Effects of buprenorphine versus buprenorphine/naloxone tablets in non-dependent opioid abusers.
BACKGROUND
Buprenorphine is an opioid agonist-antagonist under development in the United States as a sublingual medication for treatment of opioid dependence. Buprenorphine may be abused; therefore, tablets combining buprenorphine with naloxone have been developed with the intent of reducing the abuse risk in people physically dependent upon opioids. The characteristics and abuse potential of buprenorphine and buprenorphine/naloxone tablets in non-dependent opioid abusers have not been determined. Non-parenteral abuse of opioids such as buprenorphine may be more likely in people who have less severe substance abuse disorders (e.g., are not physically dependent upon opioids).


OBJECTIVE
To assess the abuse potential of sublingual buprenorphine and buprenorphine/naloxone tablets in non-dependent opioid abusers.


METHODS
Subjects (n=7) were tested with sublingual buprenorphine (4, 8, 16 mg), sublingual buprenorphine/naloxone (1/0.25, 2/0.5, 4/1, 8/2, 16/4 mg), as well as intramuscular hydromorphone as an opioid agonist control (2, 4 mg) and placebo in laboratory sessions conducted twice per week. Dosing was double-blind and double-dummy.


RESULTS
The higher doses of both buprenorphine and buprenorphine/naloxone produced similar opioid agonist-like effects. The onset of these effects was slowed, consistent with the sublingual route of administration, and the magnitude of effects was moderate. There was no evidence to suggest the addition of naloxone attenuated buprenorphine's opioid agonist effects in this population when buprenorphine was delivered by the sublingual route.


CONCLUSIONS
These results suggest that sublingual buprenorphine and buprenorphine/naloxone may both be abused by opioid users who are not physically dependent upon opioids.
Strain
E C
EC
Department of Psychiatry and Behavioral Sciences, The Johns Hopkins University School of Medicine, Baltimore, MD 21224, USA. ecsgss@aol.com
Stoller
K
K
Walsh
S L
SL
Bigelow
G E
GE
D000286:Administration, Sublingual; D000328:Adult; D000701:Analgesics, Opioid / Q000008:administration & dosage / Q000627:therapeutic use; D002047:Buprenorphine / Q000008:administration & dosage / Q000627:therapeutic use*; D004338:Drug Combinations; D006801:Humans; D004091:Hydromorphone / Q000008:administration & dosage / Q000627:therapeutic use; D007275:Injections, Intravenous; D008297:Male; D008875:Middle Aged; D009043:Motor Activity / Q000187:drug effects; D009270:Naloxone / Q000008:administration & dosage / Q000627:therapeutic use*; D009292:Narcotic Antagonists / Q000008:administration & dosage / Q000627:therapeutic use*; D009293:Opioid-Related Disorders / Q000188:drug therapy* / Q000523:psychology; D013607:Tablets; D013997:Time Factors
D000701:Analgesics, Opioid; D004338:Drug Combinations; D009292:Narcotic Antagonists; D013607:Tablets; D009270:Naloxone; D002047:Buprenorphine; D004091:Hydromorphone