Fentanyl


Concise Prescribing Info
Indications/Uses
Listed in Dosage.
Dosage/Direction for Use
Adult : Buccal Breakthrough cancer pain Patients already receiving and tolerant to opioid treatment: As loz: Initial: 200 mcg over 15 min per episode; may repeat once after 15 min if needed. Max: 1.6 mg/dose. No more than 4 unit doses should be taken daily. As tab: Initial: 100 mcg per episode; may repeat once after 30 min if needed; wait for at least 2 or 4 hr before treating another episode. As film: Initial: 200 mcg per episode; thereafter, at least 2 hr must elapsed before treating another episode. Sublingual Breakthrough cancer pain As tab: Initial: 100 mcg per episode; may repeat once after 30 min if needed; wait for at least 2 or 4 hr before treating another episode. As spray: Initially, 100 mcg per episode; may repeat once after 30 min if needed; wait for at least 4 hr before treating another episode. Nasal Breakthrough cancer pain Initial: Spray 50 or 100 mcg into 1 nostril per episode; may repeat once after 10 min; wait for at least 2 or 4 hr before treating another episode. Max: 4 episodes treated daily. IV Adjunct to general anaesthesia Patients w/ spontaneous respiration: Initial: 50-200 mcg followed by supplements of 50 mcg. Max: 200 mcg. Admin lower infusion rates of 0.05-0.08 mcg /kg/min. Patients w/ assisted ventilation: Initial: 300-3,500 mcg (up to 50 mcg/kg) followed by supplements of 100-200 mcg depending on response. Loading dose (alternatively via bolus): Approx 1 mcg/kg/min given for the 1st 10 min followed by infusion of approx 100 ng/kg/min. IM Premedication before anaesthesia 50-100 mcg to be given 30-60 min prior to induction of anaesth. Transdermal Intractable chronic pain Opioid-naive patients: Initial: Apply patch that delivers ≤25 mcg/hr. Adjust dose according to response. Patients receiving a strong opioid analgesic: Initial dose should be based on the previous 24-hr opioid requirements. Replace patch every 72 hr and apply the new patch to a different site; avoid using the same area of skin for a few days.
Dosage Details
Buccal
Breakthrough cancer pain
Adult: Patients already receiving and tolerant to opioid treatment: As loz: Initially, 200 mcg over 15 min for an episode of breakthrough pain; may repeat once after 15 min if needed. Titrate subsequent doses based on response up to 1.6 mg/dose. Once the effective dose has been identified, no more than 4 unit doses should be taken daily. As tab: Initially, 100 mcg for an episode of breakthrough pain; may repeat once after 30 min if needed; wait for at least 2 or 4 hr before treating another episode. As film: Initially, 200 mcg for an episode of breakthrough pain; thereafter, at least 2 hr must elapsed before treating another episode.
Elderly: Dose reduction may be needed.

Intramuscular
Premedication before anaesthesia
Adult: 50-100 mcg to be given 30-60 min prior to induction of anaesth.
Elderly: Dose reduction may be needed.

Intravenous
Adjunct to general anaesthesia
Adult: Patients w/ spontaneous respiration: Initially, 50-200 mcg followed by supplements of 50 mcg. Max: 200 mcg. Admin infusion rates of 0.05-0.08 mcg/kg/min. Patients w/ assisted ventilation: Initially, 300-3,500 mcg (up to 50 mcg/kg) followed by supplements of 100-200 mcg depending on patient's response. Loading dose (alternatively via bolus): Approx 1 mcg/kg/min given for the 1st 10 min followed by infusion of approx 0.1 mcg/kg/min.
Child: 2-12 yr Initially, 2-3 mcg/kg followed by supplements of 1 mcg/kg.
Elderly: Dose reduction may be needed.

Nasal
Breakthrough cancer pain
Adult: Initially, spray 50 or 100 mcg into 1 nostril for an episode of breakthrough pain; may repeat once after 10 min; wait for at least 2 or 4 hr before treating another episode. Titrate subsequent doses based on response up to max of 4 episodes treated daily.
Elderly: Dose reduction may be needed.

Sublingual
Breakthrough cancer pain
Adult: Tab: Initially, 100 mcg for an episode of breakthrough pain; may repeat once after 30 min if needed; wait for at least 2 or 4 hr before treating another episode. Spray: Initially, 100 mcg for an episode of breakthrough pain; may repeat once after 30 min if needed; wait for at least 4 hr before treating another episode.
Elderly: Dose reduction may be needed.

