Low-dose naloxone provides an abuse-deterrent effect to buprenorphine
Low-dose naloxone provides an abuse-deterrent effect to buprenorphine
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Lynn R Webster,1 Michael D Smith,1 Cemal Unal,2 Andrew Finn3 1PRA Health Sciences, Salt Lake swish supreme glide track white City, UT, USA; 2Biometrical Solutions LLC, Raleigh, NC, USA; 3BioDelivery Sciences International, Inc., Raleigh, NC, USA 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 the gel bottle audrey 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: opioid dependence, withdrawal symptoms, abuse-deterrent, buprenorphine, naloxone, intravenous.