Pharmacological properties of nimesulide

Rainsford, K. D.; Bevilacqua, Maurizio; Dallegri, Franco; Gago, Federico; Ottonello, Luciano; Sandrini, Giorgio; Tassorelli, Cristina; Tavares, I.G.

doi:10.1007/3-7643-7410-1_4

Cited by 5 publications

(5 citation statements)

References 367 publications

(488 reference statements)

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“…These observations are supported by a large amount of studies in laboratory animal models (Sigthorsson et al, 2000) (reviewed -see Bjarnason et al, 2005;Rainsford et al, 2005) showing little or no effects of nimesulide on GI mucosal production of prostaglandins coincident with low GI mucosal injury from this drug.…”

Section: Cox-2 and Anti-infl Ammatory Activitymentioning

confidence: 56%

“…Nimesulide, like some classical NSAIDs exhibits a considerable degree of anti-infl ammatory activity as a consequence of various inhibitory effects on polymorphonuclear neutrophil leucocytes (PMNs) (Dallegri et al, 1990(Dallegri et al, , 1992a(Dallegri et al, , 1992bOttonello et al, 1992Ottonello et al, , 1993Ottonello et al, , 1995Ottonello et al, , 1999Capecchi et al, 1993;Verhoeven et al, 1993;Bevilacqua et al, 1994;Dapino et al, 1994;Tool and Verhoeven, 1995;Bennett and Villa, 2000;Bennett, 2001;Mouithys-Mickalad et al, 2000;Nakatani et al, 2001;Gomez-Gaviro et al, 2002;Bravo-Cuellar et al, 2003;Kimura et al, 2003;Rainsford et al, 2005). These effects are, in some cases, relatively potent compared with the activities of other NSAIDs, and occur within the drug concentrations in plasma or synovial fl uids encountered during therapy with the drug Bennett and Villa, 2000;Bennett, 2001).…”

Section: Cox-2 and Anti-infl Ammatory Activitymentioning

confidence: 97%

“…kidney and vascular systems are considered, in part, to be due to inhibition of the synthesis of physiologically important ("housekeeping") prostaglandins (PGs) E 2 and I 2 in these systems (Vane andBotting, 1995, 2001;Rainsford, 2004a). Inhibition of COX-2 selectively inhibits the synthesis of PGE 2 and other PGs involved in infl ammation and mediating neural signals in pain pathways Vane andBotting, 1995, 2001;Rainsford 2004aRainsford , 2004bRainsford et al, 2005). NSAIDs exhibit different degrees of selectivity in their ability to differentially block COX-1 or COX-2 (Vane andBotting, 1995, 2001;Rainsford, 2004a;Tarnawski and Jones, 2003).…”

Section: Introductionmentioning

confidence: 99%

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Current status of the therapeutic uses and actions of the preferential cyclo-oxygenase-2 NSAID, nimesulide

Rainsford

2006

Inflammopharmacol

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This review summarizes the principal therapeutic responses to the preferential COX-2 NSAID, nimesulide, in treating musculo-skeletal joint symptoms and various acute and chronic pain conditions and the mode of action in relation to therapy in these states. In extensive studies in laboratory animal models and clinical trails in patients nimesulide has been found to have potent analgesic, anti-inflammatory and anti-pyretic activities. It is approved for use in over 50 countries worldwide (including those in the EU, South and Central America, China, India and some other South-East Asia) for the treatment of acute pain, the symptomatic treatment of painful osteoarthritis and primary dysmenorrhoea. Its mode of action in these states is related to the preferential inhibition of the production of cyclo-oxygenase-2 (COX-2) and other inflammatory mediators whose production is controlled by stimulation of cyclic-3 ,5'-adenosine monophosphate (cAMP); this means that nimesulide is a multi-factorial drug in controlling inflammation and pain. The adverse reaction profile of nimesulide is, in general, like that of other NSAIDs. It does, however, have relatively low occurrence of gastro-intestinal (GI) side effects which is related to its low propensity to inhibit the physiologically important COX-1 in the GI mucosa and important physicochemical properties (high pKa of 6.5 and lipophilicity) as well as inhibiting of mast cell derived histamine and acid secretion in the stomach. In contrast with the coxibs, nimesulide has not been found to have appreciable cardiovascular toxicity.

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Section: Cox-2 and Anti-infl Ammatory Activitymentioning

confidence: 56%

Section: Cox-2 and Anti-infl Ammatory Activitymentioning

confidence: 97%

Section: Introductionmentioning

confidence: 99%

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Current status of the therapeutic uses and actions of the preferential cyclo-oxygenase-2 NSAID, nimesulide

Rainsford

2006

Inflammopharmacol

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“…Inhibition of inflammation results from potent inhibitory activity on the COX-2 production of prostaglandin E2 [PGE2] [35]. Nimesulide action is also related to inhibition of histamine release from astrocytes, mast cells and basophils, scavenging of free radicals [hydroxyl radicals], hypochlorous acid production, inhibition of neutrophil adherence, inhibition of PAF from activated platelets, inhibition of metalloproteinases, and reduction of metalloproteinases release, reduction of apoptotic chondrocytes, inhibition of nitric oxide synthase (NOS) with reduction in NO production; thus acting on oxygen reactive species, the key mediators of cell death, and the inflammatory process [36]. In addition, nimesulide shares with other NSAIDs an effect on glucocorticoid receptors through which an increase in the activity of endogenous glucocorticoidsteroids is achieved [37,38].…”

