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Milella2023_Heroin and its metabolites- relevance to heroin use disorder.pdf (1.44 MB)

Heroin and its metabolites: relevance to heroin use disorder

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posted on 2023-06-10, 06:44 authored by Michele Stanislaw Milella, Ginevra D’Ottavio, Silvana De PirroSilvana De Pirro, Massimo Barra, Daniele Caprioli, Aldo Badiani
Heroin is an opioid agonist commonly abused for its rewarding effects. Since its synthesis at the end of the nineteenth century, its popularity as a recreational drug has ebbed and flowed. In the last three decades, heroin use has increased again, and yet the pharmacology of heroin is still poorly understood. After entering the body, heroin is rapidly deacetylated to 6-monoacetylmorphine (6-MAM), which is then deacetylated to morphine. Thus, drug addiction literature has long settled on the notion that heroin is little more than a pro-drug. In contrast to these former views, we will argue for a more complex interplay among heroin and its active metabolites: 6-MAM, morphine, and morphine-6-glucuronide (M6G). In particular, we propose that the complex temporal pattern of heroin effects results from the sequential, only partially overlapping, actions not only of 6-MAM, morphine, and M6G, but also of heroin per se, which, therefore, should not be seen as a mere brain-delivery system for its active metabolites. We will first review the literature concerning the pharmacokinetics and pharmacodynamics of heroin and its metabolites, then examine their neural and behavioral effects, and finally discuss the possible implications of these data for a better understanding of opioid reward and heroin addiction. By so doing we hope to highlight research topics to be investigated by future clinical and pre-clinical studies.

History

Publication status

  • Published

File Version

  • Published version

Journal

Translational Psychiatry

ISSN

2158-3188

Publisher

Springer Science and Business Media LLC

Volume

13

Page range

a120

Department affiliated with

  • Psychology Publications

Full text available

  • Yes

Peer reviewed?

  • Yes

Legacy Posted Date

2023-04-14

First Open Access (FOA) Date

2023-04-14

First Compliant Deposit (FCD) Date

2023-04-12

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