Transdermal
Intractable chronic pain
Adult: Patches deliver fentanyl in doses that range from: 12-100 mcg/hr. Doses should be individually titrated based on previous use of opioids. Opioid-naive patients: Initially, ≤25 mcg/hr; it is recommended to initially titrate w/ low doses of short-acting opioids before starting fentanyl patches. Patients receiving a strong opioid analgesic: Initial dose should be based on the previous 24-hr opioid requirements. During transfer to fentanyl patches, previous opioid treatment should be phased out gradually. If patient requires doses >100 mcg/hr, >1 patch may be used; consider alternative or additional therapy if doses >300 mcg/hr are required. Replace patch every 72 hr and apply the new patch to a different site; avoid using the same area of skin for a few days.
Elderly: Dose reduction may be needed.
Special Patient Group
Debilitated patients: Dose reduction may be needed.
Incompatibility
Thiopental Na and methohexital Na.
Contraindications
Opioid nontolerant patient. Treatment of acute pain other than breakthrough pain (e.g. migraine or other headaches) or post-op pain; acute or severe resp depression or obstructive lung disease; paralytic ileus.
Special Precautions
Head injury; increased intracranial pressure; renal or hepatic impairment; myasthenia gravis, cardiac bradyarrhythmias, pre-existing pulmonary disease (e.g. COPD) or condition (e.g. hypoxia). Cachetic or debilitated patients. Rapid IV infusion may cause skeletal muscle and chest wall rigidity. Prolonged use may cause tolerance, psychological and physical dependence. Abrupt withdrawal may lead to withdrawal symptoms, gradually taper down the dose to avoid this risk. Elderly. Pregnancy and lactation.
Adverse Reactions
Reduce pulmonary compliance and/or apnoea, bronchoconstriction, laryngospasm; nausea, vomiting; bradycardia, oedema, CNS depression, confusion, dizziness, drowsiness, headache, sedation, hypotension, peripheral vasodilation, increased intracranial pressure, itching, rash, erythema, papules, pruritus, exfoliative dermatitis, pustules, macular rash; gum bleeding and irritation, taste perversion, dental caries, tooth loss, gum line erosion; throat irritation, nasal ulcers, epistaxis, rhinorrhoea; coughing; urinary retention.
Potentially Fatal: Resp depression.
Buccal/Epidural/IM/IV/Nasal/Parenteral/PO/SL/Transdermal: C
MonitoringParameters
Monitor body temp, heart rate, BP, resp & CV status.
Overdosage
Symptoms: Altered mental status, loss of consciousness, hypotension, resp depression, resp distress and resp failure. Management: Immediately remove patch, buccal film or tab followed by naloxone admin. Stimulate patient physically or verbally. Establish and maintain patent airway, if needed.
Drug Interactions
Concomitant use w/ CYP3A4 inhibitors (e.g. erythromycin, clarithromycin, troleandomycin, azole antifungals, ritonavir, amiodarone, nefazodone, aprepitant, diltiazem and verapamil) increases serum levels of fentanyl and may potentiate fatal resp depression. Increased risk of life-threatening serotonins syndrome w/ SSRIs, SNRIs and MAOIs. May reduce serum levels w/ rifamycin derivatives. Enhanced depressant effect w/ general anaesth, tranquilisers, barbiturates and narcotics. May increase excretion w/ ammonium Cl. May increase hypotensive effect w/ phenothiazines. May reduce efficacy of pegvisomant.
Food Interaction
May enhance depressant effect w/ alcohol. Serum levels may be increased by grapefruit juice. May reduce serum levels w/ St John's wort.
Action
Description: Fentanyl is a potent opioid analgesic that increases pain threshold, alters pain reception and inhibits ascending pain pathways by binding to stereospecific receptors w/in the CNS.
Onset: IV: Rapid; IM: Approx 7-15 min; Transdermal (initial placement): 6 hr; Transmucosal: 5-15 min.
Duration: IV: 30-60 min; IM: 1-2 hr; Transdermal (removal of patch/no replacement): 72-96 hr.
Pharmacokinetics:
Absorption: Transmucosal: Rapidly absorbed from buccal and nasal mucosa, the remainder is swallowed and slowly absorbed from the GI tract. Transdermal: Slow absorption after application. Bioavailability: Buccal film: 71%; buccal tab: 65%; lozenge: Approx 50%; sublingual spray: 76%; sublingual tab: 54%. Time to peak plasma concentration: Buccal film: 0.75-4 hr; sublingual spray: 10-120 min; sublingual tab: 15-240 min; transdermal patch: 20-72 hr.
Distribution: Highly lipophilic, distributes rapidly from blood into the lungs and skeletal muscles then into deeper fat compartments. It crosses the placenta, enters the breast milk and appears in the CSF. Volume of distribution: 4-6 L/kg. Plasma protein binding: Approx 80%.
Metabolism: Hepatic via N-dealkylation and hydroxylation by CYP3A4 isoenzyme..
Excretion: Via urine (75%, primarily as metabolites; <7-10% as unchanged drug); faeces (approx 9%). Elimination half-life: IV: 2-4 hr; transdermal patch: 20-27 hr; transmucosal: 3-14 hr (dose-dependent); nasal spray: 15-25 hr.
Storage
Store between 20-25°C. Protect from light.
References
Anon. Fentanyl. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 18/11/2013.

Buckingham R (ed). Fentanyl. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 18/11/2013.

Joint Formulary Committee. Fentanyl. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 18/11/2013.

McEvoy GK, Snow EK, Miller J et al (eds). Fentanyl, Fentanyl Citrate, Fentanyl Hydrochloride. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 18/11/2013.

Sublimaze Inj (Taylor Pharmaceuticals). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 18/11/2013.

Sublimaze TM: Introduction of New Warning - Serotonin syndrome may occur with co-administration with serotonergic drugs. MHRA. https://products.mhra.gov.uk/. Accessed 18/11/2013.

Disclaimer: This information is independently developed by MIMS based on Fentanyl from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
  • Fentanyl Janssen-Cilag
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