Section: The Chemical Characteristics Phar-macokinetics and Biologicmentioning

confidence: 99%

The Spectrum of Nimesulide-Induced-Hepatotoxicity. An Overview

Bessone¹,

Colombato²,

Fassio³

et al. 2010

AIAAMC

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Nimesulide is the unique molecule of the sulphonanilides class of non-steroidal antiinflammatory drugs [NSAIDs]: Nimesulide has analgesic, anti-pyretic, potent anti-inflammatory activities and very good gastro-intestinal [GI] tolerability. Therapeutic action is multifactorial, including cyclooxigenase-2 (COX-2) inhibition, scavenging of free radicals and inhibition of various pathways of inflammation. Nimesulide is oxidatively metabolised via liver cytochromes P450. Several unproven hepatotoxicy-predisposing-factors thought to be present in rheumatologic patients have been linked to a higher incidence of hepatic reactions in this sub-population. However, the molecular mechanism underlying hepatotoxicy remains to be elucidated. Nimesulide has been associated over two decades with reports of severe liver damage. The clinical presentation of nimesulide-related-hepatoxicity includes, malaise, pruritus, a wide range of ALT/AST elevation, and an average 4 fold elevation of alkaline phosphatase and GGT. Liver biopsy shows a predominance of hepatocellular involvement, less frequently cholestatic and mixed patterns. Both, the hepatitis pattern and the mixed-type combining cholestatic jaundice, might evolve into fulminant hepatic failure. However, the incidence of nimesulide-inducedhepatotoxicity is not homogeneous across the medical literature. Indeed, most of the countries find it to be comparable to that of other NSAIDs, while a significant higher hepatotoxicity is suggested by reports from Finland, Ireland and Argentina. Our series in Argentina comprising 43 cases is worrisome particularly because it evidences a significant proportion of severe forms. In the present work we analyze the epidemilogical characteristics of nimesulide-induced-hepatotoxicity and we describe the clinical and histologic spectrum of nimesulide-associated-liver damage based on the comparison of our series of 43 cases and worldwide published observations in the pertinent medical literature.

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“…This selectivity minimizes the adverse gastrointestinal effects often associated with nonselective NSAIDs, such as gastric irritation and ulceration. Nimesulide has also shown antiinflammatory and analgesic properties, making it a valuable option for managing acute and chronic pain and musculoskeletal disorders [2,3]. On the other hand, NAP is a nonselective NSAID that inhibits both COX-1 and COX-2 enzymes, leading to a more comprehensive suppression of prostaglandin synthesis.…”

Section: Introductionmentioning

confidence: 99%

A green liquid chromatographic method using ethanol in mobile phase for the determination of nimesulide and naproxen in gel formulations

YILDIRIM

2023

Turkish Journal of Analytical Chemistry

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Dеtеrmination of nonsteroidal anti-inflammatory drugs (NSAIDs) in pharmacеutical formulations hеlps to еnsurе that thеy arе manufacturеd to thе corrеct spеcifications. Consequently, simple, reliable, and environmentally friendly analytical methods are needed for the quality control of NSAID formulations. In this study, a novel and green liquid chromatographic method was developed for the determination of nimesulide (NIM) and naproxen (NAP) in gel formulations by employing ethanol as a green alternative to hazardous methanol and acetonitrile. The high viscosity of ethanol was compensated by employing a Chromolith HighResolution RP18e monolithic column (100 × 4.6 mm) with low flow resistance. Box-Behnken design with desirability function was employed for the optimization of selected significant parameters: pH (2.8-4), ethanol ratio in the mobile phase (35-55%), and flow rate (0.7-1.5 mL/min). Under optimum conditions, satisfactory separation of analytes was achieved within 5 min. Calibration curves for both analytes were linear between 1-50 μg/mL. Accuracies of intra- and inter-day experiments at low-, middle-, and high-quality control levels ranged from 99.0-101.5% with relative standard deviation values lower than 2.3%. The limits of detection were 0.27 and 0.62 µg/mL for NIM and NAP, respectively. The applicability of the method was demonstrated by analyzing gel formulations. The results of this study indicated that monolithic columns in combination with ethanol as a mobile phase component could be considered a desirable and green alternative for the routine analysis of NSAIDs in quality control laboratories.

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Pharmacological properties of nimesulide

Cited by 5 publications

References 367 publications

Current status of the therapeutic uses and actions of the preferential cyclo-oxygenase-2 NSAID, nimesulide

Current status of the therapeutic uses and actions of the preferential cyclo-oxygenase-2 NSAID, nimesulide

The Spectrum of Nimesulide-Induced-Hepatotoxicity. An Overview

A green liquid chromatographic method using ethanol in mobile phase for the determination of nimesulide and naproxen in gel formulations

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