Comparative Pharmacology
Head-to-head clinical analysis: DARVON versus LEVORPHANOL TARTRATE.
Head-to-head clinical analysis: DARVON versus LEVORPHANOL TARTRATE.
DARVON vs LEVORPHANOL TARTRATE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Propoxyphene is a mu-opioid receptor agonist that inhibits ascending pain pathways by binding to opioid receptors in the CNS, altering pain perception. It also has weak local anesthetic effects.
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.
Propoxyphene hydrochloride (Darvon) for moderate to severe pain: 65 mg orally every 4 hours as needed; maximum 390 mg/day.
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.
None Documented
None Documented
6-12 hours (parent drug); norpropoxyphene half-life 30-36 hours, accumulates with repeated dosing, increasing risk of toxicity.
11-16 hours; extended in hepatic impairment (up to 30 hours).
Primarily hepatic metabolism to norpropoxyphene, then renal excretion of metabolites; <20% excreted unchanged in urine; minor biliary/fecal elimination.
Renal: approximately 30% as unchanged drug and 50% as glucuronide conjugates; fecal: 20% via biliary excretion.
Category C
Category C
Opioid Analgesic
Opioid Analgesic