MR-oxycodone/naloxone is an oral combination opioid analgesic. The naloxone component is subject to a significant first-pass metabolism, and bioavailability is less than 2%. The benefit of low level oral bioavailability… Click to show full abstract
MR-oxycodone/naloxone is an oral combination opioid analgesic. The naloxone component is subject to a significant first-pass metabolism, and bioavailability is less than 2%. The benefit of low level oral bioavailability of naloxone is reducedopioid-induced constipationdue to antagonism of opioid receptors in the gut while permitting the desired analgesic opioid effects. The recommended dose of MR-oxycodone/naloxone ranges from 2.5/1.25 mg to 80/40 mg twice daily— the upper limit guiding prescribers to avoid further opioid dose escalation.
               
Click one of the above tabs to view related content.