Comparative Pharmacology
Head-to-head clinical analysis: ACTIQ versus ULTIVA.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ACTIQ versus ULTIVA.
ACTIQ vs ULTIVA
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Opioid agonist; binds to mu-opioid receptors in the CNS, altering pain perception and response.
Selective mu-opioid receptor agonist with rapid onset and short duration of action; produces analgesia without significant histamine release.
200 mcg transmucosally, titrated upward as needed; initial dose for opioid-tolerant patients is 200 mcg, with additional doses possible after 15 minutes if needed. Maximum 4 doses per episode. At least 4 hours between episodes.
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
Terminal half-life 0.83–2 hours (mean 1.3 h) in adults; note that context: transmucosal absorption leads to rapid onset but short duration; half-life is not correlated with clinical effect due to oral transmucosal route and rapid redistribution.
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.
Primarily renal as metabolites (about 75% as metabolites, <10% unchanged). Fecal excretion accounts for <9%. Biliary excretion is minor.
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