buprenorphine (Rx)

Brand and Other Names:Buprenex
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Dosing & Uses


Dosage Forms & 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

Dosage Forms & 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

Moderate-to-Severe Pain

0.15 mg IV/IM q6hr; for IV, administered slowly over 2 minutes



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            Adverse Effects


            Sedation (2/3 of patients)












            Abdominal cramps



            Blurred vision










            Dry mouth



            Electrocardiographic (ECG) abnormalities






            Injection-site reactions


            Mental depression






            Respiratory depression

            Slurred speech



            Postmarketing Reports

            Adrenal Insufficiency

            Serotonin syndrome




            Balck Box Warnings

            Addiction, abuse, and misuse

            • Risk of opioid addiction, abuse, and misuse, which can lead to overdose and death
            • Assess each patient’s risk prior to prescribing and monitor all patients regularly for the development of these behaviors or conditions

            Life-threatening respiratory depression

            • Serious, life-threatening, or fatal respiratory depression may occur
            • Monitor for respiratory depression, especially during initiation or following a dose increase

            Accidental exposure

            • Accidental exposure of even 1 dose, especially by children, can result in a fatal overdose

            Neonatal Opioid Withdrawal Syndrome

            • Prolonged use during pregnancy can result in neonatal opioid withdrawal syndrome, which may be life-threatening if not recognized and treated, and requires management according to protocols developed by neonatology experts
            • Syndrome presents as irritability, hyperactivity and abnormal sleep pattern, high-pitched cry, tremor, vomiting, diarrhea, and failure to gain weight
            • Onset, duration, and severity of neonatal opioid withdrawal syndrome vary based on the specific opioid used, duration of use, timing and amount of last maternal use, and rate of elimination of the drug by the newborn
            • If opioid use is required for a prolonged period in a pregnant woman, advise the patient of the risk of neonatal opioid withdrawal syndrome and ensure that appropriate treatment will be available

            Risks From Concomitant Use With Benzodiazepines Or Other CNS Depressants

            • Concomitant use of opioids with benzodiazepines or other central nervous system (CNS) depressants, including alcohol, may result in profound sedation, respiratory depression, coma, and death; reserve concomitant prescribing for use in patients for whom alternative treatment options are inadequate; limit dosages and durations to minimum required; and follow patients for signs and symptoms of respiratory depression and sedation



            Significant respiratory depression

            Acute or severe bronchial asthma in an unmonitored setting or in the absence of resuscitative equipment

            Known or suspected gastrointestinal obstruction, including paralytic ileus


            Partial agonist at the mu opioid receptor and a schedule III controlled opioid exposes users to the risks of addiction, abuse, and misuse; there is a greater risk for overdose and death with extended-release opioids owing to the larger amount of active opioid present (see Black Box Warnings)

            Serious, life-threatening, or fatal respiratory depression reported; may occur more frequently in elderly or debilitated patients, or in conditions associated with hypoxia or hypercapnia (even moderate therapeutic doses) (see Black Box Warnings)

            Neonatal opioid withdrawal syndrome reported with long-term use during pregnancy (see Black Box Warnings)

            Accidental exposure reported, including fatalities (see Black Box Warnings)

            Associated with life-threatening respiratory depression and death; many, but not all, post-marketing reports regarding coma and death have involved misuse by self-injection or were associated with concomitant use of buprenorphine and benzodiazepines or other CNS depressants, including alcohol; warn patients of potential danger of self-administration of benzodiazepines or other CNS depressants while under treatment

            Interactions with CNS depressants (eg, alcohol, sedatives, anxiolytics, hypnotics, neuroleptics, other opioids) can cause additive effects and increase risk for respiratory depression, profound sedation, and hypotension

            Risk of apnea in patients with chronic pulmonary disease; closely monitor these patients, when initiating and titrating therapy; alternatively, consider the use of alternative non-opioid analgesics in these patients (see Black Box Warnings and Contraindications)

            QTc prolongation observed in healthy individuals at 40 mcg/hr; avoid in patients with history of long QT syndrome or coadministration with class IA (eg, quinidine, procainamide, disopyramide) or class III (eg, sotalol, amiodarone, dofetilide) antiarrhythmics

            Respiratory depressant effects of opioids may include carbon dioxide retention and lead to elevated CSF pressure

            Can cause severe hypotension; caution with depleted blood volume or coadministration of drugs that that affect vasomotor tone (eg, phenothiazines), vasodilators, or antihypertensives

            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

            Cases of cytolytic hepatitis and hepatitis with jaundice observed in individuals receiving buprenorphine SL for opioid dependence treatment; increased risk for overdose with moderate or severe hepatic impairment (see Dosage Modifications)

            Anaphylactic reactions reported

            Caution in 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)

            May cause sphincter of Oddi spasm and aggravate abdominal conditions, including ileus (see Contraindications)

            Respiratory sedation (dose-dependent; usual doses may depress respiration to same degree as 10 mg of parenteral morphine)

            Similar to other opioids, may aggravate seizure disorders by lowering seizure threshold

            Patients with cancer who have oral mucositis may absorb buprenorphine more rapidly than intended and have higher plasma levels of buprenorphine (see Dosage Modifications)

