Buprenorphine reduces cerebral glucose metabolism in polydrug abusers.
Buprenorphine is a mixed opioid agonist-antagonist, which acts as a partial mu agonist and a kappa antagonist. The present study evaluated the acute effects of buprenorphine on cerebral glucose metabolism (CMRglc) in six human substance abusers using a double-blind, placebo-controlled, counterbalanced, crossover design. Each subject participated in two positron emission tomographic (PET) studies, 1 week apart, following the injection of buprenorphine (1 mg, intramuscularly) and placebo. Buprenorphine significantly reduced CMRglc and the regional cerebral metabolic rate for glucose (rCMRglc) by up to 32% in all but three of 22 bilateral and in 4 midline regions (p < .05). No region showed an increase in rCMRglc. Buprenorphine also produced miosis, respiratory depression, and subjective ratings of euphoria and sedation in comparison to placebo (p < .05). These observations extend previous findings of reduced CMRglc following acute treatment with morphine and other nonopioid euphorigenic drugs.
Walsh
S L
SL
Department of Psychiatry, Johns Hopkins University School of Medicine, Baltimore, MD.
Gilson
S F
SF
Jasinski
D R
DR
Stapleton
J M
JM
Phillips
R L
RL
Dannals
R F
RF
Schmidt
J
J
Preston
K L
KL
Grayson
R
R
Bigelow
G E
GE
D000328:Adult; D001794:Blood Pressure / Q000187:drug effects; D001921:Brain / Q000033:anatomy & histology; D001923:Brain Chemistry / Q000187:drug effects*; D002047:Buprenorphine / Q000494:pharmacology*; D018592:Cross-Over Studies; D004311:Double-Blind Method; D005059:Euphoria / Q000187:drug effects; D005947:Glucose / Q000378:metabolism*; D006339:Heart Rate / Q000187:drug effects; D006801:Humans; D007700:Kinetics; D008279:Magnetic Resonance Imaging; D008297:Male; D009020:Morphine / Q000494:pharmacology; D011680:Pupil / Q000187:drug effects; D011957:Receptors, Opioid / Q000187:drug effects; D015656:Respiratory Mechanics / Q000187:drug effects; D019966:Substance-Related Disorders / Q000378:metabolism*; D014055:Tomography, Emission-Computed
D011957:Receptors, Opioid; D002047:Buprenorphine; D009020:Morphine; D005947:Glucose