Comparative Pharmacology
Head-to-head clinical analysis: ABSTRAL versus DURAGESIC 75.
Head-to-head clinical analysis: ABSTRAL versus DURAGESIC 75.
ABSTRAL vs DURAGESIC-75
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.
Fentanyl is a potent opioid agonist primarily at the mu-opioid receptor, exerting its analgesic effects by mimicking endogenous endorphins and enkephalins to activate G-protein-coupled inwardly rectifying potassium channels, leading to hyperpolarization and reduced neuronal excitability in pain pathways.
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.
Adults: Apply one 75 mcg/hr transdermal patch every 72 hours. Start with lower dose in opioid-naive patients.
None Documented
None Documented
Terminal elimination half-life: 6-10 hours (mean 8 hours); prolonged in elderly and hepatic impairment
22-25 hours after removal of patch; increased in elderly, hepatic/renal impairment
Renal: ~70% as metabolites (primarily fentanyl conjugates and norfentanyl), ~10% unchanged; Fecal: ~9%; Biliary: minimal
Renal (75% as metabolites, <10% unchanged), fecal (25%)
Category C
Category C
Opioid Analgesic
Opioid Analgesic