Comparative Pharmacology
Head-to-head clinical analysis: LEVORPHANOL TARTRATE versus ULTRAM ER.
Peer-Reviewed Evidence
Head-to-head clinical analysis: LEVORPHANOL TARTRATE versus ULTRAM ER.
LEVORPHANOL TARTRATE vs ULTRAM ER
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.
Tramadol is a centrally acting synthetic opioid analgesic that binds to μ-opioid receptors and inhibits serotonin and norepinephrine reuptake.
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.
100 mg orally once daily initially, titrate up to 100 mg twice daily as needed; maximum 200 mg/day.
None Documented
None Documented
11-16 hours; extended in hepatic impairment (up to 30 hours).
The terminal elimination half-life of tramadol is approximately 6.3 hours (range 5-9 hours), while its active metabolite M1 has a half-life of about 7.4 hours. Clinically, this supports dosing every 24 hours for the extended-release formulation.
Renal: approximately 30% as unchanged drug and 50% as glucuronide conjugates; fecal: 20% via biliary excretion.
Renal excretion of tramadol and its metabolites accounts for approximately 90% of total elimination. About 10% is excreted unchanged, 30% as O-desmethyltramadol (M1), and the remainder as other minor metabolites. Biliary/fecal excretion is minimal (<10%).
Category C
Category C
Opioid Analgesic
Opioid Analgesic