Abstract
BackgroundPrescribed sublingual (SL) buprenorphine is sometimes diverted for intravenous (IV) abuse, but no human pharmacokinetic data are available following high-dose IV buprenorphine. MethodsPlasma was collected for 72h after administration of placebo or 2, 4, 8, 12, or 16mg IV buprenorphine in escalating order (single-blind, double-dummy) in 5 healthy male non-dependent opioid users. Buprenorphine and its primary active metabolite, norbuprenorphine, were quantified by liquid chromatography–tandem mass spectrometry with limits of quantitation of 0.1μg/L. ResultsMaximum buprenorphine concentrations (mean±SE) were detected 10min after 2, 4, 8, 12, 16mg IV: 19.3±1.0, 44.5±4.8, 85.2±7.7, 124.6±16.6, and 137.7±18.8μg/L, respectively. Maximum norbuprenorphine concentrations occurred 10–15min (3.7±0.7μg/L) after 16mg IV administration. ConclusionsBuprenorphine concentrations increased in a significantly linear dose-dependent manner up to 12mg IV buprenorphine. Thus, previously demonstrated pharmacodynamic ceiling effects (over 2–16mg) are not due to pharmacokinetic adaptations within this range, although they may play a role at doses higher than 12mg.
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