7 days.Absorption: Well absorbed after IM and SL use; 4665% absorbed with buccal use; 15% of transdermal dose absorbed through skin; IV administration results in complete bioavailability.
Distribution: Crosses the placenta; enters breast milk. CNS concentration is 1525% of plasma.
Protein Binding: 96%.
Metabolism/Excretion: Mostly metabolized by the liver mostly via the CYP3A4 enzyme system; one metabolite is active; 70% excreted in feces; 27% excreted in urine.
Half-life: 23 hr (IV); 27 hr (buccal); 26 hr (transdermal); 37 hr (SL); 2448 hr (subdermal); 4360 days (subcut).
Contraindicated in:
Use Cautiously in:
CV: hypertension, hypotension, palpitations, QT interval prolongation.
Derm: sweating, clammy feeling, erythema, pruritus, rash.
EENT: blurred vision, diplopia, miosis (high doses).
Endo: adrenal insufficiency.
GI: HEPATOTOXICITY, nausea, constipation, dry mouth, ileus, vomiting.
GU: urinary retention.
Neuro: confusion, dysphoria, hallucinations, sedation, dizziness, euphoria, floating feeling, headache, unusual dreams.
Resp: RESPIRATORY DEPRESSION (INCLUDING CENTRAL SLEEP APNEA AND SLEEP-RELATED HYPOXEMIA).
Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS, ANGIOEDEMA, AND BRONCHOSPASM), injection site reactions, physical dependence, psychological dependence, tolerance.
Drug-Drug:
Drug-Natural Products:
Analgesia
4 days, then ↑ dose to 150 mcg every 12 hr; may then titrate dose in increments of 150 mcg every 12 hr no more frequently than every 4 days; do not exceed dose of 450 mcg every 12 hr (based on clinical studies); Previously taking <30 mg/day of morphine or equivalent Initiate therapy with 75 mcg once daily or every 12 hr for
4 days, then ↑ dose to 150 mcg every 12 hr; may then titrate dose in increments of 150 mcg every 12 hr no more frequently than every 4 days; do not exceed dose of 900 mcg every 12 hr (due to ↑ risk of QT interval prolongation); Previously taking 3089 mg/day of morphine or equivalent Initiate therapy with 150 mcg every 12 hr for
4 days; may then titrate dose in increments of 150 mcg every 12 hr no more frequently than every 4 days; do not exceed dose of 900 mcg every 12 hr (due to ↑ risk of QT interval prolongation); Previously taking 90160 mg/day of morphine or equivalent Initiate therapy with 300 mcg every 12 hr for
4 days; may then titrate dose in increments of 150 mcg every 12 hr no more frequently than every 4 days; do not exceed dose of 900 mcg every 12 hr (due to ↑ risk of QT interval prolongation); Previously taking >160 mg/day of morphine or equivalent Consider use of alternate analgesic; Patients with oral mucositis ↓initial dose by 50% then titrate dose in increments of 75 mcg every 12 hr no more frequently than every 4 days.Hepatic Impairment
Hepatic Impairment
Treatment of Opioid Use Disorder
Hepatic Impairment
IV Administration:
Belbuca, Buprenex, Butrans, Probuphine, Sublocade, Subutex
Therapeutic Classification: opioid analgesics
Pharmacologic Classification: opioid agonists antagonists
(Generic available)
(analgesia)
NDC Code*