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• W2201104103 abstract "Objective and design: The gastric toxicity of racemic-ketoprofen and its enantiomers (S(+)- and R(-)- ketoprofen), oxygen free radical generation and neutrophil infiltration in response to damage were evaluated in rats. Changes in prostaglandin synthesis, cyclooxygenase expres- sion and glutathione metabolism were also studied. Materials and methods: Studies were performed in Wistar rats. Drugs were given by oral administration: racemic-keto- profen (100, 50 and 25 mg/kg body weight); S(+) and R(-)- ketoprofen (50, 25 and 12.5 mg/kg body weight). Determi- nations were made of gastric mucosal injury, lipid peroxida- tion, xanthine oxidase, myeloperoxidase and superoxide dis- mutase activities, glutathione levels, glutathione peroxidase and glutathione reductase activities, gastric prostaglandin synthesis (PGE2 levels) and COX-expression. Results: Racemic-ketoprofen dose-dependently exhibited the highest toxicity. In contrast, S(+)-ketoprofen at half the dose of the racemic compound proved to be less ulcerogenic. R(-)-ketoprofen was also less ulcerogenic, but when admin- istered as the racemate exacerbated gastric ulceration caused by S(+)-ketoprofen. Drug administration produced signifi- cant increases in lipid peroxidation levels and xanthine-oxi- dase and a decrease in superoxide dismutase activity. Never- theless the racemate induced the highest disturbances in oxidative metabolism. No changes in myeloperoxidase val- ues and glutathione metabolism were found. Cyclooxygen- ase-1 immunoreactivity was observed and did not differ from that in control rats. Cyclooxygenase-2 could also be expressed after treatments. Conclusions: R(-)-ketoprofen and S(+)-ketoprofen have a comparable gastric toxicity and they both have a better gas- tric toxicity profile as compared to the racemate. In addition to inhibition of prostaglandin synthesis, damage resulted in" @default.
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• W2201104103 date "2002-01-01" @default.
• W2201104103 modified "2023-09-27" @default.
• W2201104103 title "Original Research Papers Gastric toxicity of racemic ketoprofen and its enantiomers in rat: oxygen radical generation and COX-expression" @default.
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