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Pregnancy Category: C
Pharmacologic: opioid agonists antagonists
ClassificationTherapeutic: opioid analgesics
Pharmacologic: opioid agonists antagonists
Intramuscular: Intravenous: Management of moderate to severe acute pain. Transdermal: Management of moderate to severe chronic pain in patients requiring use of a continuous around-the-clock opioid analgesic for an extended period of time. Sublingual: Treatment of opioid dependence; suppresses withdrawal symptoms in opioid detoxification.
Binds to opiate receptors in the CNS.
Alters the perception of and response to painful stimuli while producing generalized CNS depression.
Has partial antagonist properties that may result in opioid withdrawal in physically dependent patients when used as an analgesic.
Intramuscular: Intravenous: Transdermal: Decreased severity of pain.
Sublingual: Suppression of withdrawal symptoms during detoxification and maintenance from heroin or other opioids. Produces a relatively mild withdrawal compared to other agents.
Absorption: Well absorbed after IM and SL use; 15% of transdermal dose absorbed through skin; IV administration results in complete bioavailability.
Distribution: Crosses the placenta; enters breast milk. CNS concentration is 15–25% of plasma.
Protein Binding: 96%.
Metabolism and 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: 2–3 hr (parenteral); 26 hr (transdermal).
Time/action profile (analgesia)
|IM||15 min||60 min||6 hr†|
|IV||rapid||less than 60 min||6 hr†|
Contraindicated in: Hypersensitivity;Significant respiratory depression (transdermal);Acute or severe bronchial asthma (transdermal);Paralytic ileus (transdermal);Acute, mild, intermittent, or postoperative pain (transdermal);Long QT syndrome (transdermal);Concurrent use of class I or III antiarrhythmics (transdermal); Lactation: Enters breast milk; avoid use or discontinue nursing.
Use Cautiously in: ↑ intracranial pressure;Severe renal, hepatic, or pulmonary disease;Hypothyroidism;Seizure disorders;Adrenal insufficiency;Alcoholism;Biliary tract disease;Acute pancreatitis;Debilitated patients (dose ↓ required);Undiagnosed abdominal pain;Prostatic hyperplasia; Obstetric: Safety not established; neonatal withdrawal may occur in infants born to patients receiving SL buprenorphine during pregnancy; Pediatric: Safety not established in children (sublingual and transdermal) or children <2 yr (parenteral); Geriatric: Dose ↓ required.
Adverse Reactions/Side Effects
Central nervous system
- confusion (most frequent)
- dysphoria (most frequent)
- hallucinations (most frequent)
- sedation (most frequent)
- floating feeling
- unusual dreams
Ear, Eye, Nose, Throat
- blurred vision
- miosis (high doses)
- respiratory depression
- QT interval prolongation (transdermal)
- hepatotoxicity (life-threatening)
- nausea (most frequent)
- dry mouth
- urinary retention
- sweating (most frequent)
- clammy feeling
- anaphylaxis (life-threatening)
- physical dependence
- psychological dependence
Drug-Drug interactionUse of high-dose transdermal buprenorphine with class I antiarrhythmics or class I antiarrhythmics may ↑ risk of QT interval prolongation; avoid concurrent use.Use with extreme caution in patients receiving MAO inhibitors (↑ CNS and respiratory depression and hypotension—↓ buprenorphine dose by 50%; may need to ↓ MAO inhibitor dose; do not use transdermal formulation within 14 days of MAO inhibitor ).↑ CNS depression with alcohol, antihistamines, antidepressants, and sedative/hypnotics.May ↓ effectiveness of other opioid analgesics.Inhibitors of the CYP3A4 enzyme system including itraconazole, ketoconazole, erythromycin, ritonavir, indinavir, saquinavir, atazanavir, or fosamprenavir may ↑ blood levels and effects; may need to ↓ buprenorphine dose.Inducers of the CYP3A4 enzyme system including carbamazepine, rifampin, or phenytoin may ↓ blood levels and effects; buprenorphine dose modification may be necessary during concurrent use.Concurrent abuse of buprenorphine and benzodiazepines may result in coma and death.Concomitant use of kava-kava, valerian, chamomile, or hops can ↑ CNS depression.
Intramuscular Intravenous (Adults) 0.3 mg q 4–6 hr as needed. May repeat initial dose after 30 min (up to 0.3 mg q 4 hr or 0.6 mg q 6 hr); 0.6-mg doses should be given only IM.
Intramuscular Intravenous (Children 2–12 yr) 2–6 mcg (0.002–0.006 mg)/kg q 4–6 hr.
