Comparative Pharmacology
Head-to-head clinical analysis: DURAGESIC 75 versus ULTIVA.
Head-to-head clinical analysis: DURAGESIC 75 versus ULTIVA.
DURAGESIC-75 vs ULTIVA
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
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.
Selective mu-opioid receptor agonist with rapid onset and short duration of action; produces analgesia without significant histamine release.
Adults: Apply one 75 mcg/hr transdermal patch every 72 hours. Start with lower dose in opioid-naive patients.
IV bolus: 1 mcg/kg over 30-60 seconds, then continuous IV infusion: 0.25-1 mcg/kg/min for intraoperative analgesia. For general anesthesia induction: 0.5-1 mcg/kg IV bolus; maintenance: 0.25-1 mcg/kg/min IV infusion.
None Documented
None Documented
22-25 hours after removal of patch; increased in elderly, hepatic/renal impairment
Terminal elimination half-life is 3-10 minutes (context-sensitive half-time is 3-4 minutes independent of infusion duration due to rapid ester hydrolysis). Clinically, recovery is rapid and predictable even after prolonged infusions, with full recovery within 5-10 minutes of discontinuation.
Renal (75% as metabolites, <10% unchanged), fecal (25%)
Remifentanil is metabolized by non-specific blood and tissue esterases to a virtually inactive metabolite (remifentanil acid, 1/4600 potency). Renal excretion accounts for approximately 90% of the metabolite; fecal elimination is minimal (<5%).
Category C
Category C
Opioid Analgesic
Opioid Analgesic