Meeting the challenges of opioid-induced constipation in chronic pain management - a novel approach

Pharmacology. 2009;83(1):10-7. doi: 10.1159/000165778. Epub 2008 Oct 28.


Opioid analgesics are the cornerstone of pain management for moderate-to-severe cancer pain and, increasingly, chronic noncancer pain. Despite proven analgesic efficacy, the use of opioids is commonly associated with frequently dose-limiting constipation that seriously impacts on patients' quality of life. Agents currently used to manage opioid-induced constipation (OIC), such as laxatives, do not address the underlying opioid receptor-mediated cause of constipation and are often ineffective. A significant need therefore exists for more effective treatment options. A novel approach for selectively and locally antagonizing the gastrointestinal effects of opioids involves the coadministration of a mu-opioid receptor antagonist with negligible systemic availability, such as oral naloxone. Combination therapy with prolonged-release (PR) oxycodone plus PR naloxone has been shown to provide effective analgesia while preventing or reducing constipation. The current article highlights this novel strategy in its potential to significantly improve the quality of life of patients suffering from chronic pain, affording patients the benefit of full analgesia, without the burden of OIC.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Analgesics, Opioid / administration & dosage
  • Analgesics, Opioid / adverse effects*
  • Analgesics, Opioid / therapeutic use
  • Chronic Disease
  • Clinical Trials as Topic
  • Constipation / chemically induced*
  • Constipation / prevention & control
  • Dose-Response Relationship, Drug
  • Drug Therapy, Combination
  • Humans
  • Laxatives / therapeutic use
  • Naloxone / therapeutic use
  • Narcotic Antagonists / therapeutic use
  • Oxycodone / administration & dosage
  • Oxycodone / adverse effects
  • Oxycodone / therapeutic use
  • Pain / drug therapy*
  • Pain / etiology
  • Quality of Life


  • Analgesics, Opioid
  • Laxatives
  • Narcotic Antagonists
  • Naloxone
  • Oxycodone