Drug safety evaluation of naltrexone/bupropion for the treatment of obesity.
BACKGROUND
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.


METHODS
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.


CONCLUSIONS
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.
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 ; ntbello@aesop.rutgers.edu.
Jessica L
JL
Verpeut
Nicholas T
NT
Bello
D000818:Animals; D019440:Anti-Obesity Agents / Q000009:adverse effects* / Q000627:therapeutic use; D016642:Bupropion / Q000009:adverse effects* / Q000627:therapeutic use; D003692:Delayed-Action Preparations; D004338:Drug Combinations; D006801:Humans; D009271:Naltrexone / Q000009:adverse effects* / Q000627:therapeutic use; D009765:Obesity / Q000188:drug therapy*; D015431:Weight Loss / Q000187:drug effects
D019440:Anti-Obesity Agents; D003692:Delayed-Action Preparations; D004338:Drug Combinations; C000591595:bupropion hydrochloride, naltrexone hydrochoride drug combination; D016642:Bupropion; D009271:Naltrexone
Belviq; Contrave; Qsymia; Xenical; arcuate nucleus; cardiovascular; β-endorphin