Rutgers, The State University of New Jersey, Department of Animal Sciences and Graduate Program in Endocrinology and Animal, Biosciences , 84 Lipman Drive, New Brunswick, NJ 08901 , USA +1 848 932 2966 ; +1 732 932 6996 ;
Expert Opin Drug Saf. 2014 Jun;13(6):831-41. doi: 10.1517/14740338.2014.909405. Epub 2014 Apr 28.
Obesity is a known health risk for the development of several preventable diseases. Obesity-related metabolic alterations negatively impact different physiological mechanisms, which supports the rationale for the use of combined drug therapy. Naltrexone is an opioid antagonist for the treatment of opioid and alcohol dependency, whereas bupropion is a norepinephrine/dopamine reuptake inhibitor used to treat depression and smoking cessation. Although not effective as individual monotherapies for obesity, naltrexone and bupropion in combination produce weight loss and a metabolic profile beneficial for the potential treatment of obesity.
This review examines the safety and antiobesity effects of naltrexone and bupropion alone and in combination. It reviews the results of four Phase III clinical trials of a novel fixed dose of sustained-released naltrexone/bupropion.
Naltrexone/bupropion has a greater weight loss efficacy than two FDA-approved medications, orlistat and lorcaserin. Although the weight loss produced by phentermine/topiramate is superior to naltrexone/bupropion, the safety profile of naltrexone/bupropion has less severe adverse effects. In addition, naltrexone/bupropion is well tolerated, with nausea being the most reported adverse event. Unlike other centrally acting medications, lorcaserin and phentermine/topiramate, naltrexone/bupropion has no abuse potential.
肥胖是已知的健康风险，可导致多种可预防疾病的发生。肥胖相关的代谢改变会对不同的生理机制产生负面影响，这为联合药物治疗提供了依据。纳曲酮是一种阿片类拮抗剂，用于治疗阿片类药物和酒精依赖；而安非他酮是一种去甲肾上腺素/多巴胺再摄取抑制剂，用于治疗抑郁症和戒烟。虽然纳曲酮和安非他酮作为单独的疗法对肥胖症无效，但联合使用这两种药物可减轻体重并改善代谢状况，有希望用于肥胖症的治疗。
本文回顾了纳曲酮和安非他酮单独使用和联合使用的安全性和抗肥胖效果。本文还回顾了四项新型缓释纳曲酮/安非他酮固定剂量的 III 期临床试验结果。
纳曲酮/安非他酮比两种获得 FDA 批准的药物（奥利司他和lorcaserin）具有更强的减重效果。虽然苯丁胺/托吡酯产生的减重效果优于纳曲酮/安非他酮，但纳曲酮/安非他酮的安全性更优，不良反应更轻微。此外，纳曲酮/安非他酮具有良好的耐受性，最常见的不良反应是恶心。与其他中枢作用药物（lorcaserin 和 phentermine/topiramate）不同，纳曲酮/安非他酮没有滥用潜力。
