Comparative Pharmacology
Head-to-head clinical analysis: OXYCONTIN versus OXYMORPHONE HYDROCHLORIDE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: OXYCONTIN versus OXYMORPHONE HYDROCHLORIDE.
OXYCONTIN vs OXYMORPHONE HYDROCHLORIDE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Oxycodone is a full opioid agonist with relative selectivity for the mu-opioid receptor, although it can bind to other opioid receptors at higher doses. The principal therapeutic action of oxycodone is analgesia. Like all full opioid agonists, there is no ceiling effect for analgesia with oxycodone. Clinically, dosage is titrated to provide adequate analgesia and may be limited by adverse reactions, including respiratory and CNS depression.
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.
10 mg orally every 12 hours; titrate based on pain severity and prior opioid exposure.
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
4.5-5.0 hours (immediate-release); controlled-release OXYCONTIN has an apparent half-life of 4.5-8.7 hours. Terminal half-life is ~3.5-4 hours for immediate-release, reflecting context-sensitive elimination.
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 (90% as metabolites, 10% unchanged). Also biliary/fecal (10%).
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