Comparative Pharmacology
Head-to-head clinical analysis: DURAGESIC 75 versus LEVORPHANOL TARTRATE.
Head-to-head clinical analysis: DURAGESIC 75 versus LEVORPHANOL TARTRATE.
DURAGESIC-75 vs LEVORPHANOL TARTRATE
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.
Levorphanol is a potent opioid analgesic that acts as a mu-opioid receptor agonist. It also has NMDA receptor antagonist activity, inhibits norepinephrine and serotonin reuptake, and acts as a sigma receptor agonist, contributing to its analgesic effects and reduced tolerance development.
Adults: Apply one 75 mcg/hr transdermal patch every 72 hours. Start with lower dose in opioid-naive patients.
2 mg orally every 6-8 hours as needed for pain; for opioid-tolerant patients, doses up to 4 mg orally every 6-8 hours may be used. Parenterally: 1-2 mg subcutaneously or intramuscularly every 6-8 hours; may be given intravenously at 0.5-1 mg every 6-8 hours.
None Documented
None Documented
22-25 hours after removal of patch; increased in elderly, hepatic/renal impairment
11-16 hours; extended in hepatic impairment (up to 30 hours).
Renal (75% as metabolites, <10% unchanged), fecal (25%)
Renal: approximately 30% as unchanged drug and 50% as glucuronide conjugates; fecal: 20% via biliary excretion.
Category C
Category C
Opioid Analgesic
Opioid Analgesic