Dexamethasone and prednisolone in the horse: pharmacokinetics and action on the adrenal gland

Am J Vet Res. 1984 Sep;45(9):1750-6.

Abstract

Pharmacokinetics of dexamethasone and prednisolone were studied in 6 horses given dexamethasone alcohol (IV or IM) or dexamethasone 21-isonicotinate as a solution IV or IM (50 micrograms/kg of body weight), prednisolone 21-sodium succinate IV or IM (0.6 mg/kg of body weight), or prednisolone acetate IM (0.6 mg/kg of body weight). Plasma concentrations were determined using a high-performance liquid chromatographic method. After dexamethasone alcohol (IV) or dexamethasone 21-isonicotinate (IV), the half-life of elimination was similar (53 minutes) for both formulations. After dexamethasone (alcohol and isonicotinate, IM), concentrations were low or nondetected. After prednisolone 21-sodium succinate (IV), the half-life of elimination (99.5 minutes) was significantly (P less than 0.01) longer than that for dexamethasone. After prednisolone 21-sodium succinate (IM), absorption was rapid and bioavailability was high. After prednisolone acetate (IM), absorption was slow and prednisolone was present in plasma for about 7 days. Due to the nonlinearity of prednisolone kinetics, a bioavailability higher than 100% was obtained. The basal plasma hydrocortisone concentration was approximately 70 ng/ml. After dexamethasone (IV or IM), plasma hydrocortisone values decreased after a 2-hour delay and returned to base line after a 3 to 4 day delay. After prednisolone 21-sodium succinate (IV or IM), plasma hydrocortisone decreased immediately (IV) or rapidly (IM) and returned to base line after a 24-hour delay. After prednisolone acetate (IM), plasma hydrocortisone decreased for up to 21 days.

Publication types

  • Comparative Study

MeSH terms

  • Absorption
  • Adrenal Glands / drug effects*
  • Animals
  • Biological Availability
  • Dexamethasone / analogs & derivatives*
  • Dexamethasone / metabolism*
  • Dexamethasone Isonicotinate / metabolism*
  • Dexamethasone Isonicotinate / pharmacology
  • Female
  • Half-Life
  • Horses / metabolism*
  • Hydrocortisone / blood
  • Kinetics
  • Male
  • Prednisolone / analogs & derivatives*
  • Prednisolone / metabolism
  • Prednisolone / pharmacology

Substances

  • Dexamethasone
  • prednisolone acetate
  • Dexamethasone Isonicotinate
  • Prednisolone
  • prednisolone hemisuccinate
  • Hydrocortisone