Peripheral Opioid Antagonists:
A Therapeutic Advance for
Optimizing Opioid Gastrointestinal Tolerability

June 2007
A continuing medical education activity jointly sponsored by the University of Wisconsin School of Medicine and Public Health and the American Society of Pain Educators

Opioid analgesics remain one of the most effective treatments for moderate to severe pain, with 11 million Americans using them monthly. Opioids are safe and effective for the management of pain without producing end-organ toxicity, but their use is often limited because of predictable adverse events. Primary care physicians must be able to not only relieve their patients' pain, they must also treat any adverse events associated with these medications.

This supplement specifically addresses the impact of opioids on the gastrointestinal (GI) system; GI-related opioid physiology will be reviewed as well as current treatments for the management of opioid-induced side effects on the GI system. Beyond laxatives, treatment approaches that specifically target the underlying physiologic effects of opioids could revolutionize the management of opioid bowel dysfunction.

A novel class of medications, peripheral acting mu-opioid receptor (PAM-OR) antagonists, will be presented. PAM-OR antagonists are designed to reverse opioid-induced effects on the GI system without compromising the pain relief that is produced centrally. The mechanism of action in ameliorating peripheral opioid-induced side effects will also be discussed.

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