            Special risk groups may experience increased adverse reactions; caution with alcoholism, delirium tremens, adrenocortical insufficiency, CNS depression, debilitation, kyphoscoliosis associated with respiratory compromise, myxedema or hypothyroidism, prostatic hypertrophy or urethral stricture, severe impairment of hepatic, pulmonary or renal function, and toxic psychosis

            Prescribers should discuss with patients importance and benefits of management of opioid addiction throughout pregnancy

            Cases of adrenal insufficiency reported with opioid use, more often following greater than one month of use; symptoms may include nausea, vomiting, anorexia, fatigue, weakness, dizziness, and low blood pressure; if adrenal insufficiency is diagnosed, treat with physiologic replacement doses of corticosteroids; wean patient off of opioid to allow adrenal function to recover and continue corticosteroid treatment until adrenal function recovers; other opioids may be tried as some cases reported use of a different opioid without recurrence of adrenal insufficiency

            Consider discontinuing therapy 24-36 hr prior anticipated need for surgical anesthesia to undergo elective surgery; may administer short-acting opioids during and/or after surgery; in patients unable to abruptly discontinue therapy may add full opioid to buprenorphine to maintain proper anesthesia; increased doses my be required to overcome buprenorphine receptor blockade; monitor patients continuously if opioid therapy required as part of anesthesia in an anesthesia care setting

            Abrupt discontinuation following prolonged therapy may lead ot withdrawal symptoms; not recommended; taper gradually

            Use caution in patients who are morbidly obese

            Avoid use in patients with impaired consciousness or coma; patients are susceptible to intracranial effects of CO2 retention

            Use caution in patients with a history of ileus or bowel obstruction; contraindicated in patients with known or suspected GI obstruction including paralytic ileus

            Chronic use of opioids may cause reduced fertility in females and males of reproductive potential; unknown whether effects on fertility are reversible

            Coadministration with benzodiazepines

            • Concomitant use of buprenorphine and benzodiazepines or other CNS depressants increases risk of adverse reactions including overdose and death; medication-assisted treatment of opioid use disorder, should not be categorically denied to patients taking these drugs; prohibiting or creating barriers to treatment can pose an even greater risk of morbidity and mortality due to opioid use disorder alone; educate patients about risks of concomitant use of benzodiazepines, sedatives, opioid analgesics, and alcohol
            • Develop strategies to manage use of prescribed or illicit benzodiazepines or other CNS depressants at initiation of buprenorphine treatment, or if it emerges as a concern during treatment; adjustments to induction procedures and additional monitoring may be required; there is no evidence to support dose limitations or arbitrary caps of buprenorphine as a strategy to address benzodiazepine use in buprenorphine-treated patients; however, if a patient is sedated at the time of buprenorphine dosing, delay or omit the buprenorphine dose if appropriate
            • Cessation of benzodiazepines or other CNS depressants is preferred in most cases of concomitant use; in some cases, monitoring in a higher level of care for taper may be appropriate; in others, gradually tapering a patient off of a prescribed benzodiazepine or other CNS depressant or decreasing to the lowest effective dose may be appropriate
            • For patients in buprenorphine treatment, benzodiazepines are not the treatment of choice for anxiety or insomnia; before co-prescribing benzodiazepines, ensure that patients are appropriately diagnosed and consider alternative medications and non-pharmacologic treatments to address anxiety or insomnia
            • Ensure that other healthcare providers prescribing benzodiazepines or other CNS depressants are aware of the patient’s buprenorphine treatment and coordinate care to minimize the risks associated with concomitant use
            • Take measures to confirm that patients are taking their medications as prescribed and are not diverting or supplementing with illicit drugs; toxicology screening should test for prescribed and illicit benzodiazepines

            Pregnancy & Lactation


            Data in pregnancy are limited; however, these data do not indicate an increased risk of major malformations specifically due to buprenorphine exposure; observational studies have reported on congenital malformations among exposed pregnancies, but were also not designed appropriately to assess risk of congenital malformations specifically due to drug exposure

            Dosage adjustments of buprenorphine may be required during pregnancy, even if patient was maintained on stable dose prior to pregnancy; withdrawal signs and symptoms should be monitored closely and the dose adjusted as necessary

            Fetal/neonatal adverse reactions

            • Neonatal opioid withdrawal syndrome may occur in newborn infants of mothers who are receiving treatment


            Data on two studies in 13 lactating women receiving therapy where the drug and it metabolite were present in low levels in human milk did not show adverse reactions in breastfed infants; developmental and health benefits of breastfeeding should be considered along with mother’s clinical need for therapy and any potential adverse effects on breastfed child from drug or from underlying maternal condition; advise breastfeeding women taking buprenorphine products to monitor infant for increased drowsiness and breathing difficulties

            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.



            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


            Bioavailability: 79%

            Onset: IM, 15 min

            Duration: 4-10 hr

            Peak plasma time: <2 min

            Peak plasma concentration: 18 ng/mL


            Protein bound: 96%

            Vd: 97-187 L/kg


            Liver (N-dealkylation)

            Metabolized in liver via N-dealkylation

            Metabolites: Norbuprenorphine (N-dealkylbuprenorphine)


            Half-life: 2.2 hr

            Excretion: Urine, feces



            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


            Store at 15-30°C; protect from freezing

            Protect from prolonged exposure to light





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            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.