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  • Norbuprenorphine and respiratory depression: Exploratory analyses with new lyophilized buprenorphine and sublingual buprenorphine
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Norbuprenorphine and respiratory depression: Exploratory analyses with new lyophilized buprenorphine and sublingual buprenorphine
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International journal of clinical pharmacology and therapeutics (2017-12-13)
John Strang, Alastair Knight, Shelagh Baillie, Kylie Reed, Karolina Bogdanowicz, James Bell
PMID29231163
ABSTRACT

To investigate plasma levels of buprenorphine and norbuprenorphine and their relationship to respiratory depression. Opioid-dependent subjects were randomized 2 : 1 to novel lyophilized rapid-disintegrating tablet ("bup-lyo") or standard sublingual buprenorphine tablet ("bup-SL"). Measurements included oximetry scores and linked plasma buprenorphine and norbuprenorphine levels. Respiratory depression (cumulative duration of SpO<sub>2</sub> < 90% over 30-minute periods) increased with corresponding exposure levels (AUC<sub>30 min</sub>) of buprenorphine and particularly with norbuprenorphine. A lower buprenorphine/norbuprenorphine ratio was predictive of respiratory depression. The mean (SD) observed ratio was significantly higher for "bup-lyo" (3.4 (2.8)) compared to "bup-SL" (1.7 (0.77)), p < 0.0001. Exploratory investigation found respiratory depression more strongly associated with norbuprenorphine than with buprenorphine. This accords with animal studies.
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