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Foreseeable Advantages and Limits of Buprenorphine-Naloxone Association

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Book cover Buprenorphine Therapy of Opiate Addiction

Abstract

Drug addiction is a chronic, relapsing disease that results from the prolonged effects of drugs on the brain. Opioid dependence is a worldwide problem. In opioid-dependent humans, buprenorphine is an effective treatment alternative to methadone (1,2) and levomethadyl acetate hydrochloride (3).The pharmacological profile of buprenorphine results in greater safety, less physical dependence, and greater flexibility in dose scheduling. However, abuse of buprenorphine has been reported in many countries where it is available as an analgesic (4) and in France (5), where it is available as an opiate-analgesic for drug substitution and maintenance. Despite the partial agonist activity of buprenorphine at µ opioid receptors and its “ceiling effect”, some cases of respiratory depression and fatalities have been reported, especially in cases of high doses of intravenously injected buprenorphine. The buprenorphine/naloxone (BupNx) combination tablet capitalizes on the differential absorption of naloxone by the sublingual (sl) vs parenteral routes: naloxone has a poor sl absorption. BupNx combination has been investigated with the goal of decreasing abuse, misuse, and diversion of buprenorphine. The BupNx combination product may be interesting for use in primary care office-based settings as a safe and an effective treatment that is likely to increase the availability of agonist treatment for opioid dependence. Availability of buprenorphine and BupNx tablets in United States has been slowed by the desire to provide them outside the traditional, highly regulated methadone clinic system. The Controlled Substances Act was amended in October 2000 and allows office-based prescribing of schedule III, IV, and V medications (and combination of medications) approved for opioid dependence and detoxification.

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© 2002 Humana Press Inc., Totowa, NJ

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Mallaret, M., Dematteis, M., Villier, C., Barjhoux, C.E., Gatignol, C. (2002). Foreseeable Advantages and Limits of Buprenorphine-Naloxone Association. 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_4

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  • DOI: https://doi.org/10.1007/978-1-59259-282-1_4

  • Publisher Name: Humana Press, Totowa, NJ

  • Print ISBN: 978-1-4684-9713-7

  • Online ISBN: 978-1-59259-282-1

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