Comparative Pharmacology
Head-to-head clinical analysis: OXYCONTIN versus STADOL.
Head-to-head clinical analysis: OXYCONTIN versus STADOL.
OXYCONTIN vs STADOL
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.
Partial agonist at mu-opioid receptors and agonist at kappa-opioid receptors in the CNS, altering pain perception and emotional response to pain.
10 mg orally every 12 hours; titrate based on pain severity and prior opioid exposure.
Butorphanol tartrate 1-2 mg IV or IM every 3-4 hours as needed for pain; alternatively, 0.5-1 mg IV every 3-4 hours. For nasal spray: 1 mg (one spray) in one nostril, may repeat in 60-90 minutes if needed; then 1 mg every 3-4 hours as needed.
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.
Terminal elimination half-life: 2.5-4 hours; clinically, prolonged in hepatic impairment (up to 10-12 hours) and elderly
Primarily renal (90% as metabolites, 10% unchanged). Also biliary/fecal (10%).
Renal: 85-90% as unchanged drug and metabolites (primarily as glucuronide conjugates); Fecal: <10%; Biliary: minimal
Category C
Category C
Opioid Analgesic
Opioid Analgesic