Aim: To search the new analgesics we studied the antinociceptive activity of the new derivative 5Hpyrrolo [1,2-a]¬imidazole in comparison with this of the morphine and ketorolac.
Material and Methods: The analgesia was evaluated on hot plate and tail-flick thermal nociceptive stimulation models by intragastric administration of ketorolac and by intramuscular injection of morphine.
Results: On the hot plate model ED50 value was per body weight 0.34 (0.18 - 0.63) mg/kg of the pyrodazol /i.g, 1.00 (0.59 - 1.70) mg/kg/of the ketorolac/ i. g. in 90 minutes post administration. On the hot plate model in 0.3 - 1.3 mg/kg/doses i.m the pirodazol is similar to morphine hydrochloride in dose 2.5 mg/kg i.m. On the tail-flick model ED50 values of the pyrodazol and ketorolac are 1.9 (1.12 - 3.23) mg/kg /i.g and 3.0 (2.08 - 4.32) mg/kg/i. g, respectively.
Conclusion: The obtained data may allow to suggest that on thermal nociceptive stimulation models the pyrodazol exceeds the ketorolac and on the hot plate models it is similar to the morphine hydrochloride.
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1. Andersen KV Nikolajsen L Haraldsted V Odgaard A Soballe K. Local infiltration analgesia for total knee arthroplasty: should ketorolac be added?. Br J Anaesth. 2013 (doi: 10.1093/bja/aet030)
2. Barkin Robert L. Barkin D Pharmacologic Management of Acute and Chronic Pain: Focus on Drug Interactions and Patient-Specific Pharmacotherapeutic Selection.Southern Medical Journal. 2001; 94 (8): 756-770.
3. Blyth FM March LM Brnabic AJM Jorm LR Williamson M Cousins MJ. Chronic pain in Australia: a prevalence study. Pain. 2001; 89(2): 127-134.
4. Compton WM Volkow ND Major increases in opioid analgesic abuse in the United States: Concerns and strategies. Drug and Alcohol Dependence. 2006; 81:103-107.
5. D`Amoue FE. A method for determining lose of pain sensation . J. Pharmacol. Exp. Ther. 1941;72: 74.
6. Gad CS Chengelis CP. Acute Toxicology Testing Second Edition San Diego Academic Press 1997:534.
7. Handley DA Carvoni P McCray JE McCullough JR. Preclinical Enantioselective Pharmacology of (R)- and (S)- Ketorolac. J Clin Pharmacol. 1998; 38: 25-35.
8. King TE Joynes RL Grau JW Tail-flick test: II. The role of supraspinal systems and avoidance learning. Behav Neurosci . 1997;111:754-767.
10. Lugo RA Kern SE. Clinical pharmacokinetics of morphine. J. Pain Palliat Care Pharmacother. 2002; 16(4): 5-18.
11. Mathias SD Kuppermann M Liberman RF Lipschutz RC Steege JF. Chronic pelvic pain: prevalence health-related quality of life and economic correlates.Obstetrics & Gynecology. 1996; 87 (3): 321-327.
12. Mellon RD Bayer BM. Evidence for central opioid receptors in the immunomodulatory effects of morphine: review of potential mechanism(s) of action. J. Neuroimmunol. 1998;83 (1-2): 19-28.
13. OriginLab® Data Analysis and Graphiny Software 2012 (http://www.originlab.com/)
14. Rainsford K.D Profile and mechanisms of gastrointestinal and other side effects of nonsteroidal anti-inflammatory drugs (NSAIDs).The American Journal of Medicine. 1999; 107 (6): 27-35.
15. Scher L Hornig M Pergola C. The molecular mechanism of the inhibition by licofelone of the biosynthesis of 5- lipoxygenase products. British Journal of Pharmacology. 2007;152(4): 471-480.
16. Wiesenfeld-Hallin Z Hao J-X Xu X-J Aldskogius H Seiger A/Genetic factors influence the development of mechanical hypersensitivity motor deficits and morphological amage after transient spinal cord ischemia in the rat. Pain. 1993;55: 235-241.
17. Yadlovskyy OE Movchan OM. Pharmacological analysis of the opioid component action of analgesic pyrodazol / Pharmacology and medical toxicology. 2011;.11(3): 73-77.
18. Vogel WH. Drug Discovery and Evaluation: Pharmacological Assays. Second Edition. (http://web.squ.edu.om/med-Lib/MED_CD/E_CDs/Drug%20Discovery%20and%20Evaluatuon%202002/start.pdf)