The effects of buprenorphine in buprenorphine-maintained volunteers

Eric C. Strain, Sharon L. Walsh, Kenzie L. Preston, Ira A. Liebson, George E. Bigelow

Research output: Contribution to journalArticlepeer-review

50 Scopus citations


Buprenorphine is a mu opioid partial agonist currently used as an analgesic, and being developed for the treatment of opioid dependence. The purpose of this study was to determine the abuse liability of parenteral buprenorphine in volunteers maintained on daily sublingual (SL) buprenorphine (8 mg). In a residential laboratory, eight volunteers underwent pharmacologic challenges two times per week. Medication challenges were 16 h after the daily dose of buprenorphine, and consisted of double-blind IM injections of buprenorphine (4, 8, 16 mg), the prototypic mu opioid agonist hydromorphone (9 and 18 mg), or saline. Assessments consisted of physiologic monitoring, subjects' self-reports, and a trained observer's ratings of drug effects, and were collected for 0.5 h before and 2.0 h following injection. Supplemental doses of IM buprenorphine produced opioid agonist-like effects, indicating some abuse potential of parenteral buprenorphine in buprenorphine-maintained patients. There was incomplete cross-tolerance to the effects of hydromorphone, suggesting that higher maintenance doses of buprenorphine may be needed to maximize clinical efficacy. However, there was a lack of graded dose-effects for hydromorphone, suggesting that buprenorphine's combination of partial agonist effects and high affinity for opioid receptors may limit the magnitude of effects of supplemental full agonists. Finally, participants tolerated cumulative doses of maintenance buprenorphine plus challenge buprenorphine without adverse effects, suggesting higher doses of buprenorphine can be safely administered to opioid dependent patients.

Original languageEnglish
Pages (from-to)329-338
Number of pages10
Issue number4
StatePublished - 1997

Bibliographical note

Funding Information:
Acknowledgements The authors thank Michael Webb, Linda Felch and John Yingling for assistance in data collection and analysis. This study was supported by US Public Health Service Research Scientist Award K05 DA00050 (G.E.B.). Scientist Development Award K20 DA00166 (E.C.S.), R01 DA08045, and R18 DA06120 from the National Institute on Drug Abuse. Some of these data were presented at the annual meeting of the College on Problems of Drug Dependence, Palm Beach, Florida, June 1994.


  • Abuse liability testing
  • Agonist-antagonist
  • Buprenorphine
  • Hydromorphone
  • Opioid dependence

ASJC Scopus subject areas

  • Pharmacology


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