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Not everyone enjoys taking sublingual Suboxone. So some other forms should be coming out in the next 12-24 months—hopefully. One form is a long-term injection form or "depot" injection.
An injection depot formulation of buprenorphine: extended biodelivery and effects.
Aim
Buprenorphine is an effective medication for treatment of opioid dependence. An injectable depot formulation of buprenorphine has been developed using biodegradable polymer microcapsule technology. This formulation may offer effective treatment of opioid dependence and enhance treatment delivery while minimizing risks of patient non-adherence or illicit diversion of the medication. This report provides a characterization of the biodelivery of this injectable depot in humans and of the relationship of drug blood levels to pharmacodynamic indices.
Method and participants
The data are from two studies in which 11 opioid-dependent volunteers each received a single depot injection containing 58 mg of buprenorphine, and include previously unreported detailed plasma concentration data over a 6-week time-course following depot administration and examination of their relationship to pharmacodynamic indices.
Findings
Mean plasma buprenorphine increased gradually following depot administration, peaked at 2-3 days with a mean concentration of 1.25 ng/ml and then decreased gradually, approaching undetectable levels (< 0.10 ng/mL) by 6 weeks. There was substantial between-subject consistency in several aspects of buprenorphine biodelivery, including time to first detectable blood level (4 hours), peak blood level (2 days) and undetectable blood level (6-6.5 weeks). In contrast, there was marked between-subject variability in the magnitude of peak buprenorphine concentrations, ranging from 0.17 to 3.47 ng/ml. Extent of opioid blockade was tested by weekly opioid challenges with 3 mg subcutaneous hydromorphone; subjective response and pupillary constriction were related inversely to both buprenorphine and norbuprenorphine plasma concentrations (r = 0.84-0.95).
Conclusion
The data document that this depot formulation provides effective buprenorphine delivery for several weeks and that effects persist even at fairly low buprenorphine plasma concentrations. Suggestions are offered for further research needed to develop this formulation for clinical use as a detoxification and/or maintenance pharmacotherapy for opioid dependence.
Sigmon SC, Moody DE, Nuwayser ES, Bigelow GE. Addiction. 2006;101:420-32.
[Abstract underlines and separation of section for easier review by Dr. Schaller].
*Since we have found rare pateints are sensitive to Suboxone, we would hope anyone using a depot would try a small dose first.
*Also, while the blood level was measurable the first few weeks, it might be risking relapse to try to push depot dose frequency to a full six weeks.
