Comparative analgesic activity of nimesulide and diclofenac by intramuscular route: correlation with pharmacokinetic profile of nimesulide

Pharmacology
S K GuptaS Sengupta

Abstract

Nimesulide, a selective cyclooxygenase-2-inhibiting nonsteroidal anti-inflammatory drug, has been found to be a potent anti-inflammatory and analgesic drug, when administered orally, rectally or topically. The aim of the present study was to evaluate the comparative efficacy of intramuscularly injected nimesulide with that of diclofenac and to elucidate the pharmacokinetic profile of this formulation. Swiss albino mice were used in the experiment. Analgesic activity was tested using the acetic acid writhing test and the tail-flick latency test. Plasma levels of nimesulide and its active metabolite, hydroxynimesulide, were determined by a HPLC method. A peak analgesic effect was observed between 60 and 120 min, while Cmax (10.6 +/- 3.8 micrograms/ml) of nimesulide was reached at 60 min (Tmax). Analgesia was induced within 15 min of administration of nimesulide and was significantly higher than that of diclofenac at 90 and 120 min posttreatment in the writhing reflex and at 60 and 90 min in the tail-flick latency test. The results indicate that intramuscularly injected nimesulide may be an alternative mode of administration in uncooperative patients or when immediate analgesic effects are warranted.

Citations

Feb 19, 2008·Neuroreport·Melanie A PaquetteStephen Paul Berger
Dec 11, 1999·Alcoholism, Clinical and Experimental Research·J L CookD M Olson
Aug 12, 1999·Acta Psychiatrica Scandinavica·T Baptista
Apr 18, 2008·Canadian Journal of Physiology and Pharmacology·Dusan MladenovićOlivera Stanojlović
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Nov 20, 2002·The Journal of Pharmacology and Experimental Therapeutics·Shingo TsujiMasatsugu Hori
Aug 5, 2020·AAPS PharmSciTech·Neha PanchalSubheet Kumar Jain

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