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; may be repeated once (up to 0.3 mg) if required 30-60 minutes after initial dose

Also see Administration

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

  • No differences in pharmacokinetics observed between 9 dialysis-dependent and 6 normal patients following IV administration of 0.3 mg buprenorphine
  • Renal failure: Pharmacokinetics are unknown

Hepatic impairment

  • SL use
    • Mild: No dose adjustment is needed
    • Moderate: No dose adjustment is necessary, closely monitor for signs and symptoms of toxicity or overdose
    • Severe: Reducing starting and titration incremental dose by half, and monitor for signs and symptoms of toxicity or overdose
  • IV/IM use
    • Mild-to-moderate: No dosage adjustments provided
    • Severe: No dosage adjustment provided; use with caution

Dosing Considerations

For prescriber qualifications, see prescribing information

Also given in combination with naloxone

Induction with SL tablets

  • Patients dependent on heroin or other short-acting opioids
    • At initiation, administer first dose of buprenorphine SL tablets only when signs/symptoms of moderate opioid withdrawal appear, and ≥4 hr after patient last used an opioid
    • Titrate to clinical effectiveness achieved as rapidly as possible; dosing on the initial day of treatment may be given in 2-4 mg increments if preferred
  • Patients dependent on methadone or other long-acting opioids
    • Administer first dose of buprenorphine sublingual tablets should when clear signs/symptoms of moderate opioid withdrawal appear, and generally ≥24 hr after the patient last used a long-acting opioids

Access to naloxone for opioid overdose

  • Assess need for naloxone upon initiating and renewing treatment
  • Consider prescribing naloxone
    • Based on patient’s risk factors for overdose (eg, concomitant use of CNS depressants, a history of opioid use disorder, prior opioid overdose); presence of risk factors should not prevent proper pain management
    • Household members (including children) or other close contacts at risk for accidental ingestion or overdose
  • Consult patients and caregivers on the following:
    • Availability of naloxone for emergency treatment of opioid overdose
    • Ways differ on how to obtain naloxone as permitted by individual state dispensing and prescribing requirements or guidelines (eg, by prescription, directly from a pharmacist, as part of a community-based program)

Dosage Forms & Strengths

injectable solution: Schedule III (Buprenex)

  • 0.3mg/mL

Moderate-to-Severe Pain

<2 years: Safety and efficacy not established

2-12 years: 2-6 mcg/kg IV/IM q4-6hr PRN  

>12 years: 0.3 mg IV/IM q6hr; may be repeated once (up to 0.3 mg) if required 30-60 minutes after initial dose

Also see Administration

Moderate-to-Severe Pain

0.15 mg IV/IM q6hr; titrate slowly due to increase risk of respiratory depression



Interaction Checker

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            Adverse Effects

            >10% (SL)

            Headache (29.1-30%)

            Pain (18.4-24%)

            Withdrawal syndrome (18.4-22%)

            Insomnia (21.4%)

            Infection (20%)

            Asthenia (14%)

            Back pain (7.8-14%)

            Nausea (10-13.6%)

            Sweating (12-12.6%)

            Abdominal pain (11.7%)

            Infection (11.7%)

            Constipation (7.8-11%)

            1-10% (IV/IM)


            • Nausea
            • Dizziness/vertigo


            • Sweating
            • Headache
            • Hypotension
            • Nausea/vomiting
            • Hypoventilation
            • Miosis

            1-10% (SL)

            Rhinitis (9.7%)

            Chills (6-7.8%)

            Vomiting (5-7.8%)

            Flu syndrome (6%)

            Nervousness (6%)

            Runny eyes (5%)

            Diarrhea (4.9-5%)

            Asthenia (4.9%)

            Vasodilation (3.9%)

            Fever (3%)

            Dyspepsia (3%)

            Accidental injury (2-3%)

            Abscess (2%)


            Confusion, blurred vision, euphoria, weakness/fatigue, dry mouth, nervousness, depression, slurred speech, paresthesia

            Hypertension, tachycardia, bradycardia


            Dyspnea, cyanosis


            Diplopia, visual abnormalities

            Injection site reaction, urinary retention, dreaming, flushing/warmth, chills/cold, tinnitus, conjunctivitis, Wenckebach block, and psychosis

            Other effects observed infrequently include malaise, hallucinations, depersonalization, coma, dyspepsia, flatulence, apnea, rash, amblyopia, tremor, and pallor

            Postmarketing Reports

            Serotonin syndrome

            Adrenal insufficiency


            Androgen deficiency

            Glossodynia, glossitis, oral mucosal erythema, oral hypoesthesia, and stomatitis



            Black Box Warnings

            Opioid analgesic risk evaluation and mitigation strategy (REMS)