Transdermal (Adults) Opioid-naive-Transdermal system delivering 5–20 mcg/hr applied every 7 days. Initiate with 5 mcg/hr system; each dose titration may occur after 72 hr; do not exceed dose of 20 mcg/hr (due to ↑ risk of QT interval prolongation); Previously taking <30 mg/day of morphine or equivalent-Initiate with 5 mcg/hr system; each dose titration may occur after 72 hr; do not exceed dose of 20 mcg/hr (due to ↑ risk of QT interval prolongation); apply patch every 7 days; Previously taking 30–80 mg/day of morphine or equivalent-Initiate with 10 mcg/hr system; each dose titration may occur after 72 hr; do not exceed dose of 20 mcg/hr (due to ↑ risk of QT interval prolongation); apply patch every 7 days; Previously taking >80 mg/day of morphine or equivalent—Consider use of alternate analgesic.
Hepatic ImpairmentTransdermal (Adults) Mild to moderate hepatic impairment-Initiate with 5 mcg/hr system.
Treatment of opioid dependence
Sublingual (Adults) 12–16 mg/day as a single dose.
Availability (generic available)
Sublingual tablets (Subutex): 2 mg, 8 mgIn combination with: naloxone (Suboxone). See combination drugs.
Injection (Buprenex): 300 mcg (0.3 mg)/mL
Transdermal system (Butrans): 5 mcg/hr, 10 mcg/hr, 15 mcg/hr, 20 mcg/hr
- Pain: Assess type, location, and intensity of pain before and 1 hr after IM and 5 min (peak) after IV administration. When titrating opioid doses, increases of 25–50% should be administered until there is either a 50% reduction in the patient’s pain rating on a numerical or visual analogue scale or the patient reports satisfactory pain relief. A repeat dose can be safely administered at the time of the peak if previous dose is ineffective and side effects are minimal. Single doses of 600 mcg (0.6 mg) should be administered IM. Patients requiring doses higher than 600 mcg (0.6 mg) should be converted to an opioid agonist. Buprenorphine is not recommended for prolonged use (except transdermal) or as first-line therapy for acute or cancer pain.
- An equianalgesic chart (see ) should be used when changing routes or when changing from one opioid to another.
- Assess level of consciousness, BP, pulse, and respirations before and periodically during administration. If respiratory rate is <10/min, assess level of sedation. Dose may need to be decreased by 25–50%. Buprenorphine 0.3–0.4 mg has approximately equal analgesic and respiratory depressant effects to morphine 10 mg.
- Assess previous analgesic history. Antagonistic properties may induce withdrawal symptoms (vomiting, restlessness, abdominal cramps, increased BP and temperature) in patients who are physically dependent on opioid agonists. Symptoms may occur up to 15 days after discontinuation and persist for 1–2 wk.
- Buprenorphine has a lower potential for dependence than other opioids; however, prolonged use may lead to physical and psychological dependence and tolerance. This should not prevent patient from receiving adequate analgesia. Most patients receiving buprenorphine for pain do not develop psychological dependence. If tolerance develops, changing to an opioid agonist may be required to relieve pain.
- Assess bowel function routinely. Prevent constipation with increased intake of fluids and bulk, and laxatives to minimize constipating effects. Administer stimulant laxatives routinely if opioid use exceeds 2–3 days, unless contraindicated.
- Transdermal: Maintain frequent contact during periods of changing analgesic requirements, including initial titration, between the prescriber, other members of the healthcare team, the patient, and the caregiver/family.
- Treatment of Opioid Dependence: Assess patient for signs and symptoms of opioid withdrawal before and during therapy.
- Lab Test Considerations: May cause ↑ serum amylase and lipase levels.
If an opioid antagonist is required to reverse respiratory depression or coma, naloxone (Narcan) is the antidote. Dilute the 0.4-mg ampule of naloxone in 10 mL of 0.9% NaCl and administer 0.5 mL (0.02 mg) by direct IV push every 2 min. For children and patients weighing <40 kg, dilute 0.1 mg of naloxone in 10 mL of 0.9% NaCl for a concentration of 10 mcg/mL and administer 0.5 mcg/kg every 1–2 min. Titrate dose to avoid withdrawal, seizures, and severe pain. Naloxone may not completely reverse respiratory depressant effects of buprenorphine; may require mechanical ventilation, oxygen, IV fluids, and vasopressors.
- Monitor liver function tests prior to and periodically during therapy for opioid dependence.
Potential Nursing DiagnosesAcute pain (Indications)
Risk for injury (Side Effects)
Ineffective coping (Indications)
- high alert: Accidental overdose of opioid analgesics has resulted in fatalities. Before administering, clarify all ambiguous orders; have second practitioner independently check original order, dose calculations, route of administration, and infusion pump programming.
