Effect of age and disease on the pharmacokinetics of nimesulide.
Nimesulide is a nonsteroidal anti-inflammatory agent with additional antipyretic and analgesic activity. The recommended dosage is 100 to 200 mg twice daily orally or rectally. The pharmacokinetics profile of nimesulide has been studied in patients with a predisposition for altered pharmacokinetics. The pharmacokinetic profile of nimesulide and its hydroxy metabolite was not altered when the drug was administered in a standard regimen (100mg twice daily) to elderly patients aged < 80 years, suggesting that dosage adjustment is not necessary for such patients. In children aged 7 to 9 years, nimesulide 50mg administered in a granular formulation showed a tendency for greater absorption and elimination than that recorded for adults administered nimesulide in tablet form. These results suggest that the pharmacokinetic profile of this paediatric formulation should be assessed in children aged < 7 years to determine whether their dosage should be adjusted. In patients with moderate renal insufficiency, the pharmacokinetic profile of nimesulide was not altered even though the terminal elimination half-life of its hydroxy metabolite was greater and this resulted in slight accumulation with multiple dose administration in a standard regimen. This slight effect was not considered to be clinically significant and therefore dosage adjustment for patients with moderate renal impairment appears unnecessary. Administration of nimesulide to patients with severe renal failure should be avoided until the propensity and significance of hydroxy-nimesulide accumulation is quantified in this patient group. The pharmacokinetic profile of nimesulide has not been determined in patients with hepatic disease.(ABSTRACT TRUNCATED AT 250 WORDS)
Olive
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Department of Pharmacology, Hôpital Saint-Vincent de Paul, Faculty of Medicine COCHIN-University Rene Descartes, Paris, France.
Rey
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D000367:Age Factors; D000368:Aged; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000493:pharmacokinetics*; D002648:Child; D006801:Humans; D007674:Kidney Diseases / Q000378:metabolism*; D013449:Sulfonamides / Q000493:pharmacokinetics*
D000894:Anti-Inflammatory Agents, Non-Steroidal; D013449:Sulfonamides; C012655:nimesulide