The Medical Letter on Drugs and Therapeutics
Oral Oxymorphone (Opana)
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Oxymorphone hydrochloride, a semi-synthetic opioid agonist, has been available for many years in the US as Numorphan (Endo) for parenteral use and as a rectal suppository. Now it has been approved by the FDA for oral administration as an immediate-release (IR) tablet (Opana) for treatment of moderate to severe acute pain, and as an extended-release tablet (Opana ER) for treatment of moderate to severe pain in patients requiring continuous opioid treatment for an extended period of time.

PHARMACOKINETICS — The oral bioavailability of oxymorphone is only about 10%; it is increased in patients with diminished hepatic or renal function. Serum concentrations, which reach a peak (Cmax) in 30 minutes with the IR form and 2.5-4 hours with the ER tablet, are dose-proportional. Food increases the Cmax of oral oxymorphone by 38-50%. The drug is primarily metabolized in the liver by conjugation with ... more      

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Title: Oral Oxymorphone (Opana)
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