- Pain: Explain therapeutic value of medication before administration to enhance the analgesic effect.
- Regularly administered doses may be more effective than prn administration. Analgesic is more effective if given before pain becomes severe.
- Coadministration with nonopioid analgesics has additive effects and may permit lower opioid doses.
- Sublingual: Administer sublingually. Usually takes 2–10 min for tablets to dissolve. If more than one tablet is prescribed, place multiple tablets under the tongue or 2 at a time until all tablets are dissolved. Do not chew or swallow; decreases amount of medication absorbed.
- Intramuscular: Administer IM injections deep into well-developed muscle. Rotate sites of injections.
- pH: 4.0–6.0.
- May give IV undiluted. high alert: Administer slowly. Rapid administration may cause respiratory depression, hypotension, and cardiac arrest.
- Rate: Give over at least 2 minutes
- Y-Site Compatibility: acetaminophen, acyclovir, alfentanil, allopurinol, amifostine, amikacin, aminocaproic acid, amphotericin B lipid complex, amphotericin B liposome, anidulafungin, argatroban, ascorbic acid, atracurium, atropine, azithromycin, aztreonam, benztropine, bivalirudin, bleomycin, bumetanide, butorphanol, calcium chloride, calcium gluconate, carboplatin, carmustine, cefazolin, cefepime, cefoperazone, ceftaxime, cefotetan, cefoxitin, ceftazidime, ceftriaxome, cefuroxime, chloramphenicol, chlorpromazine, cisatracurium, cisplatin, cladribine, clindamycin, cyanocobalamin, cyclophosphamide, cyclosporine, cytarabine, dactinomycin, daptomycin, dexamethasone, dexmedetomidine, dexrazoxane, digoxin, diltiazem, diphenhydramine, dobutamine, docetaxel, dolasetron, dopamine, doxacurium, doxorubicin, doxycycline, enalaprilat, ephedrine, epinephrine, epirubicin, epoetin alfa, eptifibatide, ertapenem, erythromycin, esmolol, etoposide, etoposide phosphate, famotidine, fenoldopam, fentanyl, filgrastim, fluconazole, fludarabine, foscarnet, gemcitabine, gentamicin, glycopyrrolate, granisetron, heparin, hetastarch, hydrocortisone, idarubicin, ifosfamide, imipenem/cilastatin, insulin, irinotecan, isoproterenol, ketorolac, labetalol, leucovorin, levofloxacin, lidocaine, linezolid, lorazepam, magnesium sulfate, mannitol, mechlorethamine, melphalan, meperidine, metaraminol, methotrexate, methyldopate, methylprednisolone, metoclopramide, metoprolol, metronidazole, midazolam, milrinone, mitoxantrone, morphine, multivitamins, mycophenolate, nafcillin, nalbuphine, naloxone, nesiritide, nicardipine, nitroglycerine, nitroprusside, norepinephrine, octreotide, ondansetron, oxacillin, oxaliplatin, oxytocin, paclitaxel, palonosetron, pamidronate, pancuronium, papaverine, pemetrexed, penicillin G, pentamidine, pentazocine, phentolamine, phenylephrine, phytonadione, piperacillin/tazobactam, potassium acetate, potassium chloride, procainamide, prochlorperazine, promethazine, propofol, propranolol, protamine, pyridoxime, quinupristin/dalfopristin, ranitidine, remifentanil, rituximab, rocuronium, sodium acetate, streptokinase, succinylcholine, sufentanil, tacrolimus, teniposide, theophylline, thiamine, thiotepa, ticarcillin/clavulanate, tigecycline, tirofiban, tobramycin, tolazoline, trastuzumab, vancomycin, vasopressin, vecuronium, verapamil, vinblastine, vincristine, vinorelbine, voriconazole, zoledronic acid
- Y-Site Incompatibility: alemtuzumab, aminophylline, amphotericin B cholesteryl, ampicillin, azathioprine, dantrolene, diazepam, diazoxide, doxorubicin liposome, fluorouracil, indomethacin, pantoprazole, pentobarbital, phenobarbital, phenytoin, sodium bicarbonate, trimethoprim/sulfamethoxazole
- Solution Compatibility: 0.9% NaCl, D5W, D5/0.9% NaCl, lactated Ringer’s injection, Ringer’s injection
- Transdermal: Buprenorphine may cause withdrawal in patients who are already taking opioids. For conversion from other opioids to buprenorphine transdermal, taper current around-the-clock opioids for up to 7 days to no more than 30 mg of morphine or equivalent per day before beginning treatment with buprenorphine transdermal. May use short-acting analgesics as needed until analgesic efficacy with buprenorphine transdermal is attained. Buprenorphine transdermal may not provide adequate analgesia for patients requiring greater than 80 mg/day oral morphine equivalents.
