Comparative Pharmacology
Head-to-head clinical analysis: DURAGESIC 75 versus OXYCONTIN.
Head-to-head clinical analysis: DURAGESIC 75 versus OXYCONTIN.
DURAGESIC-75 vs OXYCONTIN
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Fentanyl is a potent opioid agonist primarily at the mu-opioid receptor, exerting its analgesic effects by mimicking endogenous endorphins and enkephalins to activate G-protein-coupled inwardly rectifying potassium channels, leading to hyperpolarization and reduced neuronal excitability in pain pathways.
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.
Adults: Apply one 75 mcg/hr transdermal patch every 72 hours. Start with lower dose in opioid-naive patients.
10 mg orally every 12 hours; titrate based on pain severity and prior opioid exposure.
None Documented
None Documented
22-25 hours after removal of patch; increased in elderly, hepatic/renal impairment
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.
Renal (75% as metabolites, <10% unchanged), fecal (25%)
Primarily renal (90% as metabolites, 10% unchanged). Also biliary/fecal (10%).
Category C
Category C
Opioid Analgesic
Opioid Analgesic