Comparative Pharmacology
Head-to-head clinical analysis: LEVORPHANOL TARTRATE versus OPANA ER.
Head-to-head clinical analysis: LEVORPHANOL TARTRATE versus OPANA ER.
LEVORPHANOL TARTRATE vs OPANA 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.
Opana ER (oxymorphone hydrochloride) is a full opioid agonist with relative selectivity for the mu-opioid receptor, although it can interact with other opioid receptors at higher doses. The principal therapeutic action is analgesia via activation of mu-opioid receptors in the central nervous system, leading to altered perception and 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.
Initial: 5 mg orally every 12 hours; titrate by 5-10 mg every 12 hours every 3-7 days; maximum 40 mg every 12 hours.
None Documented
None Documented
11-16 hours; extended in hepatic impairment (up to 30 hours).
Terminal elimination half-life: 11.1–13.8 hours; clinically relevant as steady-state achieved in 2–3 days
Renal: approximately 30% as unchanged drug and 50% as glucuronide conjugates; fecal: 20% via biliary excretion.
Renal (primarily as glucuronide conjugates and unchanged drug): 85-90%; Fecal: <10%
Category C
Category C
Opioid Analgesic
Opioid Analgesic