Comparative Pharmacology
Head-to-head clinical analysis: ABSTRAL versus XARTEMIS XR.
Head-to-head clinical analysis: ABSTRAL versus XARTEMIS XR.
ABSTRAL vs XARTEMIS XR
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Fentanyl is a potent mu-opioid receptor agonist, producing analgesia and sedation by activating G-protein coupled opioid receptors in the central nervous system.
XARTEMIS XR is a combination of oxycodone (a full mu-opioid receptor agonist) and acetaminophen (a centrally acting analgesic with antipyretic properties via cyclooxygenase inhibition).
For breakthrough pain in opioid-tolerant patients: initial dose 100 mcg sublingual tablet, titrate across strengths (100, 200, 300, 400, 600, 800 mcg) as needed; maximum 2 doses per episode, minimum 2 hours between episodes.
1 tablet (oxycodone 7.5 mg / acetaminophen 325 mg) orally every 12 hours; maximum 2 tablets per day.
None Documented
None Documented
Terminal elimination half-life: 6-10 hours (mean 8 hours); prolonged in elderly and hepatic impairment
Oxycodone: 5.3-6.6 hours (immediate-release), extended-release formulation shows prolonged absorption with apparent half-life ~7.2-9.6 hours; naloxone: 2-3 hours.
Renal: ~70% as metabolites (primarily fentanyl conjugates and norfentanyl), ~10% unchanged; Fecal: ~9%; Biliary: minimal
Renal: oxycodone and metabolites ~8.8% free oxycodone, ~8.8% noroxycodone, ~33% conjugated metabolites; naloxone: extensive hepatic metabolism, <1% excreted unchanged in urine. Fecal: naloxone metabolites ~17%.
Category C
Category C
Opioid Analgesic
Opioid Analgesic