Novel opioid antagonists for opioid-induced bowel dysfunction and postoperative ileus

Lancet. 2009 Apr 4;373(9670):1198-206. doi: 10.1016/S0140-6736(09)60139-2. Epub 2009 Feb 13.


Peripherally acting mu-opioid receptor antagonists methylnaltrexone and alvimopan are a new class of drugs designed to reverse opioid-induced side-effects on the gastrointestinal system without compromising pain relief. This article gives an overview of the pharmacology, the efficacy, and adverse effects of these drugs. Both compounds seem to be generally well tolerated and effective for the treatment of opioid-related bowel dysfunction and postoperative ileus. Methylnaltrexone recently received approval by the US Food and Drug Administration (FDA) and the European Medicines Agency for treatment of opioid-related bowel dysfunction in patients with advanced illness. Alvimopan was recently approved by the FDA for treatment of postoperative ileus, but the use of the drug is restricted to inpatients because it has been associated with an increased rate of myocardial infarction. Further research should assess the effectiveness and safety of these drugs in clinical practice.

Publication types

  • Review

MeSH terms

  • Analgesics, Opioid / adverse effects*
  • Blood-Brain Barrier / drug effects
  • Drug Approval
  • Europe
  • Humans
  • Ileus* / chemically induced
  • Ileus* / drug therapy
  • Myocardial Infarction / chemically induced
  • Naltrexone / analogs & derivatives*
  • Naltrexone / chemistry
  • Naltrexone / pharmacology
  • Naltrexone / therapeutic use
  • Narcotic Antagonists / chemistry
  • Narcotic Antagonists / pharmacology
  • Narcotic Antagonists / therapeutic use*
  • Patient Selection
  • Piperidines / chemistry
  • Piperidines / pharmacology
  • Piperidines / therapeutic use*
  • Postoperative Complications* / chemically induced
  • Postoperative Complications* / drug therapy
  • Quaternary Ammonium Compounds / chemistry
  • Quaternary Ammonium Compounds / pharmacology
  • Quaternary Ammonium Compounds / therapeutic use
  • Research Design
  • Safety
  • United States
  • United States Food and Drug Administration


  • Analgesics, Opioid
  • Narcotic Antagonists
  • Piperidines
  • Quaternary Ammonium Compounds
  • methylnaltrexone
  • Naltrexone
  • alvimopan