Comparative Pharmacology
Head-to-head clinical analysis: BUTORPHANOL TARTRATE versus OPANA ER.
Head-to-head clinical analysis: BUTORPHANOL TARTRATE versus OPANA ER.
BUTORPHANOL TARTRATE vs OPANA ER
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Butorphanol tartrate is a mixed agonist-antagonist opioid analgesic that exerts its effects primarily through partial agonism at the mu-opioid receptor and full agonism at the kappa-opioid receptor. This results in analgesia with a ceiling effect for respiratory depression. It also has weak antagonistic activity at the mu receptor.
Opana ER (oxymorphone hydrochloride) is a full opioid agonist with relative selectivity for the mu-opioid receptor, although it can interact with other opioid receptors at higher doses. The principal therapeutic action is analgesia via activation of mu-opioid receptors in the central nervous system, leading to altered perception and response to pain.
1-2 mg intravenously or intramuscularly every 3-4 hours as needed; alternatively, 1-2 mg intranasally as a single dose (for migraine, may repeat after 60 minutes). For patient-controlled analgesia (PCA): 0.5-1 mg intravenous bolus with lockout interval of 10-15 minutes. Epidural: 0.5-2 mg as a single dose.
Initial: 5 mg orally every 12 hours; titrate by 5-10 mg every 12 hours every 3-7 days; maximum 40 mg every 12 hours.
None Documented
None Documented
Terminal elimination half-life is 2.5-3.5 hours (mean ~3 hours) in adults; prolonged in hepatic impairment (up to 5-6 hours) and renal impairment (variable, may increase).
Terminal elimination half-life: 11.1–13.8 hours; clinically relevant as steady-state achieved in 2–3 days
Primarily hepatic metabolism to inactive metabolites; renal excretion accounts for approximately 70-80% of elimination (mostly metabolites), with 15-20% via feces (biliary). Less than 5% excreted unchanged in urine.
Renal (primarily as glucuronide conjugates and unchanged drug): 85-90%; Fecal: <10%
Category C
Category C
Opioid Analgesic
Opioid Analgesic