Pharmacologic treatment of opioid-induced constipation

Opioids are potent analgesics for treating moderate to severe pain, but their use is associated with a number of adverse effects, especially opioid-induced constipation (OIC). If the centrally mediated analgesia of opioids could be separated from their peripherally mediated gastrointestinal effects, by a peripherally acting opioid receptor antagonist, opioid-induced bowel dysfunction could be prevented or reversed. There has been considerable interest in peripherally acting opioid antagonists or other compounds to treat OIC. Subcutaneous methylnaltrexone is the first approved therapeutic agent for treatment of OIC, and studies have been conducted using the oral formulation. This editorial contains a brief overview of other selected compounds to treat OIC. Other potential uses of peripherally acting opioid antagonist in clinical practice are also discussed.