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Buprenorphine Therapy of Opiate Addiction pp 13–27Cite as

Controlled Drug Administration Studies of High-Dose Buprenorphine in Humans

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

Abstract

Buprenorphine was developed in the early 1970s by Reckitt and Colman Products (Hull, UK) as part of a wide-ranging search for an effective analgesic with lower abuse potential and reduced toxicity compared with morphine (1). Many of buprenorphine’s chemical and pharmacological properties, including ready diffusion of the highly lipophilic drug across the blood-brain barrier and its high binding avidity for opiate receptors, led to the selection of this thebaine derivative as the best analgesic compound for further drug development. Despite its high-affinity binding and high potency (25–40 times more potent than morphine), buprenorphine has a lower efficacy for pain relief and is classified as a partial agonist at µ opiate receptors. Buprenorphine dissociates slowly from receptors, resulting in a long duration of action and, potentially, a reduced potential for abuse. These properties led researchers at the United States Public Health Service’s Addiction Research Center to investigate buprenorphine further as a pharmacotherapy for opioid addiction (2).

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Authors
  1. Marilyn A. Huestis
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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)

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© 2002 Humana Press Inc., Totowa, NJ

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Huestis, M.A. (2002). Controlled Drug Administration Studies of High-Dose Buprenorphine in Humans. 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_2

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  • DOI: https://doi.org/10.1007/978-1-59259-282-1_2

  • 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

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