The pharmacokinetics of piroxicam in elderly persons with and without renal impairment

Br J Clin Pharmacol. 1994 Jan;37(1):1-5. doi: 10.1111/j.1365-2125.1994.tb04230.x.

Abstract

1. Piroxicam pharmacokinetics were assessed in three groups of subjects: (1) young healthy volunteers, (2) healthy elderly subjects (mean +/- s.d. creatinine clearance 88 +/- 13 ml min-1), and (3) elderly patients with renal insufficiency (creatinine clearance 60 +/- 10 ml min-1) following the administration of piroxicam 20 mg as a single dose and after chronic dosing of 20 mg once daily for 4 weeks. 2. Piroxicam and 5'-hydroxypiroxicam concentrations were measured by h.p.l.c. in serum and urine samples collected for 96 h after the single dose and for 144 h after chronic dosing. Unbound concentrations of piroxicam were determined by ultrafiltration. 3. Elimination half-lives, steady state concentrations of piroxicam and 5'-hydroxypiroxicam, clearances of total and unbound piroxicam, volumes of distribution normalized for body weight, and urinary recovery of 5'-hydroxypiroxicam were not influenced by age or renal function. Volumes of distribution after the single dose were significantly lower in women compared with men (mean +/- s.d. 10.0 +/- 2.9 l vs 12.9 +/- 5.0 l; 95% confidence interval of the difference 0.1 to 5.6). 4. Percent unbound piroxicam values were 1.46 +/- 0.3% after the single dose and 1.45 +/- 0.2% at steady state. There were significant reductions in clearance and clearance of unbound piroxicam between single and chronic doses. The half-lives of 5'-hydroxypiroxicam (80.9 +/- 44 h) were significantly longer than those of piroxicam (54.9 +/- 26 h) after chronic dosing.

Publication types

  • Comparative Study
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Adult
  • Aged
  • Aging / metabolism*
  • Chromatography, High Pressure Liquid
  • Creatinine / urine
  • Female
  • Half-Life
  • Humans
  • Male
  • Piroxicam / analogs & derivatives
  • Piroxicam / blood
  • Piroxicam / pharmacokinetics*
  • Piroxicam / urine
  • Protein Binding
  • Renal Insufficiency / blood
  • Renal Insufficiency / metabolism*

Substances

  • Piroxicam
  • 5'-hydroxypiroxicam
  • Creatinine