- Apply system to flat, nonirritated, and nonirradiated site on the upper outer arm, upper chest, upper back or the side of the chest. If skin preparation is necessary, use clear water and clip, do not shave, hair. Allow skin to dry completely before application. Apply immediately after removing from package. Do not alter the system (i.e., cut) in any way before application. Remove liner from adhesive layer and press firmly in place with palm of hand for 30 sec, especially around the edges, to make sure contact is complete. Remove used system and fold so that adhesive edges are together. Flush system down toilet immediately on removal or follow the institutional policy. Apply new system to a different site. After removal, wait a minimum of 3 weeks before applying to the same site.
- To discontinue, taper dose gradually to prevent signs and symptoms of withdrawal; consider introduction of immediate-release opioid medication.
- Treatment of Opioid Dependence: Must be prescribed by health care professional with special training. Induction is usually started with buprenorphine (Subutex) over 3–4 days. Initial dose should be administered at least 4 hr after last opioid dose and preferably when early signs of opioid withdrawal appear. Once patient is on a stable dose, maintenance therapy with buprenorphine/naloxone (Suboxone) is preferred for continued, unsupervised treatment.
- Medication may cause drowsiness or dizziness. Advise patient to call for assistance when ambulating and to avoid driving or other activities requiring alertness until response to medication is known.
- Advise patient to avoid concurrent use of alcohol or other CNS depressants.
- Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult health care professional before taking any OTC medications concurrently with this therapy.
- Advise patient to notify health care professional if pregnancy is planned or suspected, or if breast feeding.
- Pain: Instruct patient on how and when to ask for pain medication.
- Encourage patients on bedrest to turn, cough, and deep-breathe every 2 hr to prevent atelectasis.
- Instruct patient to change positions slowly to minimize orthostatic hypotension.
- Advise patient that good oral hygiene, frequent mouth rinses, and sugarless gum or candy may decrease dry mouth.
- Transdermal: Instruct patient in correct method for application, removal, storage, and disposal of transdermal system. Wear patches for 7 days. May be worn while bathing, showering, or swimming. Do not discontinue or change dose without consulting health care professional. Instruct patient to read the Medication Guide prior to starting and with each Rx refill.
- Advise patients and caregivers/family members of the potential side effects. Instruct patient to notify health care professional if pain is not controlled or if bothersome side effects occur. Contact immediately if difficulty or changes in breathing, unusual deep "sighing" breathing slow or shallow breathing, new or unusual snoring, slow heartbeat, severe sleepiness, cold, clammy skin, feeling faint, dizzy, confused, or cannot think, walk, or talk normally, or if swelling or blistering around patch occurs.
- Advise patient that fever, electric blankets, heating pads, saunas, hot tubs, and heated water beds increase the release of buprenorphine from the patch.
- Advise patient referred for MRI test to discuss patch with referring health care professional and MRI facility to determine if removal of patch is necessary prior to test and for directions for replacing patch.
- Opioid Dependence: Instruct patient in the correct use of medication; directions for use must be followed exactly. Medication must be used regularly, not occasionally. Take missed doses as soon as remembered; if almost time for next dose, skip missed dose and return to regular dosing schedule. Do not take 2 doses at once unless directed by health care professional. Do not discontinue use without consulting health care professional; abrupt discontinuation may cause withdrawal symptoms. If medication is discontinued, flush unused tablets down the toilet.
- Caution patient that buprenorphine may be a target for people who abuse drugs; store medications in a safe place to protect them from theft. Selling or giving this medication to others is against the law.
- Caution patient that injection of Suboxone can lead to severe withdrawal symptoms.
- Advise patient if admitted to the emergency room to inform treating physician and emergency room staff of physical dependence on opioids and of treatment regimen.
- Advise patient to notify health care professional promptly if faintness, dizziness, confusion, slowed breathing, skin or whites of eyes turn yellow, urine turns dark, light-colored stools, decreased appetite, nausea, or abdominal pain occur.
- Decrease in severity of pain without a significant alteration in level of consciousness or respiratory status.
- Suppression of withdrawal symptoms during detoxification and maintenance from heroin or other opioids.
Drug Guide, © 2015 Farlex and Partners
A trademark for a transdermal formulation of the drug buprenorphine.
The American Heritage® Medical Dictionary Copyright © 2007, 2004 by Houghton Mifflin Company. Published by Houghton Mifflin Company. All rights reserved.