Comparative Pharmacology
Head-to-head clinical analysis: DARVON N W ASA versus ULTRACET.
Peer-Reviewed Evidence
Head-to-head clinical analysis: DARVON N W ASA versus ULTRACET.
DARVON-N W/ ASA vs ULTRACET
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Propoxyphene is a weak opioid agonist that binds to mu-opioid receptors in the CNS, altering pain perception. Aspirin inhibits cyclooxygenase (COX-1 and COX-2), reducing prostaglandin synthesis, which mediates pain, fever, 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 capsules (propoxyphene napsylate 100 mg / aspirin 325 mg per capsule) orally every 4 hours as needed for pain; maximum 6 capsules per day.
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
Propoxyphene: terminal elimination half-life is 6-12 hours in adults with normal renal function; norpropoxyphene has a longer half-life (30-36 hours). Aspirin (as salicylate): half-life is dose-dependent, ranging from 2-3 hours at low doses to 15-30 hours at anti-inflammatory doses (300-600 mg in Darvon-N W/ASA).
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.
Renal: propoxyphene and its metabolites (norpropoxyphene) are primarily eliminated via kidneys, with ~20-25% excreted unchanged; fecal: minor; biliary: some enterohepatic recirculation occurs, but exact % are not well quantified for the combination product. Aspirin is hydrolyzed to salicylate, which is excreted renally (75% as salicyluric acid, 10% as salicylic acid, 10% as glucuronide conjugates, and minor amounts as gentisic acid).
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