Comparative Pharmacology
Head-to-head clinical analysis: LEVORPHANOL TARTRATE versus OXYCONTIN.
Peer-Reviewed Evidence
Head-to-head clinical analysis: LEVORPHANOL TARTRATE versus OXYCONTIN.
LEVORPHANOL TARTRATE vs OXYCONTIN
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
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.
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.
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.
10 mg orally every 12 hours; titrate based on pain severity and prior opioid exposure.
None Documented
None Documented
11-16 hours; extended in hepatic impairment (up to 30 hours).
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: approximately 30% as unchanged drug and 50% as glucuronide conjugates; fecal: 20% via biliary excretion.
Primarily renal (90% as metabolites, 10% unchanged). Also biliary/fecal (10%).
Category C
Category C
Opioid Analgesic
Opioid Analgesic