Comparative Pharmacology
Head-to-head clinical analysis: DARVON versus NUMORPHAN.
Head-to-head clinical analysis: DARVON versus NUMORPHAN.
DARVON vs NUMORPHAN
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.
Opioid agonist; binds to mu-opioid receptors in the CNS, inhibiting ascending pain pathways and altering pain perception.
Propoxyphene hydrochloride (Darvon) for moderate to severe pain: 65 mg orally every 4 hours as needed; maximum 390 mg/day.
Intravenous or subcutaneous: 0.5-2 mg (0.1-0.2 mg/kg for severe pain) every 2-3 hours as needed; not to exceed 20 mg/day.
None Documented
None Documented
6-12 hours (parent drug); norpropoxyphene half-life 30-36 hours, accumulates with repeated dosing, increasing risk of toxicity.
Terminal elimination half-life is 2–3 hours in adults; prolonged to 3–4 hours in elderly and up to 15 hours in patients with severe hepatic impairment.
Primarily hepatic metabolism to norpropoxyphene, then renal excretion of metabolites; <20% excreted unchanged in urine; minor biliary/fecal elimination.
Primarily renal (approximately 70% as unchanged drug, <5% as noroxymorphone and other conjugates); biliary/fecal excretion accounts for ~20%.
Category C
Category C
Opioid Analgesic
Opioid Analgesic