Comparative Pharmacology
Head-to-head clinical analysis: LEVORPHANOL TARTRATE versus ZOHYDRO ER.
Peer-Reviewed Evidence
Head-to-head clinical analysis: LEVORPHANOL TARTRATE versus ZOHYDRO ER.
LEVORPHANOL TARTRATE vs ZOHYDRO 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.
Zohydro ER is a pure opioid agonist with relative selectivity for mu-opioid receptors, although it can interact with other opioid receptors at higher doses. Its primary therapeutic action is analgesia via binding to mu-opioid receptors in the central nervous system, leading to activation of descending inhibitory pathways and modulation of 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.
Initial: 20 mg orally every 24 hours; titrate in increments of 10-20 mg every 3-7 days as needed; maximum dose 200 mg every 24 hours.
None Documented
None Documented
11-16 hours; extended in hepatic impairment (up to 30 hours).
Terminal elimination half-life is approximately 10.6 hours (range 8-17 hours) due to extended-release formulation; immediate-release hydromorphone half-life is 2-3 hours. Clinically, steady-state is achieved after 3-5 days of dosing.
Renal: approximately 30% as unchanged drug and 50% as glucuronide conjugates; fecal: 20% via biliary excretion.
Primarily renal excretion of hydromorphone-3-glucuronide (H3G, ~60%), unchanged hydromorphone (~15%), and other conjugates. Fecal excretion accounts for ~25%.
Category C
Category C
Opioid Analgesic
Opioid Analgesic