Buprenorphine and naloxone interactions in opiate-dependent volunteers.
OBJECTIVE
Sublingual buprenorphine appears useful in the treatment of opiate dependence. A combination sublingual dose of buprenorphine and naloxone could have less potential for parenteral use by opiate-dependent individuals. To estimate the abuse potential of a combination formulation, we assessed the parenteral effects of a buprenorphine and naloxone combination in untreated heroin addicts.


METHODS
Eight healthy, opiate-dependent daily users of heroin were given, under double-blind conditions on four separate occasions, either (1) 2 mg buprenorphine, (2) 2 mg naloxone, (3) 2 mg buprenorphine and 2 mg naloxone combined, or (4) placebo as a single intravenous infusion during a 30-second interval. Opiate agonist and antagonist physiologic and subjective effects were measured. Data were analyzed by analysis of variance.


RESULTS
Buprenorphine increased opiate intoxication and relieved withdrawal. The buprenorphine and naloxone combination precipitated opiate withdrawal and was unpleasant and dysphoric in all subjects. Fifty percent of the subjects were unable to distinguish between naloxone alone and the combined medications during the first hour of testing.


CONCLUSIONS
The buprenorphine and naloxone combination has a low abuse potential in opiate-dependent daily heroin users.
Mendelson
J
J
Drug Dependence Research Center, Langley Porter Psychiatric Institute, University of California, San Francisco 94143-0984, USA.
Jones
R T
RT
Fernandez
I
I
Welm
S
S
Melby
A K
AK
Baggott
M J
MJ
D000328:Adult; D002047:Buprenorphine / Q000008:administration & dosage*; D018592:Cross-Over Studies; D004311:Double-Blind Method; D004359:Drug Therapy, Combination; D005260:Female; D006801:Humans; D008297:Male; D008875:Middle Aged; D009270:Naloxone / Q000008:administration & dosage*; D009292:Narcotic Antagonists / Q000008:administration & dosage*; D009293:Opioid-Related Disorders / Q000188:drug therapy*
D009292:Narcotic Antagonists; D009270:Naloxone; D002047:Buprenorphine