Effect of age and gender on tirilazad pharmacokinetics in humans

Clin Pharmacol Ther. 1994 Apr;55(4):378-84. doi: 10.1038/clpt.1994.45.


Tirilazad mesylate pharmacokinetics were assessed in 12 young and 12 elderly volunteers (six men and six women per age group). Subjects received single 10-minute intravenous infusions of 1.5 mg/kg and 3.0 mg/kg tirilazad mesylate. Plasma tirilazad mesylate concentrations were determined by HPLC. There were no significant dose effects on clearance, but half-life increased with dose because of assay insensitivity at the lower dose. Mean half-lives were 16.3 +/- 15.5 and 21.4 +/- 12.6 hours for young and elderly subjects, respectively, at the 3.0 mg/kg dose. At the same dose, mean tirilazad mesylate systemic clearance was 0.630 +/- 0.254 and 0.428 +/- 0.090 L/hr/kg, respectively. The decreased clearance in elderly volunteers was primarily attributable to a lower clearance in elderly women relative to young women. The small effect of age on tirilazad clearance is likely to have minimum clinical impact. Tirilazad clearance was approximately 40% higher in young women than in young men. The clinical importance of this observation is unknown.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Aged
  • Aged, 80 and over
  • Aging / metabolism*
  • Female
  • Half-Life
  • Humans
  • Infusions, Intravenous
  • Lipid Peroxides / antagonists & inhibitors*
  • Male
  • Pregnatrienes / administration & dosage
  • Pregnatrienes / blood
  • Pregnatrienes / pharmacokinetics*
  • Regression Analysis
  • Sex Characteristics*


  • Lipid Peroxides
  • Pregnatrienes
  • tirilazad