Pharmacology Book

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Fentanyl

Aka: Fentanyl, Transdermal Fentanyl, Fentanyl Patch, Duragesic, Sublimaze
  1. Class
    1. Short acting Narcotic (except Transdermal Fentanyl)
  2. Indication
    1. Chronic Pain (especially Cancer Pain Management)
    2. Short-acting Labor Analgesia
  3. Contraindications
    1. Mild pain, acute pain or postoperative pain due to risk of respiratory depression (FDA Black Box warning)
  4. Dosing: Child (for anesthesia or Sedation)
    1. Dose: 1-3 mcg/kg/dose (maximum: 50 ug) IV or IM
      1. May repeat Fentanyl (same dose) q2 minutes to effect
      2. Most patients require 3-5 Fentanyl doses (3-5 ug/kg)
    2. Consider administering with Versed
      1. Versed: 0.1 mg/kg (maximum: 2 mg)
  5. Dosing: Adult
    1. Transdermal Fentanyl (Duragesic)
      1. Available strengths: 25, 50, 75, 100 mcg/hour
      2. Onset of full effect only after 24 hours (steady state may not be reached for 1 week)
      3. Change patch ever 72 hours
        1. In atypical cases may need to be changed every 48 hours for end-of-dose pain
        2. Should not be changed more often than every 48 hours
      4. Conversions from prior morphine (total per 24 hours)
        1. Fentanyl 25 mcg/h: MS 37.5 mg PO or 12.5 mg IV
        2. Fentanyl 50 mcg/h: MS 75 mg PO or 25 mg IV
        3. Fentanyl 75 mcg/h: MS 112 mg PO or 37.5 mg IV
        4. Fentanyl 100 mcg/h: MS 150 mg PO or 50 mg IV
    2. Transmucosal Lozenge (Actiq)
      1. Available strengths: 200, 400, 800, 1200, 1600 ug
      2. Maximum: 4 lozenges per day
  6. Pharmacokinetics
    1. Intramuscular
      1. Onset: 7 to 15 minutes
      2. Peak: 15 minutes
      3. Duration: 1 to 2 hours
    2. Intravenous
      1. Onset: minutes
      2. Peak: minutes
      3. Duration: 30 to 60 minutes
  7. Precautions
    1. Respiratory Depression (FDA Black Box Warning)
    2. Oversedation
      1. Antagonist: Naloxone (Narcan)
  8. Efficacy: Non-Cancer Chronic Pain
    1. Transdermal Fentanyl preferred over oral morphine
      1. Better pain relief
      2. Improved quality of life
    2. Reference
      1. Allan (2001) BMJ 322:1154-8

Duragesic (C0591423)

Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH D005283
English Janssen Pharmaceutica Brand of Fentanyl, Duragesic, Durogesic, durogesic, duragesic
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Fentanyl (C0015846)

Definition (CHV) a kind of narcotic pain relieving drug
Definition (CHV) a kind of narcotic pain relieving drug
Definition (CHV) a kind of narcotic pain relieving drug
Definition (MSH) A potent narcotic analgesic, abuse of which leads to habituation or addiction. It is primarily a mu-opioid agonist. Fentanyl is also used as an adjunct to general anesthetics, and as an anesthetic for induction and maintenance. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1078)
Definition (PSY) Synthetic opiate frequently used illicitly.
Definition (CSP) potent narcotic analgesic, abuse of which leads to habituation or addiction; primarily a mu-opioid agonist, used as an adjunct to general anesthetics, and as an anesthetic for induction and maintenance.
Definition (NCI) A synthetic, lipophilic phenylpiperidine opioid agonist with analgesic and anesthetic properties. Fentanyl selectively binds to the mu-receptor in the central nervous system (CNS) thereby mimicking the effects of endogenous opiates. Stimulation of the mu-subtype opioid receptor stimulates the exchange of GTP for GDP on the G-protein complex and subsequently inhibits adenylate cyclase. This results in a decrease in intracellular cAMP and leads to a reduction in the release of neurotransmitters such as substance P, GABA, dopamine, acetylcholine and noradrenaline. The analgesic effect of fentanyl is likely due to its metabolite morphine, which induces opening of G-protein-coupled inwardly rectifying potassium (GIRK) channels and blocks the opening of N-type voltage-gated calcium channels, thereby resulting in hyperpolarization and reduced neuronal excitability.
Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH D005283
SnomedCT 373492002, 40648001
English Fentanyl, Phentanyl, Propanamide, N-phenyl-N-(1-(2-phenylethyl)-4-piperidinyl)-, Fentyl, fentanyl, fentanyl (medication), FENTANYL, Fentanyl [Chemical/Ingredient], fentanyls, phentanyl, fentaNYL, Fentanyl product, Fentanyl (product), Fentanyl (substance)
Swedish Fentanyl
Czech fentanyl
Finnish Fentanyyli
Russian TSITRAT FENTANILA, FENTANEST, LEPTANAL, SENTONIL, SUBLIMAZ, FENTANIL, FENTANILA TSITRAT, ЛЕПТАНАЛ, СЕНТОНИЛ, СУБЛИМАЗ, ФЕНТАНЕСТ, ФЕНТАНИЛ, ФЕНТАНИЛА ЦИТРАТ, ЦИТРАТ ФЕНТАНИЛА
Japanese フェンタニル, フェンタニール
Croatian FENTANIL
Polish Fentanyl
Spanish fentanilo (producto), fentanilo (sustancia), fentanilo, Fentanilo
French Fentanyl
German Fentanyl, Phentanyl
Italian Fentanil
Portuguese Fentanila
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Sublimaze (C0015845)

Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH D005283
English sublimaze, Sublimaze
Sources
Derived from the NIH UMLS (Unified Medical Language System)


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