Acute pain: a multifaceted challenge - the role of nimesulide.

BACKGROUND: This article summarizes the outcome from an international consensus meeting, which took place in Vienna on 4 November 2014. SCOPE: The aim of the meeting was to provide the state of the art on the pathophysiology and treatment of acute pain with special emphasis on nimesulide, a non-steroidal anti-inflammatory drug (NSAID) indicated for the treatment of acute pain and primary dysmenorrhea. Besides the data on the mechanisms of acute inflammatory pain and on the efficacy and safety of nimesulide in patients affected by different forms of acute pain, the clinical experience of attending experts was discussed based on selected case reports. RESULTS: The members of this consensus group recognized that nimesulide is a NSAID highly effective in the treatment of several painful situations with an acute inflammatory component including primary dysmenorrhea. Although safety concerns regarding nimesulide have emerged in recent years, both robust new epidemiological data and clinical experience confirm a positive benefit/risk profile of nimesulide in the treatment of several forms of acute pain. CONCLUSIONS: The members of this international consensus group concluded that nimesulide, when used appropriately, remains a particularly valuable and safe option for the treatment of several conditions characterized by the presence of acute inflammatory pain because of the rapid onset of the analgesic action, and the positive evidence-based benefit/risk profile.

Profile of prostaglandins generated in the detrusor muscle of rat urinary bladder: effects of adenosine triphosphate and adenosine.

The generation and release of PGE2, PGF2 alpha, PGD2, TXB2 and 6-keto-PGF1 alpha in the rat detrusor muscle were studied by means of radioimmunoassays. The effect of ATP (0.1 mmol/1) and adenosine (0.1 mmol/1) on the content and profile of PGs in the incubation medium was investigated. It was found that PGE2 and 6-keto-PGF1 alpha accounted for more than 80% of the total PG activity. ATP increased the amounts of PGs in the incubation medium (percentage change of the control values, N = 6: PGE2 54.53 +/- 12.69, PGF2 alpha 31.01 +/- 8.82, PGD2 44.52 +/- 12.36, TXB2 17.29 +/- 10.45, 6-keto-PGF1 alpha 36.62 +/- 5.0) but did not change their profile. Adenosine had no effect on either content or profile of the PGs. The results suggest that ATP but ot adenosine may activate PG biosynthesis via P2-purinoceptor-mediated mechanisms.

On the mechanism of the anti-inflammatory action of the newly-synthesized benzoylpyrazolone derivatives.

One of the basic mechanisms of action of the nonsteroid anti-inflammatory agents is associated with prostaglandin synthesis. The effects of 1-phenyl-3-methyl-4 (4)-chlorbenzoylpyrazolone-5 (No. 151) and 1-phenyl-2-benzoyl-3-methylpyrazolone-5 (No. 76) on the quantity of prostaglandins and on the invasion of polymorphonuclear leucocytes in inflammatory exudate have been studied. Experimental inflammation is induced after Higgs et al. (1976). The level of prostaglandins in the exudate is determined through cascade superfusion of isolated smooth-muscle organs. The level of prostaglandins is found to decrease in animals treated with No. 151 and indomethacine, and to increase under the effect of No. 76. The invasion of the focus with polymorphonuclear leucocytes is inhibited by No. 151 and indomethacine. On the basis of the results obtained, No. 151 is assumed to belong to the group of prostaglandin-synthetase inhibitors, according to its mechanism of action.