Comparative Pharmacology
Head-to-head clinical analysis: LEVORPHANOL TARTRATE versus ORAMORPH SR.
Peer-Reviewed Evidence
Head-to-head clinical analysis: LEVORPHANOL TARTRATE versus ORAMORPH SR.
LEVORPHANOL TARTRATE vs ORAMORPH SR
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.
Morphine is a full opioid agonist with relative selectivity for the mu-opioid receptor, although it can interact with other opioid receptors at higher doses. Binding to mu-opioid receptors in the central nervous system (CNS) and peripheral tissues results in analgesia, euphoria, sedation, respiratory depression, and physical dependence. Morphine also activates descending inhibitory pathways and inhibits ascending nociceptive transmission.
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.
10-30 mg orally every 8-12 hours, sustained-release; titrate as needed for pain.
None Documented
None Documented
11-16 hours; extended in hepatic impairment (up to 30 hours).
2–4 hours in adults; in controlled-release formulation, effective half-life is prolonged due to sustained absorption. Clinically, steady-state is achieved in 1–2 days.
Renal: approximately 30% as unchanged drug and 50% as glucuronide conjugates; fecal: 20% via biliary excretion.
Renal (approximately 90% as morphine-3-glucuronide and morphine-6-glucuronide, minor amounts of unchanged morphine, and other conjugates); biliary/fecal (approximately 10%).
Category C
Category C
Opioid Analgesic
Opioid Analgesic