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Handbook of Methadone Prescribing and Buprenorphine Therapy pp 59–72Cite as

Methadone Pharmacodynamics and Pharmacokinetics

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Abstract

Methadone (6-dimethylamino-4, 4-diphenyl-3-heptanone) was first synthesized in 1937 by Bockmühl and Ehrhart as part of a larger pharmaceutical program synthesizing atropine derivatives as spasmolytics [1]. This program led to the development in 1939 of meperidine, which not only had spasmolytic properties but also acted as an analgesic. Subsequent testing of methadone found that it had a 5–10-fold greater analgesic effect than meperidine but its further development was limited by wartime supply shortages and potential adverse effects, such as nausea, experienced in a small group of human subjects [1, 2].

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Acknowledgment

Dr. Gavin Bart (K23 DA024663) and Dr. Sharon Walsh (R01 DA016718) would like to kindly acknowledge the support of the National Institute on Drug Abuse in preparing this chapter.

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Authors and Affiliations

  1. Department of Medicine, Hennepin County Medical Center, 701 Park Avenue, Mail Code G5, Minneapolis, MN, 55415, USA

    Gavin Bart MD

  2. Department of Behavioral Science, Center on Drug and Alcohol Research, University of Kentucky, 515 Oldham Court, Lexington, KY, 40502, USA

    Sharon L. Walsh PhD

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  1. Gavin Bart MD
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  2. Sharon L. Walsh PhD
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Correspondence to Sharon L. Walsh PhD .

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Editors and Affiliations

  1. , Dept of Pain Med and Palliative Care, Beth Israel Medical Center, Union Square East 10, New York, 10003, New York, USA

    Ricardo A. Cruciani

  2. , Dept of Pain Mgmt and Palliative Care, Beth Israel Medical Center, East 17th Street 350, New York, 10003, New York, USA

    Helena Knotkova

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Bart, G., Walsh, S.L. (2013). Methadone Pharmacodynamics and Pharmacokinetics. In: Cruciani, R., Knotkova, H. (eds) Handbook of Methadone Prescribing and Buprenorphine Therapy. Springer, New York, NY. https://doi.org/10.1007/978-1-4614-6974-2_6

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  • DOI: https://doi.org/10.1007/978-1-4614-6974-2_6

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