Comparative Pharmacology
Head-to-head clinical analysis: BUTRANS versus NUMORPHAN.
Peer-Reviewed Evidence
Head-to-head clinical analysis: BUTRANS versus NUMORPHAN.
BUTRANS vs NUMORPHAN
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Buprenorphine is a partial mu-opioid receptor agonist and a weak kappa-opioid receptor antagonist. It binds with high affinity to mu-opioid receptors, producing analgesic and opioid effects with a ceiling effect on respiratory depression.
Opioid agonist; binds to mu-opioid receptors in the CNS, inhibiting ascending pain pathways and altering pain perception.
Apply one BUTRANS (buprenorphine) transdermal system to a clean, dry, non-irritated, and non-hairy area of the chest, back, flank, or upper arm. Initial dose: 5 mcg/h for opioid-naïve patients; titrate based on pain control and tolerability. Maximum dose: 20 mcg/h. Replace every 7 days. Rotate application sites.
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 half-life: 4-6 hours in healthy adults; prolonged to 12-18 hours in elderly or renal 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: 60-70% as unchanged drug and metabolites; biliary/fecal: 20-30%
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