Abstract
Heroin is a growing national crisis in America. There is an increasing frequency of heroin overdoses. All of the currently used therapeutic approaches to treatment of heroin abuse and other opioid drugs of abuse focus on antagonizing a brain receptor (particularly µ-opiate receptors). However, it has been known that the therapeutic use of certain µ-opiate receptor antagonist may actually increase heroin overdose. Once overdosed, heroin addicts may continue to get overdosed again and again until fatal. Here we report our design and validation of a novel therapeutic strategy targeting heroin activation based on our analysis of the chemical transformation and functional change of heroin in the body. An effective blocker of heroin activation, such as ethopropazine tested in this study, may be used as a standalone therapy or in combination with a currently available, traditional medications targeting µ-opiate receptors (e.g. naltrexone or its extended-release formulation Vivitrol). The combination therapy would be ideal for heroin abuse treatment as the effects of two therapeutic agents targeting two independent mechanisms are cooperative.
Document Type
Article
Publication Date
11-13-2018
Digital Object Identifier (DOI)
https://doi.org/10.1038/s41598-018-35196-8
Funding Information
This work was supported in part by the National Institutes of Health (NIH grants UH2/UH3 DA041115, R01 DA035552, R01 DA032910, R01 DA013930, and R01 DA025100).
Repository Citation
Zhang, Ting; Zheng, Xirong; Kim, Kyungbo; Zheng, Fang; and Zhan, Chang-Guo, "Blocking Drug Activation as a Therapeutic Strategy to Attenuate Acute Toxicity and Physiological Effects of Heroin" (2018). Molecular Modeling and Biopharmaceutical Center Faculty Publications. 15.
https://uknowledge.uky.edu/mmbc_facpub/15
Included in
Chemicals and Drugs Commons, Pharmacy and Pharmaceutical Sciences Commons, Substance Abuse and Addiction Commons
Notes/Citation Information
Published in Scientific Reports, v. 8, 16762, p. 1-6.
© The Author(s) 2018
This article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made. The images or other third party material in this article are included in the article’s Creative Commons license, unless indicated otherwise in a credit line to the material. If material is not included in the article’s Creative Commons license and your intended use is not permitted by statutory regulation or exceeds the permitted use, you will need to obtain permission directly from the copyright holder. To view a copy of this license, visit http://creativecommons.org/licenses/by/4.0/.