2002
DOI: 10.1163/156856002321168204
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Recent pharmacodynamic and pharmacokinetic findings on oxaprozin

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Cited by 25 publications
(21 citation statements)
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“…(Table 1) is a non-selective COX inhibitor NSAID with effective anti-inflammatory, analgesic and antipyretic effects. These therapeutic activities derive from its capability to inhibit COX-2 [37][38][39][40][41][42]. Oxaprozin has an aliphatic propionic acid function attached to the oxazole as side chain, however contrarily to other propionic acid compounds this doesn't possess a chiral centre [40,42].…”
Section: Chemical Classificationmentioning
confidence: 99%
See 1 more Smart Citation
“…(Table 1) is a non-selective COX inhibitor NSAID with effective anti-inflammatory, analgesic and antipyretic effects. These therapeutic activities derive from its capability to inhibit COX-2 [37][38][39][40][41][42]. Oxaprozin has an aliphatic propionic acid function attached to the oxazole as side chain, however contrarily to other propionic acid compounds this doesn't possess a chiral centre [40,42].…”
Section: Chemical Classificationmentioning
confidence: 99%
“…Oxaprozin highly binds to plasma proteins (99.9%) with high affinity what leads to a long plasma elimination with a half-life of 50 to 60 hours. This elevated duration of action allows the administration of a single oxaprozin dose per day of 600 to 1800 mg [32,39,40,42,43].…”
Section: Drugmentioning
confidence: 99%
“…Among them, oxaprozin, an achiral oxazole-propionic acid derivative (4,5-diphenyl-2-oxazolepropionic acid) (Davies, 1998), is characterized by a relatively high rate of accumulation in inflamed synovium, compared with that detectable in plasma and synovial fluids (Kurowski and Thabe, 1989;Rainsford et al, 2002). In particular, following oral administration of 1200 mg of oxaprozin for 2.5 days to patients with rheumatoid arthritis, the drug concentrations in synovial tissue averaged 25 mg·mL -1 (@85.2 mmol·L -1 ), whereas the concentrations in plasma and in synovial fluids were, respectively, 4.9-7.6 mg·mL -1 (16.7-25.9 mmol·L -1 ) and 10-17 mg·mL -1 (34-58 mmol·L -1 ) (Todd and Brogden, 1986).…”
Section: Introductionmentioning
confidence: 99%
“…When the direct action of oxaprozin on COX was examined, it was found to inhibit COX activities with an IC 50 for human platelet COX-1 of 2.2 mmol·L -1 and an IC50 for IL-1-stimulated human synovial cell COX-2 of 36 mmol·L -1 (Kawai et al, 1998). In other words, oxaprozin-mediated inhibition of COX-2 is observed at drug concentrations easily achievable in inflamed joints (Kurowski and Thabe, 1989;Rainsford et al, 2002). Thus, as the biological effects of NSAIDs are generally explained on the basis of their inhibitory action on COXs (Vane and Botting, 1998), a similar inhibitory action of oxaprozin on COX-2 inhibition would be expected to contribute substantially to its anti-inflammatory effects.…”
Section: Introductionmentioning
confidence: 99%
“…This compound has been shown to be effective in in vitro and animal models of inflammation, pain and pyrexia 1 and has subsequently been shown to be effective and well tolerated in the clinical management of signs and symptoms of adult rheumatoid arthritis (RA), osteoarthritis (OA), ankylosing spondylitis, soft tissue disorders such as bursitis and tendonitis, and post operative dental pain 2 .…”
mentioning
confidence: 99%