Childers Wayne, Elokely Khaled, Abou-Gharbia Magid
Department of Pharmaceutical Sciences, School of Pharmacy, Temple University, Philadelphia, PA 19140, USA.
Department of Pharmaceutical Sciences, School of Pharmacy, College of Health Sciences, University of Wyoming, Laramie, WY 82071, USA.
Pharmaceuticals (Basel). 2025 Mar 8;18(3):386. doi: 10.3390/ph18030386.
The neurological effects of opium were first described over 8000 years ago. Morphine was isolated in 1803 and by the mid-1800s had become both a pain-relieving blessing and an addictive curse. As part of the crusade to identify safer and more reliable alternatives to morphine, dezocine (Dalgan) was marketed in the US in 1986. Its use was discontinued in the US in 2011 without revealing the reasons, but it remains one of the most widely used analgesic agents in China today. Dezocine's unique pharmacology makes it an effective analgesic with limited opioid-associated side effects and little or no reported potential for dependence and addiction. In addition, dezocine's blocking effect on serotonin and norepinephrine transporters recommends its further exploration as a potential treatment for various chronic and neuropathic pain conditions. Most recently, data suggest that dezocine might represent a viable treatment for addiction management. This report focuses on the data supporting dezocine's non-addictive profile and its potential use to treat opioid addiction and withdrawal, as well as recent efforts to generate formulations of dezocine that support sub-chronic and chronic dosing.
鸦片对神经系统的影响早在8000多年前就有记载。1803年吗啡被分离出来，到19世纪中叶，它既是缓解疼痛的福音，又是令人成瘾的祸根。作为寻找比吗啡更安全、更可靠替代品运动的一部分，地佐辛（达尔丰）于1986年在美国上市。2011年其在美国停止使用，原因未公开，但它仍是当今中国使用最广泛的镇痛药之一。地佐辛独特的药理学特性使其成为一种有效的镇痛药，与阿片类药物相关的副作用有限，且几乎没有或没有依赖性和成瘾的报道。此外，地佐辛对血清素和去甲肾上腺素转运体的阻断作用建议进一步探索其作为各种慢性和神经性疼痛疾病潜在治疗方法的可能性。最近，有数据表明地佐辛可能是一种可行的成瘾管理治疗方法。本报告重点关注支持地佐辛非成瘾特性的数据及其在治疗阿片类药物成瘾和戒断方面的潜在用途，以及最近为制备支持亚慢性和慢性给药的地佐辛制剂所做的努力。
