Dosing and uses of Buprenex (buprenorphine)
Adult dosage forms and strengths
injectable solution: Schedule III (Buprenex)
- 0.3mg/mL
tablet, sublingual: Schedule III (generic)
- 2mg
- 8mg
Moderate-to-Severe Pain
0.3 mg IV/IM q6hr; for IV, administered slowly over 2 minutes; may be repeated once (up to 0.3 mg) if required 30-60 minutes after initial dose
Opioid Dependence
Induction (sublingual tablet)
- 8 mg SL on day 1, then 16 mg SL on day 2; continued over 3-4 days
Maintenance (buprenorphine-naloxone combination)
- Switch to buprenorphine/naloxone combination for unsupervised maintenance
- For dosing, see drug monograph for buprenorphine/naloxone
Dosage modifications
Renal impairment: Use with caution; dosage adjustments recommended
Hepatic impairment
- Mild: No dose adjustment is needed
- Moderate: No dose adjustment is necessary, closely monitor patients for signs and symptoms of toxicity or overdose
- Severe: Reducing the starting and titration incremental dose by half, and monitor for signs and symptoms of toxicity or overdose
Dosing Considerations
For prescriber qualifications, see prescribing information
Also given in combination with naloxone
Decrease dose with hepatic or renal impairment, respiratory disease, geriatric or debilitated patients
Pediatric dosage forms and strengths
injectable solution: Schedule III (Buprenex)
- 0.3mg/mL
tablet, sublingual: Schedule III (generic)
- 2mg
- 8mg
Moderate-to-Severe Pain
<2 years: Safety and efficacy not established
2-12 years: 2-6 mcg/kg slow IV/IM q4-6hr PRn
>12 years: As in adults
Opioid Dependence
<16 years: Not recommended
≥16 years: As in adults
Geriatric dosage forms and strengths
Moderate-to-Severe Pain
0.15 mg IV/IM q6hr; for IV, administered slowly over 2 minutes
Buprenex (buprenorphine) adverse (side) effects
>10%
Sedation (2/3 of patients)
1-10%
Dizziness
Headache
Hypotension
Hypoventilation
Miosis
Nausea
Sweating
Vertigo
Vomiting
<1%
Abdominal cramps
Amblyopia
Apnea
Blurred vision
Bradycardia
Coma
Confusion
Conjunctivitis
Constipation
Cyanosis
Depersonalization
Diplopia
Dreaming
Dry mouth
Dyspepsia
Dyspnea
Electrocardiographic (ECG) abnormalities
Euphoria
Fatigue
Flatulence
Hallucinations
Hypertension
Injection-site reactions
Malaise
Mental depression
Mydriasis
Nervousness
Paresthesia
Pruritus
Psychosis
Respiratory depression
Slurred speech
Tachycardia
Urticaria
Warnings
Contraindications
Hypersensitivity
Cautions
Respiratory depression, pulmonary impairment, concomitant respiratory depressants
Hypothyroidism, myxedema, adrenocortical insufficiency, alcohol intoxication, alcohol withdrawal syndrome, coma, geriatric or debilitated patients, delirium tremens, toxic psychoses, kyphoscoliosis, prostatic hypertrophy, urethral stricture, central nervous system (CNS) depression, biliary tract dysfunction, head injury, intracranial lesions, intracranial hypertension or conditions in which intracranial pressure may be increased
Severe renal impairment
Severe hepatic impairment can cause increased buprenorphine plasma levels and prolonged half-life, but not in subjects with mild hepatic impairment; dose adjustment recommended in patients with moderate or severe hepatic; consider reducing the dose by half and closely monitor for signs and symptoms of toxicity and overdose (see Dosage modifications)
Concurrent use with other CNS depressants
Respiratory sedation (dose-dependent; usual doses may depress respiration to same degree as 10 mg of parenteral morphine)
May produce withdrawal in opioid-dependent patients
Pregnancy and lactation
Pregnancy category: C
Lactation: Drug enters breast milk; use not recommended
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Buprenex (buprenorphine)
Mechanism of action
Semisynthetic narcotic mixed agonist-antagonist analgesic; exerts agonistic effects at mu and delta opioid receptors in CNS and antagonistic effects at kappa opioid receptor
Absorption
Bioavailability: 79%
Onset: IM, 15 min
Duration: 4-10 hr
Peak plasma time: <2 min
Peak plasma concentration: 18 ng/mL
Distribution
Protein bound: 96%
Vd: 97-187 L/kg
Metabolism
Liver (N-dealkylation)
Metabolized in liver via N-dealkylation
Metabolites: Norbuprenorphine (N-dealkylbuprenorphine)
Elimination
Half-life: 2.2 hr
Excretion: Urine, feces
Administration
IV Incompatibilities
Additive: Floxacillin, furosemide
Y-site: Amphotericin B cholesteryl sulfate, doxorubicin liposomaL
IV Compatibilities
Additive: Bupivacaine
Syringe: Heparin, midazolam
Y-site: Allopurinol, amifostine, aztreonam, cefepime, cisatracurium, cladribine, docetaxel, etoposide phosphate, filgrastim, gatifloxacin, gemcitabine, granisetron, linezolid, melphalan, piperacillin-tazobactam, propofol, remifentanil, teniposide, thiotepa, vinorelbine
IV Preparation
Solution: Dilute to final concentration of 15 mcg/mL in D5W, D5/NS, NS, or Lr
Administer via controlled infusion device
IV/IM Administration
Administer by deep IM injection, by slow IV injection over ≥2 minutes, or by continuous IV infusion
Also may be given by epidural injection at concentration of 6-30 mcg/mL
Storage
Store at 15-30°C; protect from freezing
Protect from prolonged exposure to light
