The role of oxycodone/naloxone in the management of patients with pain and opioid-induced constipation

Expert Opin Pharmacother. 2019 Apr;20(5):511-522. doi: 10.1080/14656566.2018.1561863. Epub 2019 Jan 9.

Abstract

Common opioid adverse effects (AE) of the gastrointestinal tract include opioid-induced constipation (OIC) and opioid-induced bowel dysfunction (OIBD) with traditional laxatives being of limited efficacy, having AEs and not addressing the pathophysiology of OIC or OIBD. Targeted treatment comprises of PAMORA (peripherally acting mu-opioid receptor antagonists) and a combination of an opioid receptor agonist with its antagonist, namely prolonged-release oxycodone with prolonged-release naloxone (OXN) tablets at a fixed ratio of 2:1. Oxycodone provides analgesia, whereas naloxone prevents binding or displaces it from opioid receptors located in the gut wall. Areas covered: The authors review the role of OXN in the management of patients with pain and OIC. A literature search was performed using the search terms 'oxycodone/naloxone' and 'opioid-induced constipation' using the PubMed database up to October 2018. Expert opinion: OXN delivers analgesia comparable (or superior versus placebo and in observational studies) to oxycodone alone and other opioids with a limited or decreased disturbing effect on bowel function. OXN in daily doses of up to 160 mg/80 mg provides effective analgesia with little negative impact on bowel function. OXN may be successfully used in patients with chronic pain, to prevent or treat symptoms of OIC and OIBD.

Keywords: Opioid–induced constipation; chronic pain; opioid receptor antagonist; opioid–induced bowel dysfunction; oxycodone/naloxone.

Publication types

  • Review

MeSH terms

  • Analgesics, Opioid / administration & dosage
  • Analgesics, Opioid / adverse effects
  • Chronic Pain / drug therapy*
  • Constipation / chemically induced
  • Delayed-Action Preparations
  • Drug Combinations
  • Gastrointestinal Diseases / chemically induced
  • Humans
  • Laxatives / administration & dosage
  • Naloxone / administration & dosage*
  • Naloxone / adverse effects
  • Narcotic Antagonists / administration & dosage
  • Narcotic Antagonists / adverse effects
  • Oxycodone / administration & dosage*
  • Oxycodone / adverse effects
  • Receptors, Opioid / drug effects
  • Receptors, Opioid, mu / antagonists & inhibitors
  • Tablets

Substances

  • Analgesics, Opioid
  • Delayed-Action Preparations
  • Drug Combinations
  • Laxatives
  • Narcotic Antagonists
  • Receptors, Opioid
  • Receptors, Opioid, mu
  • Tablets
  • oxycodone naloxone combination
  • Naloxone
  • Oxycodone