Comparative Pharmacology
Head-to-head clinical analysis: DOLENE AP 65 versus ULTRACET.
Peer-Reviewed Evidence
Head-to-head clinical analysis: DOLENE AP 65 versus ULTRACET.
DOLENE AP-65 vs ULTRACET
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
DOLENE AP-65 is a combination of dipyrone (metamizole) and propantheline. Dipyrone is a non-opioid analgesic and antipyretic that acts centrally and peripherally via inhibition of cyclooxygenase and activation of the endocannabinoid system. Propantheline is an anticholinergic agent that inhibits muscarinic acetylcholine receptors, reducing gastrointestinal motility and spasm.
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.
DOLENE AP-65 (propoxyphene napsylate 100 mg and acetaminophen 650 mg). Adult: 1 tablet orally every 4 hours as needed for pain. Maximum: 6 tablets 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
2-3 hours in adults with normal hepatic function; prolonged in hepatic impairment (up to 5-10 hours) and in neonates (up to 3-5 hours)
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: 90% (50% as acetaminophen glucuronide, 30% as sulfate, 5% as cysteine, 3% as unchanged drug, 2% as other metabolites); Fecal: <5%
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