Review Article

Dezocine as a potent analgesic: overview of its pharmacological characterization

Rong-Rong Ye1,2, Shuang Jiang2,3, Xu Xu1, Yan Lu1, Yu-Jun Wang2, Jing-Gen Liu2
1 School of Chemical and Environmental Engineering, Shanghai Institute of Technology, Shanghai 201418, China
2 CAS Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China
3 School of Chinese Materia Medica, Nanjing University of Chinese Medicine, Nanjing 210023, China
Correspondence to: Yan Lu: luuyann@sit.edu.cn, Yu-Jun Wang: yjwang@simm.ac.cn,
DOI: 10.1038/s41401-021-00790-6
Received: 5 March 2021
Accepted: 4 October 2021
Advance online: 4 November 2021

Abstract

Dezocine, a synthetic opioid, introduced in 1970s as an analgesic, was redeveloped for relieving moderate to severe pain by Yangtze River Pharmaceutical Group in China in 2009. To date, dezocine occupies 45% of China’s opioid analgesic market. Along with dezocine being a dominated painkiller, a certain amount of research was conducted to elucidate dezocine’s action. In this review we summarize the current knowledge on the receptor, preclinical and clinical pharmacology of dezocine. Briefly, preclinical data show that dezocine is effective under varying pain conditions, particularly chronic neuropathic pain and cancer pain, through activation of opioid receptors, and inhibition of norepinephrine reuptake. Clinical data establish the effectiveness of dezocine either as a primary analgesic for postoperative pain management or a supplement for balanced analgesia. The receptor profile of dezocine is different from known pure μ agonists, and allows it to be used in combination with other opioids for additivity in efficacy or lower incidence of adverse effects.
Keywords: dezocine; opioid receptors; norepinephrine; serotonin transporter; postoperative pain; anesthesia

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