Comparative Pharmacology
Head-to-head clinical analysis: ABSTRAL versus NUMORPHAN.
Head-to-head clinical analysis: ABSTRAL versus NUMORPHAN.
ABSTRAL vs NUMORPHAN
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.
Opioid agonist; binds to mu-opioid receptors in the CNS, inhibiting ascending pain pathways and altering pain perception.
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.
Intravenous or subcutaneous: 0.5-2 mg (0.1-0.2 mg/kg for severe pain) every 2-3 hours as needed; not to exceed 20 mg/day.
None Documented
None Documented
Terminal elimination half-life: 6-10 hours (mean 8 hours); prolonged in elderly and hepatic impairment
Terminal elimination half-life is 2–3 hours in adults; prolonged to 3–4 hours in elderly and up to 15 hours in patients with severe hepatic impairment.
Renal: ~70% as metabolites (primarily fentanyl conjugates and norfentanyl), ~10% unchanged; Fecal: ~9%; Biliary: minimal
Primarily renal (approximately 70% as unchanged drug, <5% as noroxymorphone and other conjugates); biliary/fecal excretion accounts for ~20%.
Category C
Category C
Opioid Analgesic
Opioid Analgesic