Skip to main content
SpringerLink
Log in
Book cover

Buprenorphine Therapy of Opiate Addiction pp 1–11Cite as

Pharmacology of High-Dose Buprenorphine

  • Chapter

  • 125 Accesses

Part of the book series: Forensic Science and Medicine ((FSM))

Abstract

Buprenorphine is a semisynthetic opioid derived from thebaine, an alcaloid of the poppy Papaver somniferum. Alan Cowan and John Lewis first synthesized buprenorphine in the United States in 1973 and also described its main properties, including its potential efficacy as a substitution treatment for heroin (1).

This is a preview of subscription content, log in via an institution.

Chapter
USD   29.95
Price excludes VAT (USA)
  • Available as PDF
  • Read on any device
  • Instant download
  • Own it forever
eBook
USD   89.00
Price excludes VAT (USA)
  • Available as EPUB and PDF
  • Read on any device
  • Instant download
  • Own it forever
Softcover Book
USD   119.99
Price excludes VAT (USA)
  • Compact, lightweight edition
  • Dispatched in 3 to 5 business days
  • Free shipping worldwide - see info
Hardcover Book
USD   169.99
Price excludes VAT (USA)
  • Durable hardcover edition
  • Dispatched in 3 to 5 business days
  • Free shipping worldwide - see info

Tax calculation will be finalised at checkout

Purchases are for personal use only

Learn about institutional subscriptions

Preview

Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.

References

  1. Cowan A, Lewis JW, Macfarlane IR. Agonist and antagonist properties of buprenorphine, a new antinociceptive agent. Br J Pharmacol 1977; 60: 537–45.

    PubMed  CAS  Google Scholar 

  2. Stinchcomb AL, Paliwal A, Dua R, Imoto H, Woodard RW, Flynn GL. Permeation of buprenorphine and its 3—alkyl-ester prodrugs through human skin. Pharm Res 1996; 13: 1519–23.

    Article  PubMed  CAS  Google Scholar 

  3. Kuhlman JJ Jr, Lalani S, Magluilo J Jr, Levine B, Darwin WD. Human pharmacokinetics of intravenous, sublingual, and buccal buprenorphine. J Anal Toxicol 1996; 20: 369–78.

    PubMed  CAS  Google Scholar 

  4. Mendelson J, Upton RA, Everhart ET, Jacob P III, Jones RT. Bioavailability of sublingual buprenorphine. J Clin Pharmacol 1997; 37: 31–7.

    Article  PubMed  CAS  Google Scholar 

  5. Nath RP, Upton RA, Everhart ET, Cheung P, Shwonek P, Jones RT, Mendelson JE. Buprenorphine pharmacokinetics: relative bioavailability of sublingual tablet and liquid formulations. J Clin Pharmacol 1999; 39: 619–23.

    Article  PubMed  CAS  Google Scholar 

  6. Schuh KJ, Johanson CE. Pharmacokinetic comparison of the buprenorphine sublingual liquid and tablet. Drug Alcohol Depend 1999; 56: 55–60.

    Article  PubMed  CAS  Google Scholar 

  7. Linhardt K, Ravn C, Gizurarson S, Bechgaard E. Intranasal absorption of buprenorphine-in vivo bioavailability in sheep. Int J Pharm 2000; 205 (1–2): 159–63.

    Article  Google Scholar 

  8. Mandai TK. Development of biodegradable drug delivery system to treat addiction. Drug Dev Ind Pharm 1999; 25 (6): 773–9.

    Article  Google Scholar 

  9. Ohtani M, Kotaki H, Nishitateno K, Sawada Y, Iga T. Kinetics of respiratory depression in rats induced by buprenorphine and its metabolite, norbuprenorphine. J Pharmacol Exp Ther 1997; 281: 428–33.

    PubMed  CAS  Google Scholar 

  10. Gaulier TM, Marquet P, Lacassie E, Dupuy JL, Lachatre G. Fatal intoxication following self-administration of a massive dose of buprenorphine. J Forensic Sci 2000; 45: 226–8.

