Comparative Pharmacology
Head-to-head clinical analysis: LEVORPHANOL TARTRATE versus MS CONTIN.
Head-to-head clinical analysis: LEVORPHANOL TARTRATE versus MS CONTIN.
LEVORPHANOL TARTRATE vs MS CONTIN
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; binds to mu-opioid receptors in the CNS, modulating pain perception and emotional response to pain.
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.
Oral: 15-30 mg every 8-12 hours; adjust based on pain severity and prior opioid use. Extended-release tablets must be swallowed whole; do not crush or chew. For opioid-naïve patients, start at 15 mg every 12 hours.
None Documented
None Documented
11-16 hours; extended in hepatic impairment (up to 30 hours).
Terminal elimination half-life: 11-13 hours (range 8-24 hours). In elderly or hepatic impairment, half-life may be prolonged; acute dosing half-life ~2-4 hours.
Renal: approximately 30% as unchanged drug and 50% as glucuronide conjugates; fecal: 20% via biliary excretion.
Renal: ~90% (mostly as morphine-3-glucuronide and morphine-6-glucuronide, with ~10% as unchanged morphine); Fecal: <10%
Category C
Category C
Opioid Analgesic
Opioid Analgesic