Description

Simple

A strong painkiller used for anesthesia, as well as the treatment of cancer pain and constant pain management.

Clinical

An opioid analgesic used in anesthesia, for breakthrough cancer pain, or round the clock pain management.

Overview

Fentanyl, a potent opioid agonist, was developed in the 1950s to fill a need for strong and rapid analgesia.[8] Because of these characteristics, fentanyl is commonly used to treat chronic cancer pain or in anesthesia.[Label,15,16,17,18,19,20,21] Fentanyl is related to other opioids like [morphine] and [oxycodone].

Fentanyl's high potency has also made it... Read more

Pharmacology

Indication

Fentanyl intravenous or intramuscular injections are indicated for short term analgesia during induction, maintenance, and recovery from general or regional anesthesia.[Label] These injections are also used with a neuroleptic for premedication, induction, and as an adjunct to maintenance of anesthes... Read more

Pharmacodynamic

Fentanyl produces strong analgesia through its activation of opioid receptors.[Label, Read more

Mechanism of action

Fentanyl binds to opioid receptors, especially the mu opioid receptor, which are coupled to G-proteins.[ Read more

Absorption

Fentanyl sublingual tablets are 54% bioavailable[15], transmucosal lozenges are 50% bioavailable[ Read more

Protein binding

Fentanyl is 80-85% bound to plasma proteins.[15,16, Read more

Volume of distribution

The intravenous volume of distribution is 4L/kg (3-8L/kg)[Label,19]. The oral volume of distribution is 25.4L/kg.[ Read more

Clearance

Total plasma clearance of fentanyl is 0.5L/hr/kg (0.3-0.7L/hr/kg)[16] or 42L/hr.[ Read more

Half life

The half life of fentanyl is 7 hours.[16] The half life of fentanyl sublingual spray is 5-12 hours.[ Read more

Route of elimination

Within 72 hours, 75% of a dose of fentanyl is excreted in the urine with Read more

Toxicity

Fentanyl has an intravenous LD50 of 2.91mg/kg in rats[ Read more

Adverse Effects

Contraindications

  • Recommended Actions:
    • Avoid
  • Regions: US
  • Patient Conditions:
      • Name: Known or suspected paralytic ileus
      • Drugbank Id: DBCOND0120037
  • Recommended Actions:
    • Avoid
  • Regions: US
  • Patient Conditions:
      • Name: Known or suspected gastrointestinal obstruction
      • Drugbank Id: DBCOND0101705
  • Recommended Actions:
    • Avoid
  • Regions: US
  • Patient Conditions:
      • Name: Significant respiratory depression
      • Drugbank Id: DBCOND0107580
  • Hypersensitivity:
    • true
  • Regions: US
  • Route:
    • Transdermal
  • Regions: US
  • Patient Conditions:
      • Name: Paralytic Ileus
      • Drugbank Id: DBCOND0047064
  • Route:
    • Transdermal
  • Regions: US
  • Patient Conditions:
      • Name: Severe bronchial asthma
      • Drugbank Id: DBCOND0107864
      • Modification Of:
        • Base:
          • Name: Bronchial Asthma
          • Drugbank Id: DBCOND0031527
        • Severity:
          • Includes:
            • severe
  • Route:
    • Buccal
    • Transdermal
  • Regions: US
  • Patient Conditions:
      • Name: Management of postoperative pain
      • Drugbank Id: DBCOND0108019
  • Route:
    • Transdermal
  • Regions: US
  • Patient Conditions:
      • Name: Management of acute or intermittent pain
      • Drugbank Id: DBCOND0108020
  • Route:
    • Buccal
    • Transdermal
  • Regions: US
  • Patient Conditions:
      • Name: Opioid non-tolerant patients
      • Drugbank Id: DBCOND0108017
  • Route:
    • Buccal
    • Transdermal
  • Regions: US
  • Patient Conditions:
      • Name: Management of acute pain
      • Drugbank Id: DBCOND0108018
  • Route:
    • Transdermal
  • Regions: US
  • Patient Conditions:
      • Name: Respiratory compromise
      • Drugbank Id: DBCOND0108023
  • Route:
    • Transdermal
  • Regions: US
  • Patient Conditions:
      • Name: Acute bronchial asthma
      • Drugbank Id: DBCOND0107863
      • Modification Of:
        • Base:
          • Name: Bronchial Asthma
          • Drugbank Id: DBCOND0031527
        • Severity:
          • Includes:
            • acute
  • Route:
    • Transdermal
  • Regions: US
  • Patient Conditions:
      • Name: Short opioid analgesia requirement
      • Drugbank Id: DBCOND0108021
  • Route:
    • Transdermal
  • Regions: US
  • Patient Conditions:
      • Name: Management of mild pain
      • Drugbank Id: DBCOND0108022

Food Interactions

  • Avoid alcohol.

