Comparative Pharmacology
Head-to-head clinical analysis: ACTIQ versus OPANA ER.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ACTIQ versus OPANA ER.
ACTIQ vs OPANA ER
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Opioid agonist; binds to mu-opioid receptors in the CNS, altering pain perception and response.
Opana ER (oxymorphone hydrochloride) is a full opioid agonist with relative selectivity for the mu-opioid receptor, although it can interact with other opioid receptors at higher doses. The principal therapeutic action is analgesia via activation of mu-opioid receptors in the central nervous system, leading to altered perception and response to pain.
200 mcg transmucosally, titrated upward as needed; initial dose for opioid-tolerant patients is 200 mcg, with additional doses possible after 15 minutes if needed. Maximum 4 doses per episode. At least 4 hours between episodes.
Initial: 5 mg orally every 12 hours; titrate by 5-10 mg every 12 hours every 3-7 days; maximum 40 mg every 12 hours.
None Documented
None Documented
Terminal half-life 0.83–2 hours (mean 1.3 h) in adults; note that context: transmucosal absorption leads to rapid onset but short duration; half-life is not correlated with clinical effect due to oral transmucosal route and rapid redistribution.
Terminal elimination half-life: 11.1–13.8 hours; clinically relevant as steady-state achieved in 2–3 days
Primarily renal as metabolites (about 75% as metabolites, <10% unchanged). Fecal excretion accounts for <9%. Biliary excretion is minor.
Renal (primarily as glucuronide conjugates and unchanged drug): 85-90%; Fecal: <10%
Category C
Category C
Opioid Analgesic
Opioid Analgesic