Comparative Pharmacology
Head-to-head clinical analysis: ACTIQ versus OXYMORPHONE HYDROCHLORIDE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ACTIQ versus OXYMORPHONE HYDROCHLORIDE.
ACTIQ vs OXYMORPHONE HYDROCHLORIDE
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.
Oxymorphone is a semi-synthetic opioid agonist that binds to mu-opioid receptors in the central nervous system, inhibiting ascending pain pathways and altering pain perception and response. It also has affinity for kappa and delta opioid receptors.
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: 1 mg IV/IM every 3-4 hours as needed for moderate to severe pain; titrate to effect. For patient-controlled analgesia (PCA), 0.5 mg IV loading dose, then 0.25-0.5 mg every 6-15 minutes with lockout. Rectal suppository: 5 mg every 4-6 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: 7-9 hours (range 4-12 h in elderly/renal impairment). Clinically, steady-state achieved within 24-36 hours.
Primarily renal as metabolites (about 75% as metabolites, <10% unchanged). Fecal excretion accounts for <9%. Biliary excretion is minor.
Primarily renal (90% as parent drug and metabolites); <1% fecal. Unchanged oxymorphone accounts for ~30% of urinary recovery.
Category C
Category C
Opioid Analgesic
Opioid Analgesic