Comparative Pharmacology
Head-to-head clinical analysis: PERCODAN versus ULTRACET.
Head-to-head clinical analysis: PERCODAN versus ULTRACET.
PERCODAN vs ULTRACET
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. Oxycodone acts on the central nervous system (CNS) to produce analgesia. Aspirin inhibits cyclooxygenase, leading to decreased prostaglandin synthesis, which reduces pain and inflammation.
ULTRACET is a combination of tramadol (a centrally acting opioid agonist) and acetaminophen (a centrally acting analgesic with antipyretic effects). Tramadol binds to mu-opioid receptors and inhibits norepinephrine and serotonin reuptake. Acetaminophen's mechanism is not fully understood but involves inhibition of cyclooxygenase (COX) enzymes in the central nervous system.
1-2 tablets orally every 4-6 hours as needed for pain. Each tablet contains oxycodone 4.5 mg and aspirin 325 mg.
1-2 tablets (37.5 mg tramadol/325 mg acetaminophen per tablet) orally every 4-6 hours as needed for pain, not to exceed 8 tablets per day.
None Documented
None Documented
Oxycodone: 3-5 hours, prolonged in elderly, hepatic/renal impairment. Aspirin: 2-3 hours at low doses; 15-30 hours at anti-inflammatory doses due to saturable metabolism.
Tramadol: 5.1 ± 0.9 hours (range 4-6 hours) for the parent drug; the active M1 metabolite has a half-life of 6.7 ± 1.7 hours. In hepatic impairment, tramadol half-life increases ~2-3 fold. Acetaminophen: 2-3 hours (range 1.25-3 hours); prolonged in overdose.
Oxycodone: primarily renal (65-87% as parent and metabolites, mostly noroxycodone and oxymorphone conjugates); ~10% fecal. Aspirin: renal (75-90% as salicylates and metabolites, dose-dependent).
Tramadol and its metabolites are primarily excreted via the kidneys (approximately 90% of the dose), with about 30% excreted as unchanged drug and 60% as metabolites. Approximately 10% is excreted in feces. Acetaminophen is primarily conjugated in the liver and excreted renally as glucuronide (60-80%) and sulfate (20-30%) conjugates, with about 5% excreted unchanged.
Category C
Category C
Opioid Analgesic Combination
Opioid Analgesic Combination