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Hagelberg NM, Fihlman M, Hemmilä T, et al. Rifampicin decreases exposure to sublingual buprenorphine in healthy subjects. Pharmacol Res Perspect. 2016;4(6):e00271doi: 10.1002/prp2.271.
Hagelberg, N. M., Fihlman, M., Hemmilä, T., Backman, J. T., Laitila, J., Neuvonen, P. J., Laine, K., Olkkola, K. T., & Saari, T. I. (2016). Rifampicin decreases exposure to sublingual buprenorphine in healthy subjects. Pharmacology research & perspectives, 4(6), e00271. https://doi.org/10.1002/prp2.271
Hagelberg, Nora M, et al. "Rifampicin decreases exposure to sublingual buprenorphine in healthy subjects." Pharmacology research & perspectives vol. 4,6 (2016): e00271. doi: https://doi.org/10.1002/prp2.271
Hagelberg NM, Fihlman M, Hemmilä T, Backman JT, Laitila J, Neuvonen PJ, Laine K, Olkkola KT, Saari TI. Rifampicin decreases exposure to sublingual buprenorphine in healthy subjects. Pharmacol Res Perspect. 2016 Nov 03;4(6):e00271. doi: 10.1002/prp2.271. eCollection 2016 Dec. PMID: 28097004; PMCID: PMC5226287.
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Pharmacol Res Perspect. 2016 Nov 03;4(6):e00271. doi: 10.1002/prp2.271. eCollection 2016 Dec.

Rifampicin decreases exposure to sublingual buprenorphine in healthy subjects.

Pharmacology research & perspectives

Nora M Hagelberg, Mari Fihlman, Tuija Hemmilä, Janne T Backman, Jouko Laitila, Pertti J Neuvonen, Kari Laine, Klaus T Olkkola, Teijo I Saari

Affiliations

  1. Department of Anaesthesiology, Intensive Care and Pain Medicine University of Turku and Turku University Hospital Turku Finland.
  2. Department of Clinical Pharmacology University of Helsinki and Helsinki University Hospital Helsinki Finland.
  3. Department of Pharmacology Drug Development and Therapeutics University of Turku Turku Finland; Medbase Ltd Turku Finland.
  4. Department of Anaesthesiology, Intensive Care and Pain Medicine University of Helsinki and Helsinki University Hospital Helsinki Finland.

PMID: 28097004 PMCID: PMC5226287 DOI: 10.1002/prp2.271

Abstract

Buprenorphine is mainly metabolized by the cytochrome P450 (CYP) 3A4 enzyme. The aim of this study was to evaluate the role of first-pass metabolism in the interaction of rifampicin and analgesic doses of buprenorphine. A four-session paired cross-over study design was used. Twelve subjects ingested either 600 mg oral rifampicin or placebo once daily in a randomized order for 7 days. In the first part of the study, subjects were given 0.6-mg (placebo phase) or 0.8-mg (rifampicin phase) buprenorphine sublingually on day 7. In the second part of the study, subjects received 0.4-mg buprenorphine intravenously. Plasma concentrations of buprenorphine and urine concentrations of buprenorphine and its primary metabolite norbuprenorphine were measured over 18 h. Adverse effects were recorded. Rifampicin decreased the mean area under the dose-corrected plasma concentration-time curve (AUC

Keywords: Cytochrome (P450) 3A4; first‐pass metabolism; interaction; rifampicin; sublingual and intravenous buprenorphine

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