Intravenous buprenorphine and norbuprenorphine pharmacokinetics in humans

M. A. Huestis, E. J. Cone, S. O. Pirnay, A. Umbricht, K. L. Preston

Research output: Contribution to journalArticlepeer-review

27 Scopus citations


Background: Prescribed sublingual (SL) buprenorphine is sometimes diverted for intravenous (IV) abuse, but no human pharmacokinetic data are available following high-dose IV buprenorphine. Methods: Plasma was collected for 72. h after administration of placebo or 2, 4, 8, 12, or 16. mg 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 0.1 μg/L. Results: Maximum buprenorphine concentrations (mean ± SE) were detected 10. min after 2, 4, 8, 12, 16 mg IV: 19.3 ± 1.0, 44.5 ± 4.8, 85.2 ± 7.7, 124.6 ± 16.6, and 137.7 ± 18.8 μg/L, respectively. Maximum norbuprenorphine concentrations occurred 10-15. min (3.7 ± 0.7 μg/L) after 16. mg IV administration. Conclusions: Buprenorphine concentrations increased in a significantly linear dose-dependent manner up to 12. mg IV buprenorphine. Thus, previously demonstrated pharmacodynamic ceiling effects (over 2-16. mg) are not due to pharmacokinetic adaptations within this range, although they may play a role at doses higher than 12 mg.

Original languageEnglish (US)
Pages (from-to)258-262
Number of pages5
JournalDrug and alcohol dependence
Issue number3
StatePublished - Aug 1 2013
Externally publishedYes


  • Buprenorphine
  • Intravenous
  • Norbuprenorphine
  • Pharmacokinetics

ASJC Scopus subject areas

  • Toxicology
  • Pharmacology
  • Psychiatry and Mental health
  • Pharmacology (medical)


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