Names and pronunciation
(byoo-tor′fa-nole)
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Drug reference
(byoo-tor′fa-nole)
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Func. class.: Opioid analgesic
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Chem. class.: Mixed opioid antagonist, partial agonist Controlled Substance Schedule IV
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ACTION: Depresses pain impulse transmission at the spinal cord level by interacting with opioid receptors
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USES: Moderate to severe pain, gen- eral anesthesia induction/maintenance, headache, migraine, preanesthesia
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CONTRAINDICATIONS: Hyper- sensitivity to product, preservative; addiction (opioid) Precautions: Pregnancy, breastfeeding, children <18 yr, addictive personality, increased intracranial pressure, renal/ hepatic disease, ileus, COPD, potential for overdose
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Black Box Warning: Coadministration with other CNS depressants, respiratory depression, accidental exposure (intra- nasal), neonatal opioid withdrawal syn- drome, substance abuse Black Box Warning: Increase: CNS effects—alcohol, benzodiazepines, opi- oids, sedative/hypnotics, antipsychotics, skeletal muscle relaxants, other CNS de- pressants, MAOIs Increase: butorphanol effect—CYP3A4 inhibitors (azoles, macrolides, protease inhibitors), monitor for severe respira- tory depression Increase: serotonin syndrome—SSRIs and other serotonergic agents, monitor for serotonin syndrome Decrease: butorphanol effect—CYP3A4 inducers (carBAMazepine, phenytoin, rifAMPin), dosage increase may be needed Drug/Herb St. John’s wort: Increased serotonin syn- drome risk Black Box Warning: Respiratory dys- function: respiratory depression, char- acter, rate, rhythm; notify prescriber if respirations are <10/min Black Box Warning: Neonatal opioid withdrawal: if mother used this product for prolonged periods during pregnancy, monitor neonate for withdrawal Black Box Warning: Substance abuse: identify if there has been sub- stance abuse (including alcoholism) in the past or present; addiction is more common in these patients Black Box Warning: Accidental expo- sure (intranasal): keep out of reach of children Black Box Warning: Avoid with benzo- diazepines B • Need for pain medication, physical dependence • Safety measures: night-light, call bell within easy reach, assistance with ambu- lation, especially for geriatric patients • Pregnancy/breastfeeding: use only if benefits outweigh risks; usually com- patible with breastfeeding Black Box Warning: To report any symp- toms of CNS changes, if using with other opioids, benzodiazepines, alcohol, or other CNS depressants, to seek medical care immediately for stupor, slow breath- ing, severe sleepiness Black Box Warning: Accidental over- dose: May be fatal, keep out of reach of children • To report all products taken (OTC, Rx, herbs, supplements) • That physical dependency may result when used for extended periods • That withdrawal symptoms may occur: nausea, vomiting, cramps, fever, faint- ness, anorexia • How to use nasal product • To avoid hazardous activities, to have help getting out of bed or walking
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SIDE EFFECTS CNS: Drowsiness, dizziness, confusion, headache, sedation, euphoria, weak- ness, hallucinations, insomnia (nasal) CV: Palpitations, bradycardia, hypotension EENT: Tinnitus, blurred vision, miosis, dip- lopia, nasal congestion, unpleasant taste GI: Nausea, vomiting, anorexia, con- stipation, cramps GU: Urinary retention INTEG: Rash, urticaria, bruising, flush- ing, diaphoresis, pruritus RESP: Respiratory depression
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INTERACTIONS
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TREATMENT OF OVERDOSE: Naloxone 0.4-2 mg IV, IM/SUBCUT/O2, IV fluids, vasopressors
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DOSAGE AND ROUTES Moderate-severe pain • Adult: IM 1-4 mg q3-4hr prn; IV B 0.5-2 mg q3-4hr prn; INTRANASAL 1 spray in 1 nostril, may give another dose 1-1½ hr later; repeat if needed 3-4 hr after last dose • Geriatric: IV ½ adult dose at 2× the interval; INTRANASAL if no relief after 90-120 min, may repeat with 1 spray Anesthesia—maintenance in balanced anesthesia; anesthetic adjunct • Adult: IV Initially, 2 mg shortly before anesthesia induction. Maintenance, 0.5-1 mg IV during anesthesia, up to 0.06 mg/kg; usual total dose, 4-12.5 mg (approximately 0.06 to 0.18 mg/kg) Atrial cardioversion—pain • Adult: INTRANASAL 1 mg 30 min before internal atrial defibrillation shock Renal/hepatic dose • Adult: INTRANASAL max 1 mg followed by 1 mg after 90-120 min; IM/IV give 50% of dose (0.5 mg IV, 1 mg IM), do not repeat within 6 hr
