Comparative Pharmacology
Head-to-head clinical analysis: LEVORPHANOL TARTRATE versus OPANA.
Head-to-head clinical analysis: LEVORPHANOL TARTRATE versus OPANA.
LEVORPHANOL TARTRATE vs OPANA
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.
Mu-opioid receptor agonist; produces analgesia by binding to opioid receptors in the CNS, inhibiting ascending pain pathways and altering pain perception.
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.
5-20 mg orally every 4-6 hours as needed for pain; extended-release tablets: 5 mg orally every 12 hours, titrated up to 20 mg every 12 hours.
None Documented
None Documented
11-16 hours; extended in hepatic impairment (up to 30 hours).
Terminal elimination half-life is 11-16 hours (mean 14 hours) in adults; prolonged in hepatic impairment (up to 30 hours) and elderly.
Renal: approximately 30% as unchanged drug and 50% as glucuronide conjugates; fecal: 20% via biliary excretion.
Primarily renal (approximately 90% as conjugated metabolites, 10% unchanged); biliary/fecal elimination accounts for <10%.
Category C
Category C
Opioid Analgesic
Opioid Analgesic