The undertreatment of acute and chronic pain continues to be a significant health concern in the U.S. Opioids are recommended for the treatment of acute or chronic pain of moderate to severe intensity that is not responsive to other pharmacologic agents, such as nonsteroidal antiinflammatory drugs. A high level of interindividual responses to the analgesic effects and side effects of opioids necessitates the availability of multiple treatment options. Extended-release and immediate-release oral formulations of oxymorphone hydrochloride were recently approved by the U.S. Food and Drug Administration and may provide new options for patients who have not achieved adequate and well-tolerated analgesia with their current opioid. This review provides an overview of the basic pharmacology (including pharmacokinetic and pharmacodynamic profiles), clinical efficacy and tolerability of both oral oxymorphone formulations.
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