Classifications: analgesic; narcotic (opiate) agonist-antagonist; Therapeutic: narcotic analgesic; opiate
Pregnancy Category: C
Controlled Substance: Schedule III
0.3 mg (base)/mL injection; 2 mg, 8 mg sublingual tablets
Opiate agonist-antagonist with agonist activity approximately 30 times that of morphine and antagonist activity equal to
or up to 3 times that of naloxone. Respiratory depression occurs infrequently, probably due to drug's opiate antagonist
activity. Has a low level of physical dependence.
Dose-related analgesia results from a high affinity of buprenorphine for mu-opioid receptors and an antagonist at the kappa-opiate
receptors in the CNS. Naloxone is an antagonist at the mu-opioid receptor.
Injectable used for moderate to severe pain. Sublingual tablets used for treatment of opioid dependence.
Injectable to reverse fentanyl-induced anesthesia. Sublingual tablets may be used to ease cocaine withdrawal.
Hypersensitivity to buprenorphine or hypersensitivity to naloxone; pregnancy (category C), lactation, children <2 y.
Patient with history of opiate use; compromised respiratory function [e.g., chronic obstructive pulmonary disease (COPD),
cor pulmonale, decreased respiratory reserve, hypoxia, hypercapnia, or preexisting respiratory depression]; concomitant
use of other respiratory depressants; hypothyroidism, myxedema, Addison's disease; severe renal or hepatic impairment; geriatric
or debilitated patients; acute alcoholism, delirium tremens; prostatic hypertrophy, urethral stricture; comatose patient;
patients with CNS depression, head injury, or intracranial lesion; biliary tract dysfunction.
Route & Dosage
Adult/Adolescent (>12 y): IV/IM 0.3 mg q6h up to 0.6 mg q4h or 2550 mcg/h by IV infusion
Geriatric: IV/IM 0.15 mg q6h
Child (212 y): IV/IM 26 mcg/kg q46h prn
Opioid Dependence/Cocaine Withdrawal
Adult: SL Initiate with 8 mg q.d. Subutex on day 1 at least 4 h after last opioid dose, 16 mg q.d. Subutex on day 2, then switch to
Suboxone for maintenance therapy at the same buprenorphine dose as day 2 (e.g., 16 mg q.d.). Adjust dose daily until opiate
withdrawal effects are suppressed. Maintenance dose range 424 mg/d buprenorphine.
- Place SUBONONE and SUBUTEX tablets under tongue until dissolved. For doses requiring more than two tablets, place all tablets at once under tongue,
or if patient cannot accommodate all tablets, place two tablets at a time under tongue.
- Instruct to hold the tablets under tongue until dissolved; advise not to swallow.
- Give undiluted, deep IM into a large muscle.
PREPARE: Direct/IV Infusion: May be given undiluted direct IV or further dilute each 1 mL (0.3 mg) ampule in 50 mL of D5W, NS, D5NS, or RL to yield 6
mcg/mL for infusion. Do not use if discolored or contains particulate matter.
ADMINISTER: Direct: ??Give slowly at a rate of 0.3 mg over 2 min to a patient in a recumbent position. IV Infusion: Give by slow infusion over 3 min or longer depending on volume of IV solution.
INCOMPATIBILITIES Solution/Additive: Diltiazem, floxacillin, furosemide, lorazepam. Y-site: Amphotericin B cholesteryl sulfate complex, doxorubicin liposome, lansoprazole.
- Store at 15°30° C (59°86° F); avoid freezing.
Adverse Effects (≥1%)CNS: Sedation, drowsiness,
dizziness, vertigo, headache,
amnesia, euphoria, asthenia, insomnia, pain
(when used for withdrawal), withdrawal symptoms. CV:
Hypotension, vasodilation. Special Senses:
Miosis. GI: Nausea,
vomiting, diarrhea, constipation. Respiratory:
, hyperventilation. Skin:
Pruritus, injection site reactions, sweating.
InteractionsDrug: Alcohol, opiates
, other cns depressants
augment CNS depression; diazepam
may cause respiratory or cardiovascular collapse; azole antifungals
), macrolide antibiotics
), and protease inhibitors
) may increase buprenorphine levels.
Widely variable sublingual absorption. Onset:
1030 min IM/IV. Peak:
1 h IM/IV; 26 h SL. Duration:
610 h. Metabolism:
Extensively in liver by CYP3A4 to active metabolite norbuprenorphine. Elimination:
70% in feces, 30% in urine in 7 d. Half-Life:
2.2 h IM/IV; 37 h SL.
Assessment & Drug Effects
- Monitor respiratory status during therapy. Buprenorphine-induced respiratory depression is about equal to that produced
by 10 mg morphine, but onset is slower, and if it occurs, it lasts longer.
- Note: Respiratory depression in the healthy adult plateaus or may even decrease in severity with doses more than 1.2 mg because
of antagonist activity of the drug.
- Use lower dosing of buprenorphine with a concurrent NSAID or other nonnarcotic analgesic due to additive analgesic effect.
- Monitor I&O ratio and pattern during buprenorphine therapy; urinary retention is a potential adverse effect.
- Lab tests: Baseline liver function, renal function, alkaline phosphatase, and PSA.
- Supervise ambulation; drowsiness occurs in 66% of patients taking this drug.
Patient & Family Education
- Do not drive or engage in other potentially hazardous activities until response to drug is known.
- Do not use alcohol or other CNS depressing drugs without consulting physician. An additive effect exists between buprenorphine
hydrochloride and other CNS depressants including alcohol.