Interactions

Type in a drug name to check for interaction with Fentanyl
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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
(R)-warfarin
The risk or severity of adverse effects can be increased when Fentanyl is combined with (R)-warfarin.
(S)-Warfarin
The risk or severity of adverse effects can be increased when Fentanyl is combined with (S)-Warfarin.
1-benzylimidazole
The risk or severity of hypertension can be increased when Fentanyl is combined with 1-benzylimidazole.
2,5-Dimethoxy-4-ethylamphetamine
2,5-Dimethoxy-4-ethylamphetamine may increase the analgesic activities of Fentanyl.
2,5-Dimethoxy-4-ethylthioamphetamine
2,5-Dimethoxy-4-ethylthioamphetamine may increase the analgesic activities of Fentanyl.
4-Bromo-2,5-dimethoxyamphetamine
4-Bromo-2,5-dimethoxyamphetamine may increase the analgesic activities of Fentanyl.
4-hydroxycoumarin
The risk or severity of adverse effects can be increased when Fentanyl is combined with 4-hydroxycoumarin.
4-Methoxyamphetamine
The therapeutic efficacy of Fentanyl can be decreased when used in combination with 4-Methoxyamphetamine.
5-methoxy-N,N-dimethyltryptamine
The risk or severity of adverse effects can be increased when Fentanyl is combined with 5-methoxy-N,N-dimethyltryptamine.
6-Deoxyerythronolide B
The metabolism of Fentanyl can be decreased when combined with 6-Deoxyerythronolide B.
7-ethyl-10-hydroxycamptothecin
The metabolism of Fentanyl can be decreased when combined with 7-ethyl-10-hydroxycamptothecin.
7-Nitroindazole
The risk or severity of adverse effects can be increased when Fentanyl is combined with 7-Nitroindazole.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline
The risk or severity of adverse effects can be increased when 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline is combined with Fentanyl.
9-aminocamptothecin
The metabolism of Fentanyl can be decreased when combined with 9-aminocamptothecin.
Abacavir
Abacavir may decrease the excretion rate of Fentanyl which could result in a higher serum level.
Abatacept
The metabolism of Fentanyl can be increased when combined with Abatacept.
Abediterol
The risk or severity of hypertension can be increased when Fentanyl is combined with Abediterol.
Acalabrutinib
The metabolism of Fentanyl can be decreased when combined with Acalabrutinib.
Acarbose
Acarbose may decrease the excretion rate of Fentanyl which could result in a higher serum level.
Acebutolol
Fentanyl may decrease the antihypertensive activities of Acebutolol.
23 References
  1. 1 . Van Bever WF, Niemegeers CJ, Janssen PA: Synthetic analgesics. Synthesis and pharmacology of the diastereoisomers of N-(3-methyl-1-(2-phenylethyl)-4-piperidyl)-N-phenylpropanamide and N-(3-methyl-1-(1-methyl-2-phenylethyl)-4-piperidyl)-N-phenylpropanamide. J Med Chem. 1974 Oct;17(10):1047-51.PubMed: 4420811
  2. 2 . Taylor DR: Fentanyl buccal tablet: rapid relief from breakthrough pain. Expert Opin Pharmacother. 2007 Dec;8(17):3043-51.PubMed: 18001263
  3. 3 . Simpson DM, Messina J, Xie F, Hale M: Fentanyl buccal tablet for the relief of breakthrough pain in opioid-tolerant adult patients with chronic neuropathic pain: a multicenter, randomized, double-blind, placebo-controlled study. Clin Ther. 2007 Apr;29(4):588-601.PubMed: 17617282
