Comparative Pharmacology
Head-to-head clinical analysis: BUTORPHANOL TARTRATE PRESERVATIVE FREE versus OPANA.
Head-to-head clinical analysis: BUTORPHANOL TARTRATE PRESERVATIVE FREE versus OPANA.
BUTORPHANOL TARTRATE PRESERVATIVE FREE vs OPANA
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Butorphanol is a mixed agonist-antagonist opioid analgesic acting at mu- and kappa-opioid receptors; it exerts its analgesic effects primarily via kappa-opioid receptor agonism and partial mu-opioid receptor agonism/antagonism.
Mu-opioid receptor agonist; produces analgesia by binding to opioid receptors in the CNS, inhibiting ascending pain pathways and altering pain perception.
Adults: 1-2 mg intramuscularly or intravenously every 3-4 hours as needed for pain; alternatively, 0.5-1 mg intravenously every 3-4 hours. For epidural administration: 1-2 mg at the lumbar level, may repeat once after 60 minutes if needed.
5-20 mg orally every 4-6 hours as needed for pain; extended-release tablets: 5 mg orally every 12 hours, titrated up to 20 mg every 12 hours.
None Documented
None Documented
Terminal elimination half-life: 2.5-3.5 hours (IV); 4-6 hours (IM). In hepatic impairment, half-life may increase to 5-9 hours; in renal impairment, minimal change unless severe.
Terminal elimination half-life is 11-16 hours (mean 14 hours) in adults; prolonged in hepatic impairment (up to 30 hours) and elderly.
Primarily renal (70-80% as unchanged drug and metabolites; 5% unchanged), biliary/fecal (15-20%), with enterohepatic recirculation.
Primarily renal (approximately 90% as conjugated metabolites, 10% unchanged); biliary/fecal elimination accounts for <10%.
Category C
Category C
Opioid Analgesic
Opioid Analgesic