    PubMed  CAS  Google Scholar 

  11. Wilkins DG, Rollins DE, Valdez AS, Mizuno A, Krueger GG, Cone EJ. A retrospective study of buprenorphine and norbuprenorphine in human hair after multiple doses. J Anal Toxicol 1999; 23 (6); 409–5.

    PubMed  CAS  Google Scholar 

  12. Vincent F, Bessard J, Vacheron J, Mallaret M, Bessard G. Determination of buprenorphine and norbuprenorphine in urine and hair by gas chromatography-mass spectrometry. J Anal Toxicol 1999; 23 (4): 270–9.

    PubMed  CAS  Google Scholar 

  13. Cirimele V, Kintz P, Lohner S, Ludes B. Buprenorphine to norbuprenorphine ratio in human hair. J Anal Toxicol 2000; 24 (6): 448–9.

    PubMed  CAS  Google Scholar 

  14. Iribarne C, Picart D, Dreano Y, Bail JP, Berthou F. Involvement of cytochrome P450 3A4 in N-dealkylation of buprenorphine in human liver microsomes. Life Sci 1997; 60: 1953–64.

    Article  PubMed  CAS  Google Scholar 

  15. Ibrahim RB, Wilson JG, Thorsby ME, Edwards DJ. Effect of buprenorphine on CYP3A activity in rat and human liver microsomes. Life Sci 2000; 66: 1293–8.

    Article  PubMed  CAS  Google Scholar 

  16. Kilicarslan T, Sellers EM. Lack of interaction of buprenorphine with flunitrazepam metabolism. Am J Psychiatry 2000; 157: 1164–6.

    Article  PubMed  CAS  Google Scholar 

  17. Tracqui A, Kintz P, Ludes B. Buprenorphine-related deaths among drug addicts in France: a report on 20 fatalities. J Anal Toxicol 1998; 22 (6): 430–4.

    PubMed  CAS  Google Scholar 

  18. Kintz P. Deaths involving buprenorphine: a compendium of French cases. Forensic Sci Int 2001; 121: 65–9.

    Article  PubMed  CAS  Google Scholar 

  19. Ohtani M, Kotaki H, Uchino K, Sawada Y, Iga T. Pharmacokinetic analysis of enterohepatic circulation of buprenorphine and its active metabolite, norbuprenorphine, in rats. Drug Metab Dispos 1994; 22 (1): 2–7.

    PubMed  CAS  Google Scholar 

  20. Chawarski MC, Schottenfeld RS, O’Connor PG, Pakes J. Plasma concentrations of buprenorphine 24 to 72 hours after dosing. Drug Alcohol Depend 1999; 55 (1–2): 157–163.

    Article  PubMed  CAS  Google Scholar 

  21. Walsh SL, Preston KL, Stitzer ML, Cone EJ, Bigelow GE. Clinical pharmacology of buprenorphine: ceiling effects at high doses. Clin Pharmacol Ther 1994; 55: 569–80.

    Article  PubMed  CAS  Google Scholar 

  22. Walker EA, Zernig G, Young AM. In vivo apparent affinity and efficacy estimates for mu opiates in a rat tail-withdrawal assay. Psychopharmacology (Berl) 1998; 136 (1): 15–23.

    Article  CAS  Google Scholar 

  23. Ohtani M, Kotaki H, Sawada Y, Iga T. Comparative analysis of buprenorphine-and norbuprenorphine-induced analgesic effects based on pharmacokinetic-pharmacodynamic modeling. J Pharmacol Exp Ther 1995; 272: 505–10.

    PubMed  CAS  Google Scholar 

  24. Rang HP, Dale MM, Ritter JM. Pharmacology, 4th ed., Churchill Livingstone, Edinburgh, UK; 1999.

    Google Scholar 

  25. Ohta S, Niwa M, Nozaki M, Hattori M, Shimonaka H, Dohi S. The mu, delta and kappa properties of various opioids. Masui 1995; 44 (9): 1228–32.

