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Comparisons of Analgesic Potency and Side Effects of Buprenorphine and Buprenorphine With Ultra-low-dose Naloxone

Ling, Walter MD; Hillhouse, Maureen PhD; Jenkins, Jessica MA; Miotto, Karen MD; Torrington, Matthew MD; Chapleo, Christopher PhD

Journal of Addiction Medicine: June 2012 - Volume 6 - Issue 2 - p 118–123
doi: 10.1097/ADM.0b013e31824fceca
Original Research

Objectives: Opioids are the most effective pain medication available, yet concerns about their safety may limit their administration to those in need. In efforts to identify analgesics with lower potential for abuse and dependence, recent evidence suggests that combinations of opioids with ultra-low doses of the opioid antagonist naloxone may enhance the analgesic effect with increased safety. This study investigated the use of buprenorphine (0.3 mg) plus ultra-low-dose naloxone (0.02 mg) (BUP + ULDN) as compared with buprenorphine alone (0.3 mg) (BUP) for the treatment of pain.

Methods: In a double-blind, placebo-controlled, randomized cross-over design, 12 study participants with lingering, noncancer pain received each medication intravenously for 5 days of dosing, separated by an intertrial interval of at least 7 days to avoid possible carryover effects.

Results: We found no order effects and no differences between medications in pre- to postdose pain ratings, side effects, or adverse events.

Conclusions: These findings suggest that BUP + ULDN is not more effective in reducing pain than BUP.

From the Integrated Substance Abuse Programs (WL, MH, JJ, KM, MT), University of California, Los Angeles; and Reckitt Benckiser Healthcare (UK) Limited (CC), Hull, United Kingdom.

Send correspondence and reprint requests to Maureen Hillhouse, PhD, Integrated Substance Abuse Programs, University of California, Los Angeles, 1640 S. Sepulveda, Ste 120, Los Angeles, CA 90025. E-mail:

This research was funded by Reckitt Benckiser Healthcare (UK) Limited (Hull, GB), as an investigator-initiated study and as such did not play any role in the design or implementation of this study.

The authors report no conflict of interest with the exception that Christopher Chapleo is employed by Reckitt Benckiser Healthcare (UK) Limited.

Received June 08, 2011

Accepted June 10, 2012

© 2012 American Society of Addiction Medicine