“I’ll Be Back”: The Resurrection of Dezocine

Abstract

Beginning with opium itself, natural and synthetic opioids have been used as analgesics for over 8000 years and were likely abused as drugs of recreation for that long as well. However, the “opioid crisis” resulted in attempts to avoid or limit opioid analgesics in favor of other therapies and methods. Mu opioid agonists can be effective analgesics but suffer from addiction, tolerance, and dangerous, sometimes fatal, side effects. One exception to this generalization is dezocine (Dalgan), a mixed mu/kappa opioid partial agonist. Dezocine is at least as effective as morphine in reducing acute pain in animal models and clinical applications such as postoperative pain. And while dezocine was discontinued in western markets in 2011, it has become the favored opioid analgesic in China, capturing over 40% of the market. Additionally, dezocine possesses norepinephrine uptake inhibitory activity, which may synergize with mu agonism in the case of acute pain treatment and possibly endow the drug with antinociceptive activity in neuropathic pain conditions. This Innovations article summarizes the history and properties of dezocine and presents evidence and rationale for why dezocine has undergone a resurrection.

Effects of Dezocine and Sufentanil on Th1/Th2 Balance in Breast Cancer Patients Undergoing Surgery

“… 48 , 55 Second, studies have shown that tramadol, as a weak agonist of μ receptors, can reduce the differentiation of Th cells into Th2 types. 52–54 Dezocine, with similar pharmacological characteristics to tramadol, such as partial activation on μ receptors and inhibiting noradrenaline and serotonin reuptake 17 , 32 , 33 may have an immune-stimulating effect. Previous studies have confirmed that serotonin (5-HT) may mediate the Th1 transition.…”

“…18,19 Opioids such as morphine, fentanyl, sufentanil and dezocine were usually used for anesthesia induction and postoperative analgesia in clinical practice. 16,17,20 However, clinical studies on opioids usually involve with one opioid such as fentanyl or sufentanil for anesthesia induction and other opioids such as morphine or dezocine for postoperative analgesia 16,17,20 .…”

“…30,31 Dezocine is widely used in perioperative anesthesia and postoperative analgesia in China due to its effective analgesic efficacy and fewer adverse events. 16,17 Dezocine is a partial μ receptor agonist and partial κ receptor agonist, which can inhibit the uptake of serotonin and epinephrine, similar to tramadol, and may have a similar…”

“…Dezocine is widely used in perioperative anesthesia and postoperative analgesia in China due to its effective analgesic efficacy and fewer adverse events. 16 , 17 Dezocine is a partial μ receptor agonist and partial κ receptor agonist, which can inhibit the uptake of serotonin and epinephrine, similar to tramadol, and may have a similar protective effect on immunity. 32 , 33 Studies have found that dezocine can up-regulate the level of IL-12 and down-regulate the level of IL-10 in human umbilical cord blood dendritic cells, 34 improve the proliferation and cytotoxicity of CD8 + cells, promote the maturation of BMDC, and inhibit tumor metastasis in rats.…”

Dezocine Has the Potential to Regulate the Clinical and Biological Features of Tumors

“… 39 Novel opioids, represented by dezocine, with specific pharmacological mechanisms have initially demonstrated their potential for better analgesia, immune protection, antitumor proliferation, antitumor migration, vascular growth suppression and antidepressants in cancer. 40 …”