            • To ensure that benefits of opioid analgesics outweigh risks of addiction, abuse, and misuse, the Food and Drug Administration (FDA) has required a REMS for these products; under requirements of the REMS, drug companies with approved opioid analgesic products must make REMS-compliant education programs available to healthcare providers
            • Healthcare providers are strongly encouraged to:
              • Complete a REMS-compliant education program
              • Counsel patients and/or their caregivers, with every prescription, on safe use, serious risks, storage, and disposal of these products
              • Emphasize to patients and their caregivers the importance of reading the Medication Guide every time it is provided by their pharmacist
              • Consider other tools to improve patient, household, and community safety
              • To obtain further information on opioid analgesic REMS and for a list of accredited REMS CME/CE, call 1-800-503-0784, or log on to www.opioidanalgesicrems.com; the FDA Blueprint can be found at www.fda.gov/OpioidAnalgesicREMSBlueprint

            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 use in patients for whom alternative treatment options are inadequate; limit dosages and durations to minimum required; and monitor 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)

            Do not abruptly discontinue buprenorphine in a patient physically dependent on opioids; when discontinuing therapy, in a physically dependent patient, gradually taper the dosage; rapid tapering in a patient physically dependent on opioids may lead to a withdrawal syndrome and return of pain

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

            May impair mental or physical abilities needed to perform potentially hazardous activities (eg, driving a car, operating machinery)

            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

            Opioids can cause sleep-related breathing disorders including central sleep apnea (CSA) and sleep-related hypoxemia; opioid use increases risk of CSA in a dose-dependent fashion; in patients who present with CSA, consider decreasing opioid dosage using best practices for opioid taper

            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

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

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

            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 may be required to overcome buprenorphine receptor blockade; continuously monitor if opioid therapy required as part of anesthesia in an anesthesia care setting

            Abrupt discontinuation following prolonged therapy may lead to 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 (see Pregnancy)

            Patient access to naloxone for emergency treatment of opioid overdose

            • Assess potential need for naloxone; consider prescribing for emergency treatment of opioid overdose
            • Consult on availability and ways to obtain naloxone as permitted by individual state naloxone dispensing and prescribing requirements or guidelines
            • Educate patients regarding the signs and symptoms of respiratory depression and to call 911 or seek immediate emergency medical help in the event of a known or suspected overdose

            Drug interactions overview

            • Concomitant use of buprenorphine and benzodiazepines, a muscle relaxant, or other CNS depressants increases risk of adverse reactions including overdose and death; if an opioid analgesic is initiated in a patient already taking a benzodiazepine or other CNS depressant, prescribe a lower initial dose of the opioid analgesic, and titrate based on clinical response; follow patients closely for signs and symptoms of respiratory depression and sedation; if concomitant use with benzodiazepine ior muscle relaxant s warranted, consider prescribing naloxone for the emergency treatment of opioid overdose (See Black Box Warnings)
            • Opioids may reduce efficacy of diuretics by inducing release of antidiuretic hormone
            • Anticholinergic drugs may increase risk of urinary retention and/or severe constipation, which may lead to paralytic ileus; monitor for signs of urinary retention or reduced gastric motility when buprenorphine is concomitantly used with anticholinergics
            • Serotonergic drugs
              • Opioids may enhance serotonergic effect of drugs (eg, selective serotonin reuptake inhibitors, monoamine oxidase inhibitors) that affect the serotonergic neurotransmitter system; which increases the risk of serotonin syndrome; if concomitant use is warranted, monitor; discontinue if serotonin syndrome is suspected
              • Use of MAOIs with buprenorphine is not recommended during or within 14 days of discontinuing treatment
            • CYP3A4 inhibitors
              • Concomitant use of buprenorphine and CYP3A4 inhibitor may increase the plasma concentration of buprenorphine, resulting increased or prolonged opioid effects; specifically when adding a CYP3A4 inhibitor after achieving a stable buprenorphine dose
            • CYP3A4 inducers
              • Concomitant use of buprenorphine and CYP3A4 inducers may decrease plasma concentration of buprenorphine, potentially resulting in decreased efficacy or onset of a withdrawal syndrome in patients who have developed physical dependence to buprenorphine

            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 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


            Onset: 15 min (IM); ~1 hr (IV)

            Duration: >6 hr (IM)

            Peak plasma time: 1.84 hr (2-mg SL dose); 1.28 hr (8-mg SL dose); 1.42 hr (16-mg SL dose)

            Peak plasma concentration: 1.25 ng/mL (2-mg SL dose); 2.88 ng/mL (8-mg SL dose); 4.7 ng/mL (16-mg SL dose)

            AUC: 10.93 hr·ng/mL (2-mg SL dose); 28.39 hr·ng/mL (8-mg SL dose); 47.09 hr·ng/mL (16-mg SL dose)


            Protein bound: 96%, primarily to alpha and beta globulin


            Buprenorphine undergoes both N-dealkylation to norbuprenorphine and glucuronidation

            N-dealkylation pathway is mediated primarily by CYP3A4

            Metabolites: Norbuprenorphine (N-dealkylbuprenorphine)


            Mean half-life: 2.2 hr (IV); 31-35 hr (SL)

            Excretion: Urine (30%), feces (69%)



            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 or by slow IV injection over ≥2 minutes


            Injection: Store at 20-25°C (68-77°F)

            SL tablets: Store at 20-25°C (68-77°F); excursions permitted between 15-30°C (59-86°F)

            Protect from prolonged exposure to light





            FormularyPatient Discounts

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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.