Clinical Pharmacokinetics of Nimesulide

@article{Bernareggi1998ClinicalPO,
  title={Clinical Pharmacokinetics of Nimesulide},
  author={Alberto Bernareggi},
  journal={Clinical Pharmacokinetics},
  year={1998},
  volume={35},
  pages={247-274}
}
  • A. Bernareggi
  • Published 1 October 1998
  • Medicine, Biology, Chemistry
  • Clinical Pharmacokinetics
Nimesulide is a selective COX-2 inhibitor used in a variety of inflammatory, pain and fever states. After healthy volunteers received oral nimesulide 100mg in tablet, granule or suspension form the drug was rapidly and extensively absorbed. Mean peak concentrations (Cmax) of 2.86 to 6.50 mg/L were achieved within 1.22 to 2.75 hours of administration. The presence of food did not reduce either the rate or extent of nimesulide absorption. When nimesulide was administered in the suppository form… 
Pharmacokinetics of nimesulide
TLDR
This chapter provides an up-to-date description of the processes related to nimesulide absorption, distribution, metabolism and elimination in animal species and in humans.
Pharmacokinetics and bioavailability of nimesulide in goats.
TLDR
The pharmacokinetic data suggest that nimesulide given intramuscularly may be useful in the treatment of inflammatory disease conditions in goats.
Oral and intravenous administration of nimesulide in the horse: rational dosage regimen from pharmacokinetic and pharmacodynamic data.
TLDR
The findings suggest that 1.5 mg/kg bwt may produce adequate clinical effects, and the dosing interval should be 12-24 h depending on condition severity, however, at that dose, the concentration in the animal exceeds the in vitro IC50 for both isoforms, so that COX-1/COX-2 selectivity is lost and side-effects due to COx-1 inhibition are a possibility.
Pharmacokinetic profile and in vitro selective cyclooxygenase-2 inhibition by nimesulide in the dog.
TLDR
The pharmacokinetic properties and in vitro potency of nimesulide, a nonsteroidal anti-inflammatory drug (NSAID) were investigated and it was concluded that at the currently recommended dosage regimen (5 mg/kg), the plasma concentration totally inhibits COX-2 and partly inhibitsCOX-1 isoenzyme.
Pharmacokinetic Profile of Nimesulide in Bovine Calves
TLDR
Pharmacokinetic data suggests that nimesulide given intramuscularly may be useful in the treatment of inflammatory disease conditions in bovines.
The Biotransformation and Pharmacokinetics of 14C-Nimesulide in Humans Following a Single Dose Oral Administration
TLDR
The biotransformation pathway for nimesulide in man has now been comprehensively determined with 92% of the urinary metabolites fully characterised and may help in understanding the mechanisms of hepatotoxicity from this drug.
A pharmacokinetic comparison of three pharmaceutical formulations of nimesulide in healthy volunteers.
TLDR
Only a 90% confidence interval for the relative differences of log-transformed AUC(0-infinity) values of nimesulide absorbed from mouth dissolving tablets vs. suspension is expected after switching the patient from one to another.
Urinary Excretion and Renal Clearance of Nimesulide in Male Volunteers
TLDR
Urinary excretion and renal clearance of nimesulide after its oral administration correlated with creatinine clearance and statistical analysis was performed in order to determine the significance of the results.
Plasma and Synovial Fluid Concentrations of Nimesulide and its Main Metabolite after a Single or Repeated Oral Administration in Patients with Knee Osteoarthritis
TLDR
Evaluated plasma and synovial fluid concentrations of the non-steroidal anti-inflammatory drug nimesulide and its major metabolite (hydroxynimesulides, M1) after a single 100 mg dose and a repeated administration, 100 mg twice a day, in patients with osteoarthritis of the knee and joint effusion help to explain the rapid onset of the analgesic effect of nimesULide demonstrated in several clinical conditions.
Nimesulide, a Cyclooxygenase-2 Preferential Inhibitor, Impairs Renal Function in the Newborn Rabbit
TLDR
The experiments confirm that prostaglandins, by maintaining renal vasodilation, play a key role in the delicate balance regulating neonatal GFR, and COX2-selective/preferential inhibitors thus should be prescribed with the same caution as nonselective NSAIDs during pregnancy and in the neonatal period.
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