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Available forms: Injection 1, 2 mg/mL; nasal spray 10 mg/mL
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Administer: • With antiemetic if nausea, vomiting occur • When pain is beginning to return; deter- mine dosage interval according to patient response • Store in light-resistant container at room temperature Nasal route • Prime before first use, point sprayer away from the face, pump activator 7× until a fine, wide spray occurs; if not used for 48 hr, reprime by pumping 1-2× • If more than 1 spray is needed, use other nostril • Do not share with others • Nasal congestion/irritation may occur IM route • Deeply in large muscle mass IV direct route • Undiluted at a rate of <2 mg/>3-5 min, titrate to patient response; inject directly in vein or tubing of free-flowing compatible IV infusion Y-site compatibilities: Acyclovir, alfent- anil, allopurinol, amifostine, amikacin, aminocaproic acid, aminophylline, amphotericin B liposome (AmBisome), anidulafungin, ascorbic acid injection, atenolol, atracurium, atropine, aztreo- nam, benztropine, bivalirudin, bleomy- cin, bumetanide, buprenorphine, cal- cium chloride/gluconate, CARBOplatin, caspofungin, cefamandole, ceFAZolin, cefepime, cefotaxime, cefoTEtan, cefOXi- tin, cefTAZidime, ceftizoxime, cefTRIAX- one, cefuroxime, cephalothin, chlor- proMAZINE, cimetidine, cisatracurium, CISplatin, cladribine, clindamycin, cya- nocobalamin, cyclophosphamide, cyclo- SPORINE, cytarabine, DACTINomycin, DAPTOmycin, dexamethasone phos- phate, dexmedetomidine, digoxin, diltia- zem, diphenhydrAMINE, DOBUTamine, DOCEtaxel, DOPamine, doxacurium, DOXOrubicin, DOXOrubicin liposomal, doxycycline, enalaprilat, ePHEDrine, EPI- NEPHrine, epirubicin, epoetin alfa, eptifi- batide, ertapenem, erythromycin, esmo- lol, etoposide, famotidine, fenoldopam, fentaNYL, filgrastim, fluconazole, fludara- bine, fluorouracil, gatifloxacin, gem- citabine, gentamicin, glycopyrrolate, granisetron, heparin, hydrocortisone, hydrOXYzine, IDArubicin, ifosfamide, imipenem-cilastatin, irinotecan, isopro- terenol, ketorolac, labetalol, lactated Ringer’s injection, levofloxacin, lido- caine, linezolid injection, LORazepam, magnesium, mannitol, mechlorethamine, melphalan, meperidine, metaraminol, methicillin, methotrexate, methoxamine, methyldopate, methylPREDNISolone, metoclopramide, metoprolol, metroNI- DAZOLE, mezlocillin, milrinone, minocy- cline, mitoXANtrone, morphine, multiple vitamins injection, mycophenolate mofetil, nafcillin, nalbuphine, naloxone, nesiritide, netilmicin, niCARdipine, nitro- glycerin, nitroprusside, norepinephrine, octreotide, ondansetron, oxacillin, oxaliplatin, oxytocin, palonosetron, pamidronate, pancuronium, papaverine, PEMEtrexed, penicillin G potassium/ sodium, pentazocine, PHENobarbital, phenylephrine, phytonadione, piperacil- lin, piperacillin-tazobactam, polymyxin B, potassium chloride, procainamide, prochlorperazine, promethazine, propo- fol, propranolol, protamine, pyridoxine, quiNIDine, ranitidine, remifentanil, Ring- er’s injection, riTUXimab, rocuronium, sargramostim, sodium acetate, succinyl- choline, SUFentanil, tacrolimus, tenipo- side, theophylline, thiamine, thiotepa, ticarcillin, ticarcillin-clavulanate, tigecy- cline, tirofiban, TNA, tobramycin, tolazo- line, TPN, trastuzumab, urokinase, vancomycin, vasopressin, vecuronium, verapamil, vinCRIStine, vinorelbine, voriconazole
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Assess: • For decreasing output; may indicate urinary retention • For withdrawal symptoms in opioid- dependent patients; PE, vascular occlu- sion, abscesses, ulcerations • CNS changes: dizziness, drowsiness, hal- lucinations, euphoria, LOC, pupil reaction • Allergic reactions: rash, urticaria
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Evaluate: • Therapeutic response: decrease in pain
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CLINICAL CONSIDERATIONS
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Patient and caregiver information:
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PHARMACOKINETICS Metabolized by liver, excreted by kidneys, crosses placenta, excreted in breast milk, half-life 2-9 hr, protein binding 80% IM: Onset 5-15 min, peak 30-60 min, duration 3-4 hr INTRANASAL: Onset within 15 min, peak 1-2 hr, duration 4-5 hr IV: Onset 1 min, peak 4-5 min, duration 2-4 hr
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• Geriatric: IV ½ adult dose at 2× the interval; INTRANASAL if no relief after 90-120 min, may repeat with 1 spray Anesthesia—maintenance in balanced anesthesia; anesthetic adjunct
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