School of Chemical and Environmental Engineering, Shanghai Institute of Technology, Shanghai, 201418, China.
CAS Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, China.
Acta Pharmacol Sin. 2022 Jul;43(7):1646-1657. doi: 10.1038/s41401-021-00790-6. Epub 2021 Nov 4.
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.
地佐辛，一种合成阿片类药物，于 20 世纪 70 年代作为一种镇痛药推出，由中国扬子江药业集团于 2009 年重新开发用于缓解中重度疼痛。迄今为止，地佐辛占据了中国阿片类镇痛药市场的 45%。随着地佐辛成为一种主要的止痛药，人们进行了一定数量的研究来阐明地佐辛的作用。在这篇综述中，我们总结了地佐辛的受体、临床前和临床药理学的最新知识。简而言之，临床前数据表明，地佐辛通过激活阿片受体和抑制去甲肾上腺素再摄取，在各种疼痛情况下都有效，特别是慢性神经病理性疼痛和癌症疼痛。临床数据证实了地佐辛作为术后疼痛管理的主要镇痛药或平衡镇痛的补充剂的有效性。地佐辛的受体谱与已知的纯 μ 激动剂不同，使其可以与其他阿片类药物联合使用，以提高疗效或降低不良反应发生率。