    PubMed  CAS  Google Scholar 

  26. Pick CG, Peter Y, Schreiber S, Weizman R. Pharmacological characterization of buprenorphine, a mixed agonist-antagonist with kappa 3 analgesia. Brain Res 1997; 744: 41–6.

    Article  PubMed  CAS  Google Scholar 

  27. Huang P, Kehner GB, Cowan A, Liu-Chen LY. Comparison of pharmacological activities of buprenorphine and norbuprenorphine: norbuprenorphine is a potent opioid agonist. J Pharmacol Exp Ther 2001; 297: 688–95.

    PubMed  CAS  Google Scholar 

  28. Belcheva MM, Ho MT, Igantova EG, Jefcoat LB, Barg J, Vogel Z, McHale RJ, Johnson FE, Coscia CJ. Buprenorphine differentially alters opioid receptor adaptation in rat brain regions. J Pharmacol Exp Ther 1996; 277: 1322–7.

    PubMed  CAS  Google Scholar 

  29. Yu Y, Zhang L, Yi X, Sun H, Uhl GR, Wang JB. Mu opioid receptor phosphorylation, desensitization and ligand efficacy. J Biol Chem 1997; 272: 28, 869–74.

    Google Scholar 

  30. Sharma SK, Nirenberg M, Klee WA. Morphine receptors as regulators of adenylate cyclase activity. Proc Natl Acad Sci USA 1975; 72 (2): 590–4.

    Article  PubMed  CAS  Google Scholar 

  31. Blake AD, Bot G, Freeman JC, Reisine T. Differential opioid agonist regulation of the mouse opioid receptor. JBC 1997; 272 (2): 782–90.

    Article  CAS  Google Scholar 

  32. Petry NM, Bickel WK, Badger GJ. A comparison of four buprenophine dosing regimens in the treatment of opioid dependence. Clin Pharmacol Ther 1999; 66: 306–14.

    Article  PubMed  CAS  Google Scholar 

  33. Vignau J. Preliminary assessment of a 10–day rapid detoxification programme using high dosage buprenorphine. Eur Addict Res 1998;4 Suppl 1: 29–31.

    Google Scholar 

  34. Gowing L, Ali R, White J. Buprenorphine for the management of opioid withdrawal. Cochrane Database Syst Rev 2000;3:CD002025.

    Google Scholar 

  35. Pratiques en évolution: bonnes pratiques de prise en charge des pharmacodépendances majeures aux opiacés. Ed. Schering-Plough, Levallois Perret;1999.

    Google Scholar 

Download references

Authors
  1. Pierre Marquet
    View author publications

    You can also search for this author in PubMed Google Scholar

Editor information

Editors and Affiliations

  1. Institute of Legal Medicine, Strasbourg, France

    Pascal Kintz PharmD, PhD (President) (President)

  2. Societé Française de Toxicologie Analytique, France

    Pascal Kintz PharmD, PhD (President) (President)

  3. Department of Pharmacology and Toxicology, University Hospital, France

    Pierre Marquet MD, PhD (Professor of Pharmacology) (Professor of Pharmacology)

  4. Faculty of Medicine, Limoges University, Limoges, France

    Pierre Marquet MD, PhD (Professor of Pharmacology) (Professor of Pharmacology)

Rights and permissions

Reprints and permissions

Copyright information

© 2002 Humana Press Inc., Totowa, NJ

About this chapter

Cite this chapter

Marquet, P. (2002). Pharmacology of High-Dose Buprenorphine. In: Kintz, P., Marquet, P. (eds) Buprenorphine Therapy of Opiate Addiction. Forensic Science and Medicine. Humana Press, Totowa, NJ. https://doi.org/10.1007/978-1-59259-282-1_1

Download citation

  • DOI: https://doi.org/10.1007/978-1-59259-282-1_1

  • Publisher Name: Humana Press, Totowa, NJ

  • Print ISBN: 978-1-4684-9713-7

  • Online ISBN: 978-1-59259-282-1

  • eBook Packages: Springer Book Archive

Publish with us

Policies and ethics

Search

Navigation