Comparative Pharmacology
Head-to-head clinical analysis: OXYCONTIN versus ULTRAM ER.
Head-to-head clinical analysis: OXYCONTIN versus ULTRAM ER.
OXYCONTIN vs ULTRAM ER
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.
Tramadol is a centrally acting synthetic opioid analgesic that binds to μ-opioid receptors and inhibits serotonin and norepinephrine reuptake.
10 mg orally every 12 hours; titrate based on pain severity and prior opioid exposure.
100 mg orally once daily initially, titrate up to 100 mg twice daily as needed; maximum 200 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.
The terminal elimination half-life of tramadol is approximately 6.3 hours (range 5-9 hours), while its active metabolite M1 has a half-life of about 7.4 hours. Clinically, this supports dosing every 24 hours for the extended-release formulation.
Primarily renal (90% as metabolites, 10% unchanged). Also biliary/fecal (10%).
Renal excretion of tramadol and its metabolites accounts for approximately 90% of total elimination. About 10% is excreted unchanged, 30% as O-desmethyltramadol (M1), and the remainder as other minor metabolites. Biliary/fecal excretion is minimal (<10%).
Category C
Category C
Opioid Analgesic
Opioid Analgesic