Pharmacokinetics of butorphanol in cats after intramuscular and buccal transmucosal administration

Am J Vet Res. 2008 Dec;69(12):1548-54. doi: 10.2460/ajvr.69.12.1548.

Abstract

Objective: To determine the pharmacokinetics of butorphanol in cats following IM and buccal transmucosal (BTM) administration, to determine the relative bioavailability of butorphanol following BTM administration, and to extrapolate a plasma concentration associated with antinociception on the basis of existing data from pharmacologic studies of butorphanol in cats.

Animals: 6 healthy adult cats.

Procedures: Following IM or BTM butorphanol tartrate (0.4 mg/kg) administration to cats in a 2-way crossover trial, plasma samples were obtained from blood collected via a central venous catheter during a 9-hour period. Plasma butorphanol concentrations were determined by high-performance liquid chromatography.

Results: Data from 1 cat contained outliers and were excluded from pharmacokinetic analysis. Mean+/-SD terminal half-life of butorphanol for the remaining 5 cats was 6.3+/-2.8 hours and 5.2+/-1.7 hours for IM and BTM administration, respectively. Peak plasma butorphanol concentrations were 132.0 and 34.4 ng/mL for IM and BTM administration, respectively. Time to maximal plasma concentration was 0.35 and 1.1 hours for IM and BTM administration, respectively. Extent of butorphanol absorption was 37.16% following BTM application. On the basis of data from extant pharmacologic studies of butorphanol in cats, mean+/-SD duration of antinociception was 155+/-130 minutes. The estimated plasma concentration corresponding to this time point was 45 ng/mL.

Conclusions and clinical relevance: In cats, IM butorphanol administration at 0.4 mg/kg maintained a plasma concentration of >45 ng/mL for 2.7+/-2.2 hours, whereas BTM administration at the same dose was not effective at maintaining plasma concentrations at >45 ng/mL.

Publication types

  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Buccal
  • Analgesics, Opioid / administration & dosage*
  • Analgesics, Opioid / blood
  • Analgesics, Opioid / pharmacokinetics*
  • Animals
  • Butorphanol / administration & dosage*
  • Butorphanol / blood
  • Butorphanol / pharmacokinetics*
  • Cats / metabolism*
  • Cross-Over Studies
  • Female
  • Injections, Intramuscular
  • Male

Substances

  • Analgesics, Opioid
  • Butorphanol