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Etodolac clinical pharmacokinetics

D R Brocks1, F Jamali

  • 1SmithKline Beecham Pharmaceuticals, Drug Metabolism and Pharmacokinetics, King of Prussia, Pennsylvania.

Clinical Pharmacokinetics
|April 1, 1994
PubMed
Summary

Etodolac, a chiral NSAID, exhibits unique stereoselective pharmacokinetics with higher R-enantiomer levels than the active S-enantiomer. Its disposition involves extensive distribution and metabolism, with implications for arthritis treatment.

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Area of Science:

  • Pharmacology
  • Drug Metabolism and Disposition

Background:

  • Etodolac is a chiral nonsteroidal anti-inflammatory drug (NSAID) used for arthritis and pain relief.
  • It is marketed as a racemate, with distinct pharmacokinetic profiles for its enantiomers.

Purpose of the Study:

  • To investigate the unique disposition features and stereoselective pharmacokinetics of etodolac.
  • To understand the absorption, distribution, metabolism, and elimination (ADME) of etodolac enantiomers.

Main Methods:

  • Analysis of plasma and synovial fluid concentrations of etodolac and its metabolites.
  • Pharmacokinetic evaluation in healthy volunteers and patients with arthritis.

Main Results:

  • The R-enantiomer of etodolac is found at 10-fold higher concentrations than the S-enantiomer in plasma.
  • Etodolac is well absorbed, highly protein-bound, and extensively metabolized to oxidised metabolites and acyl-glucuronides.
  • The volume of distribution is higher for the S-enantiomer due to less plasma protein binding.

Conclusions:

  • Etodolac's stereoselective pharmacokinetics, particularly the enantiomer concentration difference and distribution, are unique among chiral NSAIDs.
  • Acyl-glucuronides of etodolac are present in plasma and synovial fluid, with potential renal clearance implications.
  • Hepatic cirrhosis and aging do not significantly affect racemic etodolac pharmacokinetics in individuals with good kidney function.

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