Names and pronunciation
Abstral
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Drug reference
Abstral
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Func. class.: Opioid analgesic
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Chem. class.: Synthetic phenylpi- peridine Controlled Substance Schedule II
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Do not confuse: fentaNYL/sufentanil
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ACTION: Inhibits ascending pain pathways in CNS, increases pain thresh- old, alters pain perception by binding to opiate receptors
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USES: Controls moderate to severe pain; preoperatively, postoperatively; adjunct to general anesthetic, adjunct to regional anesthesia; fentaNYL: anesthesia as premedication, conscious sedation; Actiq: breakthrough cancer pain
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CONTRAINDICATIONS: Hyper- sensitivity to opiates; myasthenia gravis
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Black Box Warning: Headache, migraine (Actiq, ABSTRAL, Fentora, Lazanda); emer- gency room use (ABSTRAL, Lazanda); out- patient surgeries (Duragesic TD); opioid- naive patients, respiratory depression Precautions: Pregnancy, breastfeeding, geriatric patients, increased intracranial pressure, seizure disorders, severe respi- ratory disorders, cardiac dysrhythmias Black Box Warning: Accidental expo- sure, ambient temperature increase, fe- ver, skin abrasion (TD patch), substance abuse, surgery, requires an experienced clinician Black Box Warning: Increase: fen- taNYL effect, fetal respiratory depres- sion: CYP3A4 inhibitors (cycloSPORINE, ketoconazole, itraconazole, cimetidine, conivaptan, fluconazole, nefazodone, ranolazine), zafirlukast, zileuton Increase: fatal reactions—MAOIs Increase: hypotension—droperidol Increase: CV depression—diazepam Increase: fentaNYL effect with other CNS depressants—alcohol, opioids, sedative/ hypnotics, antipsychotics, skeletal mus- cle relaxants, protease inhibitors Decrease: fentaNYL effect—CYP3A4 inducers (carBAMazepine, phenytoin, PHENobarbital, rifampin) Drug/Herb Increase: action of fentaNYL—St. John’s wort Decrease: effect of fentaNYL—echinacea Drug/Lab Test Increase: amylase, lipase Black Box Warning: Respiratory dys- function: respiratory depression, char- acter, rate, rhythm; notify prescriber if respirations are <10/min Black Box Warning: Headache/migraine: Actiq, Fentora, Lazanda not to be used for this condition; Lazanda not to be used in ER; Duragesic TD not to be used for out- patient surgery patients Black Box Warning: Apnea, respiratory arrest in opioid-naive patients: do not use Actiq, Duragesic, Fentora, Lazanda; opioid-tolerant patients are those using ≥60 mg/day oral morphine, ≥30 mg/day oxyCODONE PO, 8 mg/day HYDROmor- phone, 25 mcg TD fentaNYL/hr Black Box Warning: Pregnancy/breast- feeding: no well-controlled studies; use only if benefits outweigh fetal risk; if used for prolonged periods, neonatal with- drawal syndrome may occur; discontinue breastfeeding or product, excreted in breast milk • Beers: avoid in older adults unless safer alternative is unavailable; may cause ataxia, impaired psychomotor function Black Box Warning: Accidental expo- sure: discuss the danger of children or pets ingesting or coming in contact with product; there are increasing numbers of fatal overdose with drugs laced with fen- tanyl, tests are available to identify illicit drugs for the presence of fentanyl Transdermal route Black Box Warning: Ambient tempera- ture: that excessive heat may increase absorption; do not use with heating pads, electric blankets, heat/tanning lamps, saunas, hot tubs, heated waterbeds, when sunbathing, never cut patch in half • That excessive perspiration may alter adhesiveness • To dispose of patch by placing sticky sides together and flushing down toilet • That patient may need to clip hair be- fore applying to ensure adhesion • May add first aid tape around the edges if there is a problem with adhesion, always remove old patch before applying new patch
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SIDE EFFECTS CNS: Dizziness, delirium, euphoria, sedation, confusion, weakness, dizziness, seizures CV: Bradycardia, arrest, hypo/hyperten- sion, DVT, PE EENT: Blurred vision, miosis GI: Nausea, vomiting, constipation GU: Urinary retention INTEG: Rash, diaphoresis MS: Muscle rigidity RESP: Respiratory depression, arrest, laryngospasm
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INTERACTIONS
