Pharmacokinetics and adverse effects of butorphanol administered by single intravenous injection or continuous intravenous infusion in horses

Am J Vet Res. 2001 Feb;62(2):183-9. doi: 10.2460/ajvr.2001.62.183.

Abstract

Objective: To determine an infusion rate of butorphanol tartrate in horses that would maintain therapeutic plasma drug concentrations while minimizing development of adverse behavioral and gastrointestinal tract effects.

Animals: 10 healthy adult horses.

Procedure: Plasma butorphanol concentrations were determined by use of high-performance liquid chromatography following administration of butorphanol by single IV injection (0.1 to 0.13 mg/kg of body weight) or continuous IV infusion (loading dose, 17.8 microg/kg; infusion dosage, 23.7 microg/kg/h for 24 hours). Pharmacokinetic variables were calculated, and changes in physical examination data, gastrointestinal tract transit time, and behavior were determined over time.

Results: A single IV injection of butorphanol was associated with adverse behavioral and gastrointestinal tract effects including ataxia, decreased borborygmi, and decreased defecation. Elimination half-life of butorphanol was brief (44.37 minutes). Adverse gastrointestinal tract effects were less apparent during continuous 24-hour infusion of butorphanol at a dosage that resulted in a mean plasma concentration of 29 ng/ml, compared with effects after a single IV injection. No adverse behavioral effects were observed during or after continuous infusion.

Conclusions and clinical relevance: Continuous IV infusion of butorphanol for 24 hours maintained plasma butorphanol concentrations within a range associated with analgesia. Adverse behavioral and gastrointestinal tract effects were minimized during infusion, compared with a single injection of butorphanol. Continuous infusion of butorphanol may be a useful treatment to induce analgesia in horses.

Publication types

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

MeSH terms

  • Analgesics, Opioid / administration & dosage
  • Analgesics, Opioid / adverse effects*
  • Analgesics, Opioid / pharmacokinetics*
  • Animals
  • Behavior, Animal / drug effects*
  • Butorphanol / administration & dosage
  • Butorphanol / adverse effects*
  • Butorphanol / pharmacokinetics*
  • Chromatography, High Pressure Liquid
  • Cross-Over Studies
  • Female
  • Gastrointestinal Transit / drug effects*
  • Half-Life
  • Horses / metabolism*
  • Infusions, Intravenous / veterinary
  • Injections, Intravenous / veterinary
  • Male

Substances

  • Analgesics, Opioid
  • Butorphanol