The effects of butorphanol administered by a nasal spray (transnasal,
TN) and by intramuscular (IM) injection were compared to determine the
onset of action, relative potency, profile of effects, and relative a
buse liability of TN butorphanol. TN/IM placebo and TN and IM butorpha
nol (1, 2, and 4 mg) were tested in seven male opioid abusers not curr
ently physically dependent on opioids using a double-blind, double-dum
my, Latin square design. Measures of subjective, behavioral and physio
logical response were assessed. The onset and duration of action of bu
torphanol administered by the IM and TN routes were similar at low dos
es, but onset of TN butorphanol 4 mg was slower than that of 4 mg IM.
IM butorphanol produced miosis, some opiate-like behavioral and subjec
tive effects, and increasing dysphoric sedation and perceptual effects
with increasing dose. TN and IM butorphanol 1 and 2 mg produced effec
ts that were qualitatively and quantitatively similar; however, TN but
orphanol 4 mg was less potent than 4 mg IM. Pharmacodynamic evidence s
uggests that the abuse potential of TN butorphanol is not different fr
om that of IM butorphanol.