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DOSAGE AND ROUTES FentaNYL (parenteral) Anesthetic (adjunct to regional anesthesia) • Adult: IV 50-100 mcg/kg over 1-2 min Anesthesia supplement to general anesthesia • Adult/child >12 yr: IM/IV (low dose) 1-2 mcg/kg; IV (moderate dose) 2-20 mcg/kg; IM/IV (high dose) 20-50 mcg/kg, then 25 mcg to y2 initial loading dose as needed Induction and maintenance • Child 2-12 yr: IV 2-3 mcg/kg q1-2hr as needed Preoperatively • Adult/child >12 yr: IM/IV 50-100 mcg q30-60min before surgery Postoperatively • Adult/child >12 yr: IM/IV 50-100 mcg q1-2hr prn Moderate/severe pain • Adult: IV/IM 50-100 mcg q1-2hr; na- sal; 100 mcg spray in one nostril, titrate stepwise Actiq • Adult: TRANSMUCOSAL 200 mcg; re- dose if needed 15 min after completion of 1st dose; do not give more than 2 doses during titration period, max 4 doses/day Fentora • Adult: BUCCAL/SL 100 mcg placed above rear molar between upper cheek and gum; a second 100 mcg dose, if needed, may be started 30 min after 1st dose FentaNYL transdermal • Adult: Duragesic: 25 mcg/hr; may in- crease until pain relief occurs; apply patch to flat surface on upper torso and wear for 72 hr; apply new patch on different site; may use 12.5 mcg/hr if <60 mg/day mor- phine equivalent FentaNYL nasal spray • Adult: 100 mcg (1 spray in 1 nostril), may retreat after ≥2 hr, titrate upward until adequate analgesia; treat a max of 4 episodes daily FentaNYL SL spray • Adult: 100 mcg sprayed under tongue, titrate stepwise carefully
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Available forms: Inj 0.05 mg/mL; loz- enges 100, 200, 300, 400, 600, 800, 1200, 1600 mcg; lozenges on a stick 200, 400, 600, 800, 1200, 1600 mcg; buccal tab 100, 200, 400, 600, 800 mcg; trans- dermal: patch 12, 25, 50, 75, 100 mcg/ hr; SL spray 100, 200, 400, 600, 800, 1200, 1600 mcg/spray; nasal spray 100, 400 mcg/actuation
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Administer: • By inj (IM, IV); give slowly to prevent rigidity • Overdose has been fatal when confusing products/dose; recheck both before using • Must have emergency equipment avail- able, opioid antagonists, O2; to be used only by those appropriately trained; IV products to be used in OR, ER, ICU Transmucosal route • Remove foil just before administration; instruct patient to place product between cheek and lower gum, moving it back and forth and sucking, not chewing (Ac- tiq); place above rear molar (Fentora); place film on the inside of the cheek; all products not used or only partially used should be flushed down the toilet; this product may be used SL Transdermal route • q72hr for continuous pain relief; dos- age adjusted after at least 2 applications; apply to clean, dry skin and press firmly • Give short-acting analgesics until patch takes effect (8-24 hr); when reducing dosage or switching to alternative IV treatment, withdraw gradually; serum levels drop gradually, give 1⁄2 the equian- algesic dose of new analgesic 12-18 hr after removal as ordered IV route • IV undiluted by anesthesiologist or di- luted with 5 mL or more sterile water or 0.9% NaCl given through Y-tube or 3-way stopcock at 0.1 mg or less/1-2 min. Muscular rigidity may occur with rapid IV administration Y-site compatibilities: Abciximab, acyclovir, alfentanil, alemtuzumab alprostadil, amika- cin, aminocaproic acid, aminophylline, amiodarone, amphotericin B cholesteryl, amphotericin B lipid complex, amphotericin B liposome, anidulafungin, argatroban, ascorbic acid injection, atenolol, atracurium, atropine, azaTHIOprine, aztreonam, benz- tropine, bivalirudin, bleomycin, bumetanide, buprenorphine, butorphanol, calcium chloride/gluconate, CARBOplatin, caspo- fungin, ceFAZolin, cefmetazole, cefonicid, cefotaxime, cefoTEtan, cefOXitin, cefTAZi- dime, ceftizoxime, ceftobiprole, cefTRIAX- one, cefuroxime, cephalothin, chloramphenicol, chlorproMAZINE, cimeti- dine, cisatracurium, CISplatin, clindamy- cin, cloNIDine, cyanocobalamin, cyclophosphamide, cycloSPORINE, cytara- bine, DACTINomycin, DAPTOmycin, dexamethasone, dexmedetomidine, digox- in, diltiazem, diphenhydrAMINE, DOBUTa- mine, DOCEtaxel, DOPamine, doripenem, doxacurium, doxapram, DOXOrubicin, doxycycline, enalaprilat, ePHEDrine, EPI- NEPHrine, epirubicin, epoetin alfa, eptifiba- tide, erythromycin, esmolol, etomidate, etoposide, famotidine, fenoldopam, flu conazole, fludarabine, fluorouracil, folic acid, furosemide, ganciclovir, gatifloxacin, gemcitabine, gentamicin, glycopyrrolate, granisetron, heparin, hydrocortisone, HYDROmorphone, hydrOXYzine, IDA rubicin, ifosfamide, imipenem-cilastatin, inamrinone, insulin (regular), irinotecan, isoproterenol, ketorolac, labetalol, lanso- prazole, levofloxacin, lidocaine, linezolid, LORazepam, LR, magnesium sulfate, manni- tol, mechlorethamine, meperidine, meta- raminol, methicillin, methotrexate, methotrimeprazine, methoxamine, methyl- dopate, methylPREDNISolone, metoclo- pramide, metoprolol, metroNIDAZOLE, mezlocillin, miconazole, midazolam, milri- none, minocycline, mitoXANtrone, mivacu- rium, morphine, moxalactam, multiple vitamins injection, mycophenolate, nafcillin, nalbuphine, naloxone, nesiritide, netilmicin, niCARdipine, nitroglycerin, nitroprusside, norepinephrine, octreotide, ondansetron, oxacillin, oxaliplatin, oxytocin, PACLitaxel, palonosetron, pamidronate, pancuroni- F um, papaverine, PEMEtrexed, penicillin G potassium/sodium, pentamidine, pentazo- cine, PENTobarbital, PHENobarbital, phen- ylephrine, phytonadione, piperacillin, piperacillin-tazobactam, polymyxin B, potassium chloride, procainamide, pro- chlorperazine, promethazine, propofol, propranolol, protamine, pyridoxine, quiN- IDine, quinupristin-dalfopristin, ranitidine, remifentanil, Ringer’s, ritodrine, riTUXimab, rocuronium, sargramostim, scopolamine, sodium acetate/bicarbonate, succinylcho- line, SUFentanil, tacrolimus, teniposide, the- ophylline, thiamine, thiopental, thiotepa, ticarcillin, ticarcillin-clavulanate, tigecycline, tirofiban, TNA, tobramycin, tolazoline, TPN, trastuzumab, trimetaphan, urokinase, vancomycin, vasopressin, vecuronium, verapamil, vinCRIStine, vinorelbine, vitamin B complex/C, voriconazole, zoledronic acid
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Assess: • VS after parenteral route; note muscle rigidity, drug history, hepatic/renal func- tion tests • CNS changes: dizziness, drowsiness, hallucinations, euphoria, LOC, pupil re- action • Allergic reactions: rash, urticaria
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Evaluate: • Therapeutic response: induction of an- esthesia, relief of breakthrough cancer pain, general pain relief
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • About CNS changes: physical depen- dence; not to use with alcohol, other CNS depressants
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PHARMACOKINETICS Metabolized by liver, excreted by kidneys, crosses placenta, excreted in breast milk; half-life: IV, 2-4 hr; transdermal, 13-22 hr; transmucosal, 7 hr; buccal, 4-12 hr; 80% bound to plasma proteins IM: Onset 7-15 min, peak 30 min, dura- tion 1-2 hr IV: Onset 1 min, peak 3-5 min, duration 1⁄2-1 hr Intranasal: Onset 15-20 min, peak 25-30 min Transdermal: Onset 12-24 hr, peak 1-3 days Transmucosal: Onset 5-15 min, peak 30 min
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• Adult: IV 50-100 mcg/kg over 1-2 min Anesthesia supplement to general anesthesia
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• Adult/child >12 yr: IM/IV (low dose) 1-2 mcg/kg; IV (moderate dose) 2-20 mcg/kg; IM/IV (high dose) 20-50 mcg/kg, then 25 mcg to y2 initial loading dose as needed Induction and maintenance
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• Child 2-12 yr: IV 2-3 mcg/kg q1-2hr as needed Preoperatively
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• Adult/child >12 yr: IM/IV 50-100 mcg q30-60min before surgery Postoperatively
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• Adult/child >12 yr: IM/IV 50-100 mcg q1-2hr prn Moderate/severe pain
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• Adult: IV/IM 50-100 mcg q1-2hr; na- sal; 100 mcg spray in one nostril, titrate stepwise Actiq
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• Adult: TRANSMUCOSAL 200 mcg; re- dose if needed 15 min after completion of 1st dose; do not give more than 2 doses during titration period, max 4 doses/day Fentora
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• Adult: BUCCAL/SL 100 mcg placed above rear molar between upper cheek and gum; a second 100 mcg dose, if needed, may be started 30 min after 1st dose FentaNYL transdermal
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• Adult: Duragesic: 25 mcg/hr; may in- crease until pain relief occurs; apply patch to flat surface on upper torso and wear for 72 hr; apply new patch on different site; may use 12.5 mcg/hr if <60 mg/day mor- phine equivalent FentaNYL nasal spray
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• Adult: 100 mcg (1 spray in 1 nostril), may retreat after ≥2 hr, titrate upward until adequate analgesia; treat a max of 4 episodes daily FentaNYL SL spray
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• Adult: 100 mcg sprayed under tongue, titrate stepwise carefully
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