Combination therapy with naltrexone and bupropion for obesity

Expert Opin Pharmacother. 2011 Aug;12(11):1813-26. doi: 10.1517/14656566.2011.591382. Epub 2011 Jun 21.


Introduction: Although pharmacological treatments for obesity represent only one option in managing obesity, they are a useful tool in an otherwise extremely limited armamentarium. Naltrexone/bupropion combination therapy was developed by using technological advances that have improved our understanding of how the brain regulates body weight.

Areas covered: This review covers the development of naltrexone/bupropion combination therapy for obesity, as well as the published clinical trials on the safety and efficacy of the combination in overweight and obese humans. The effect of naltrexone/bupropion on food craving seems to be unique, and the implications of this finding for weight loss are discussed.

Expert opinion: Safety and tolerability issues seem to be manageable and consistent with the documented effects of each component. Appropriate patient management should address the mild sympathomimetic effect of bupropion, although the FDA has required that a cardiovascular outcomes study be conducted preapproval to determine the effects of long-term use of naltrexone/bupropion in an overweight/obese population. When used in conjunction with diet and exercise, the naltrexone/bupropion combination may be a useful treatment option for obesity, especially for overweight and obese adults who report difficulty controlling eating behavior and their response to food cravings.

Publication types

  • Review

MeSH terms

  • Animals
  • Bupropion / administration & dosage
  • Bupropion / adverse effects
  • Bupropion / therapeutic use*
  • Dopamine Uptake Inhibitors / administration & dosage
  • Dopamine Uptake Inhibitors / adverse effects
  • Dopamine Uptake Inhibitors / therapeutic use
  • Drug Combinations
  • Humans
  • Naltrexone / administration & dosage
  • Naltrexone / adverse effects
  • Naltrexone / therapeutic use*
  • Narcotic Antagonists / administration & dosage
  • Narcotic Antagonists / adverse effects
  • Narcotic Antagonists / therapeutic use
  • Obesity / drug therapy*
  • Obesity / physiopathology
  • Overweight / drug therapy
  • Overweight / physiopathology
  • Weight Loss / drug effects


  • Dopamine Uptake Inhibitors
  • Drug Combinations
  • Narcotic Antagonists
  • Bupropion
  • Naltrexone