutic properties of the new entity. The acetic acid induced writhing test was employed to study visceral pain. The percentage of inhibition in writhing and stretching was 78.9% and 46.2% for the [Cu(fen)2(im)2] and Fenoprofen calcium, respectively. This result indicates that the complex could be more effective in diminishing visceral pain. The formalin test was evaluated to study the impact of the drugs over nociceptive and inflammatory pain. The complex is a more potent analgesic on inflammatory pain than the parent drug. Ulcerogenic effects were evaluated using a model of gastric lesions induced by hypothermic-restraint stress. Fenoprofen calcium salt caused an ulcer index of about 79 mm(2) while the one caused by [Cu(fen)2(im)2] was 22 mm(2). The complex diminished the development of gastric mucosal ulcers in comparison to the uncomplexed drug. Possible mechanisms of action related to both therapeutic properties have been discussed.
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PMID:Enhanced analgesic properties and reduced ulcerogenic effect of a mononuclear copper(II) complex with fenoprofen in comparison to the parent drug: promising insights in the treatment of chronic inflammatory diseases. 2505 Mar 53