Pharmacokinetics and pharmacodynamics of glucocorticoid suspensions after intra-articular administration

Clin Pharmacol Ther. 1986 Mar;39(3):313-7. doi: 10.1038/clpt.1986.45.

Abstract

Triamcinolone acetonide, triamcinolone hexacetonide, and a combination of betamethasone phosphate and acetate were given intra-articularly in different doses. Plasma levels of the steroids were measured and pharmacokinetic parameters were calculated. As a pharmacodynamic parameter for systemic steroid activity, plasma hydrocortisone levels were monitored for 3 weeks. Results indicate complete absorption from the site of injection over a period of 2 to 3 weeks. Because of its lower solubility, triamcinolone hexacetonide is absorbed slower than triamcinolone acetonide, thus maintaining synovial levels for a longer time and creating lower systemic corticoid levels. Endogenous hydrocortisone suppression correlated with exogenous steroid levels. Threshold concentrations for maximum suppression were determined.

MeSH terms

  • Absorption
  • Adolescent
  • Adult
  • Aged
  • Betamethasone / blood
  • Female
  • Half-Life
  • Humans
  • Hydrocortisone / blood
  • Injections, Intra-Articular
  • Kinetics
  • Male
  • Middle Aged
  • Radioimmunoassay
  • Triamcinolone Acetonide / analogs & derivatives
  • Triamcinolone Acetonide / blood
  • Triamcinolone Acetonide / metabolism*

Substances

  • Betamethasone
  • Triamcinolone Acetonide
  • triamcinolone hexacetonide
  • Hydrocortisone