  4. 4 . Roy SD, Flynn GL: Solubility behavior of narcotic analgesics in aqueous media: solubilities and dissociation constants of morphine, fentanyl, and sufentanil. Pharm Res. 1989 Feb;6(2):147-51.PubMed: 2569731
  5. 5 . DePriest AZ, Puet BL, Holt AC, Roberts A, Cone EJ: Metabolism and Disposition of Prescription Opioids: A Review. Forensic Sci Rev. 2015 Jul;27(2):115-45.PubMed: 26227254
  6. 6 . Al-Hasani R, Bruchas MR: Molecular mechanisms of opioid receptor-dependent signaling and behavior. Anesthesiology. 2011 Dec;115(6):1363-81. doi: 10.1097/ALN.0b013e318238bba6.PubMed: 22020140
  7. 7 . Bista SR, Haywood A, Hardy J, Lobb M, Tapuni A, Norris R: Protein binding of fentanyl and its metabolite nor-fentanyl in human plasma, albumin and alpha-1 acid glycoprotein. Xenobiotica. 2015 Mar;45(3):207-12. doi: 10.3109/00498254.2014.971093. Epub 2014 Oct 14.PubMed: 25314012
  8. 8 . Raffa RB, Pergolizzi JV Jr, LeQuang JA, Taylor R Jr, Colucci S, Annabi MH: The fentanyl family: A distinguished medical history tainted by abuse. J Clin Pharm Ther. 2018 Feb;43(1):154-158. doi: 10.1111/jcpt.12640. Epub 2017 Oct 4.PubMed: 28980330
  9. 9 . Schaefer CP, Tome ME, Davis TP: The opioid epidemic: a central role for the blood brain barrier in opioid analgesia and abuse. Fluids Barriers CNS. 2017 Nov 29;14(1):32. doi: 10.1186/s12987-017-0080-3.PubMed: 29183383
  10. 10 . Cooper J, Jauniaux E, Gulbis B, Quick D, Bromley L: Placental transfer of fentanyl in early human pregnancy and its detection in fetal brain. Br J Anaesth. 1999 Jun;82(6):929-31. doi: 10.1093/bja/82.6.929.PubMed: 10562792
  11. 11 . Streisand JB, Busch MA, Egan TD, Smith BG, Gay M, Pace NL: Dose proportionality and pharmacokinetics of oral transmucosal fentanyl citrate. Anesthesiology. 1998 Feb;88(2):305-9.PubMed: 9477048
  12. 12 . Parikh N, Goskonda V, Chavan A, Dillaha L: Pharmacokinetics and dose proportionality of fentanyl sublingual spray: a single-dose 5-way crossover study. Clin Drug Investig. 2013 Jun;33(6):391-400. doi: 10.1007/s40261-013-0079-8.PubMed: 23605506
  13. 13 . Ashburn MA, Ogden LL, Zhang J, Love G, Basta SV: The pharmacokinetics of transdermal fentanyl delivered with and without controlled heat. J Pain. 2003 Aug;4(6):291-7.PubMed: 14622685
  14. 14 . Nave R, Schmitt H, Popper L: Faster absorption and higher systemic bioavailability of intranasal fentanyl spray compared to oral transmucosal fentanyl citrate in healthy subjects. Drug Deliv. 2013 Jun-Jul;20(5):216-23. doi: 10.3109/10717544.2012.762435. Epub 2013 May 8.PubMed: 23650968
  15. 15 . FDA Approved Drug Products: Abstral Sublingual Tablet Link
  16. 16 . FDA Approved Drug Products: Actiq Transmucosal Lozenge Link
  17. 17 . FDA Approved Drug Products: Fentora Buccal Tablet Link
  18. 18 . FDA Approved Drug Products: Subsys Sublingual Spray Link
  19. 19 . FDA Approved Drug Products: Duragesic Transdermal System Link
  20. 20 . FDA Approved Drug Products: Lazanda Metered Nasal Spray Link
  21. 21 . FDA Approved Drug Products: Sublimaze Preservative Free Intramuscular and Intravenous Injection Link
  22. 22 . CDC Drug Overdose Deaths 2017 Link
  23. 23 . Government of Canada: Canada's opioid crisis Link