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Webster LR, Smith MD, Unal C, et al. Low-dose naloxone provides an abuse-deterrent effect to buprenorphine. J Pain Res. 2015;8:791-8doi: 10.2147/JPR.S90780.
Webster, L. R., Smith, M. D., Unal, C., & Finn, A. (2015). Low-dose naloxone provides an abuse-deterrent effect to buprenorphine. Journal of pain research, 8791-8. https://doi.org/10.2147/JPR.S90780
Webster, Lynn R, et al. "Low-dose naloxone provides an abuse-deterrent effect to buprenorphine." Journal of pain research vol. 8 (2015): 791-8. doi: https://doi.org/10.2147/JPR.S90780
Webster LR, Smith MD, Unal C, Finn A. Low-dose naloxone provides an abuse-deterrent effect to buprenorphine. J Pain Res. 2015 Nov 04;8:791-8. doi: 10.2147/JPR.S90780. eCollection 2015. PMID: 26604818; PMCID: PMC4639562.
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J Pain Res. 2015 Nov 04;8:791-8. doi: 10.2147/JPR.S90780. eCollection 2015.

Low-dose naloxone provides an abuse-deterrent effect to buprenorphine.

Journal of pain research

Lynn R Webster, Michael D Smith, Cemal Unal, Andrew Finn

Affiliations

  1. PRA Health Sciences, Salt Lake City, UT, USA.
  2. Biometrical Solutions LLC, Raleigh, NC, USA.
  3. BioDelivery Sciences International, Inc., Raleigh, NC, USA.

PMID: 26604818 PMCID: PMC4639562 DOI: 10.2147/JPR.S90780

Abstract

In developmental research, plasma buprenorphine concentrations comparable to a 2 mg buprenorphine-naloxone (BN) sublingual tablet have been achieved with a 0.75 mg dose of BN buccal film, a small, bioerodible polymer film for application to mucosal membranes. This was a randomized, double-blind, placebo-controlled, single-dose, four-period crossover study in opioid-dependent subjects with chronic pain receiving >100 mg oral morphine equivalents daily who experienced withdrawal following a naloxone challenge dose. The objective of the study was to determine if intravenous (IV) naloxone doses of 0.1 and 0.2 mg would produce a withdrawal response when coadministered with a 0.75 mg IV dose of buprenorphine. Fifteen subjects receiving 90-1,260 mg oral morphine equivalents per day enrolled and completed the study. Precipitated withdrawal occurred in 13% (2/15) of placebo-treated subjects and 47% (7/15) of buprenorphine-treated subjects. When combined with the 0.75 mg dose of buprenorphine, a 0.1 mg dose of naloxone increased the incidence of precipitated withdrawal to 60%, and a 0.2 mg dose of naloxone increased the incidence to 73%. By 15 minutes postdose, the mean change in Clinical Opioid Withdrawal Scale (COWS) score from predose was 3.0 for placebo, 6.9 for buprenorphine, 9.8 for BN 0.1 mg, and 12.4 for BN 0.2 mg. The mean COWS score with each active treatment was significantly greater than placebo (P<0.001), and the mean COWS score for each of the naloxone-containing treatments was significantly greater than for buprenorphine alone (P<0.001). Naloxone doses as low as 0.1 mg added an abuse-deterrent effect to a 0.75 mg IV dose of buprenorphine.

Keywords: abuse-deterrent; buprenorphine; intravenous; nalox-one; opioid dependence; withdrawal symptoms

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