Comparative Pharmacology
Head-to-head clinical analysis: OXYCONTIN versus PROPOXYPHENE HYDROCHLORIDE 65.
Peer-Reviewed Evidence
Head-to-head clinical analysis: OXYCONTIN versus PROPOXYPHENE HYDROCHLORIDE 65.
OXYCONTIN vs PROPOXYPHENE HYDROCHLORIDE 65
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Oxycodone is a full opioid agonist with relative selectivity for the mu-opioid receptor, although it can bind to other opioid receptors at higher doses. The principal therapeutic action of oxycodone is analgesia. Like all full opioid agonists, there is no ceiling effect for analgesia with oxycodone. Clinically, dosage is titrated to provide adequate analgesia and may be limited by adverse reactions, including respiratory and CNS depression.
Propoxyphene is a centrally acting opioid agonist that binds to mu-opioid receptors in the central nervous system, inhibiting pain signal transmission and altering pain perception. It also has local anesthetic effects.
10 mg orally every 12 hours; titrate based on pain severity and prior opioid exposure.
65 mg orally every 4 hours as needed for pain; maximum 390 mg/day.
None Documented
None Documented
4.5-5.0 hours (immediate-release); controlled-release OXYCONTIN has an apparent half-life of 4.5-8.7 hours. Terminal half-life is ~3.5-4 hours for immediate-release, reflecting context-sensitive elimination.
6-12 hours (mean ~8 hours); prolonged in hepatic impairment and elderly; accumulation possible with repeated dosing.
Primarily renal (90% as metabolites, 10% unchanged). Also biliary/fecal (10%).
Renal excretion of unchanged drug (approximately 20-30%) and metabolites; approximately 40-60% as conjugated metabolites; minor biliary/fecal elimination.
Category C
Category C
Opioid Analgesic
Opioid Analgesic