Revisiting dezocine for opioid use disorder: A narrative review of its potential abuse liability

• Published in: CNS neuroscience & therapeutics 2024-09, Vol.30 (9), p.e70034-n/a
• Main Authors: Barr, Gordon A., Schmidt, Heath D., Thakrar, Ashish P., Kranzler, Henry R., Liu, Renyu
• Format: Article
• Language: English
• Subjects: Addictions; Analgesics; Analgesics, Opioid - therapeutic use; Animals; Antidepressants; biased mu‐opioid ligand; Binding sites; Bridged Bicyclo Compounds, Heterocyclic - therapeutic use; Case reports; dependence; dezocine; Drug abuse; Drug addiction; drug discrimination; Drug overdose; drug self‐administration; Drug use; FDA approval; Federal regulation; Fentanyl; Humans; Methadone; Morphine; Mortality; Narcotics; opioid use disorder; Opioid-Related Disorders - prevention & control; Opioids; Overdose; Patients; Proteins; Public health; Review; Substance abuse treatment; Substance use disorder; Tetrahydronaphthalenes - therapeutic use
• ISSN: 1755-5930; 1755-5949; 1755-5949
• DOI: 10.1111/cns.70034

Aims Opioid use disorder (OUD) remains a serious public health problem. Opioid maintenance treatment is effective but under‐utilized, hard to access under existing federal regulations, and, once patients achieve OUD stability, challenging to discontinue. Fewer than 2% of persons with OUD stop using opioids completely. There have been calls from public advocacy groups, governmental agencies, and public health officials for new treatments for OUD. Dezocine, a non‐scheduled opioid previously used in the United States and currently widely prescribed in China for pain management, could be a candidate for a novel OUD treatment medication in the U.S. Nonetheless, to date, there have been no reviews of the clinical and preclinical literature detailing dezocine's abuse potential, a key consideration in assessing its clinical utility. Discussion There are no English language reports of human abuse, dependence, or overdose of dezocine, despite years of extensive clinical use. There are a few case reports of dezocine abuse in the Chinese literature, but there are no reports of overdose deaths. Dezocine is perceived as an opioid and is “liked” by opioid‐experienced human and non‐human primates, properties that are not dose‐dependent and are mitigated by ceiling effects—higher doses do not result in more “liking.” There is little withdrawal, spontaneous or precipitated, in humans, monkeys, rats, or mice treated chronically with dezocine alone. However, at some doses, dezocine can precipitate withdrawal in humans and monkeys dependent on other opioids. In rodents, dezocine reduces the severity of morphine withdrawal and the rewarding properties of other opioids. Conclusions Although dezocine is reinforcing in humans and monkeys with prior or concurrent opioid use within a restricted dose range, there are only a few anecdotal reports of dezocine abuse despite of the long history of use in humans. Given the evidence of dezocine's limited abuse potential, it could be useful both as a treatment for OUD. However, in‐depth studies would be required for dezocine to be re‐considered for clinical use. Dezocine is a partial MOR agonist previously used clinically in the USA and currently in China. It has been proposed that dezocine be reintroduced to clinical use in the USA, as an analgesia and/or an additional tool to treat opioid use disorder. To consider the clinical reintroduction of dezocine knowing its abuse liability is important. In this review, we found no reports of abuse