International Journal of Pharma and Bio Sciences
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10.22376/ijpbs.2019.10.1.p1-12
Volume 5 Issue 1
2014 (January - March)
ANTINOCICEPTIVE ACTIVITY OF A NEW NON-OPIOID ANALGESIC PYRODAZOL AND KETOROLAC
The search for new analgesics that exceed existing analogues in efficacy and/or safety is important. Existing drugs do not fully meet the modern clinic requirements because of side effects and lack of effectiveness. In the search for new analgesics, antinociceptive activity of the new derivative of 5Ð-pyrrollo 1,2-aimidazole (pyrodazol) was examined in comparison with that of ketorolac. Anti-inflammatory (antiexudative) activity was evaluated in the model of carrageenan edema. Analgesia was evaluated in the models of carrageenin edema, Randall and Selitto and acetic acid-induced writhing on nonlinear white mice and Wistar rats after a single orally administration. Pyrodazol is not shown an antiexudative action in the model of carrageenan edema at doses of 1, 5 and 10 mg/kg. In the model of acetic acid-induced writhing, pyrodazol at a dose of 2.5 mg/kg showed an antinociceptive effect up to 2 hours, and in the peak of analgesia (60 min) in a dose range of 0.5 - 5 mg/kg it was superior to ketorolac: ED lessThan sub greaterThan 50 lessThan /sub greaterThan 0.92 (0.48 - 1.75) mg/kg and 2.9 (1.45 - 5.8) mg/kg, respectively. In the model of Randall and Salitto in the dose range of 1-20 mg/kg, pyrodazol showed a reliable antinociceptive effect lasting up to 3 hours at dose of 5 mg/kg significantly outperforming the similar effect of ketorolac. The data obtained suggest that in the model of peripheral pain, pyrodazol outperforms ketorolac. An antinociceptive activity of pyrodazol isn`t associated with an effect on COX isoenzymes.
YADLOVSKYI OLEH
Pyrodazol, ketorolac, analgesia, derivative of pyrrollo-imidazole.
219-224