- March 15, 2022
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Brand Name :
Sublimaze
Synonyms :
fentanyl
Class :
Opioids, Opioid Analgesics; Synthetic
Dosage forms & Strengths
IM/IV injection
0.05mg/mL
Indicated for Surgery Premedication
Administer a dose of 50-100 mcg via IM injection or slow IV infusion 30-60 min before the surgery.
As an adjunct to regional anesthesia, administer a slow IV infusion of 25-100 mcg over a period of 1-2 min.
General Anesthesia
For minor surgical procedures, administer an IV dose of 0.5-2 mcg /kg of body weight. For major surgeries, start with an initial dose of 2-20 mcg/kg of body weight, followed by a maintenance infusion of 1-2 mcg/kg of body weight per hour via IV route. Stop the infusion 30-60 minutes before the surgery ends and restrict the total amount of fentanyl doses to 10-15 mcg/ kg of body weight to enable rapid recovery and early removal of the breathing tube. fentanyl is rarely used as an adjunct to general anesthesia, but if required, administer an IV dose of 20-50 mcg/kg of body weight.
Analgesia as off-label
Administer a bolus IV dose of 1-2 mcg/kg of body weight or a dose of 25-100 mcg as needed or deliver a continuous IV infusion of 1-2 mcg/kg of body weight/hr, or 25-200 mcg/hr. In cases of severe pain, administer a dose of 50-100 mcg via IV or IM route every 1-2 hours as needed. Patients who have been previously exposed to opioids may tolerate higher initial doses.
For patient-controlled analgesia (PCA), use a concentration of 10 mcg/ml via IV route. The demand dose should be 20 mcg, with a lockout interval of 5-10 minutes, and a base rate of no more than 50 mcg per hour.
Dosage forms & Strengths
IM/IV injection
0.05mg/mL
Indicated for Surgery Premedication as off-label
For patients aged 1-12 years, administer an IV dose of 0.5-2 mcg/kg of body weight 3 minutes before the procedure. The dose can be repeated every 1-2 hours as needed.
For patients over 12 years of age, administer an IV dose of 0.5-2 mcg/kg of body weight per dose, not exceeding 50 mcg/dose, 3 minutes prior to the procedure. If necessary, the dose can be repeated after 5 minutes. If more than two doses are needed, the dose can be repeated up to 5 times, with a maximum dose of 25 mcg/dose.
Continuous Sedation or Analgesia
Administer a continuous IV infusion of 0.5-2 mcg /kg of body weight/hr and titrate the dose to achieve the desired effect.
Adjunct Anesthesia
Age < 2years: safety and efficacy of this medication have not been established.
Age > 2years: Administer a dose of 2-3 mcg/kg of body weight via IV or IM route every 1-2 hours as needed.
Refer to adult dosing
may enhance the concentration of serum when combined with fentanyl
may enhance the concentration of serum when combined with fentanyl
may enhance the concentration of serum when combined with fentanyl
may enhance the concentration of serum when combined with fentanyl
may enhance the concentration of serum when combined with fentanyl
fentanyl: they may enhance the serum concentration of CYP3A Inhibitors
fentanyl: they may enhance the serum concentration of CYP3A Inhibitors
fentanyl: they may enhance the serum concentration of CYP3A Inhibitors
fentanyl: they may enhance the serum concentration of CYP3A Inhibitors
fentanyl: they may enhance the serum concentration of CYP3A Inhibitors
may enhance the serum concentration of CYP3A4 Inhibitors
It may enhance effects when combined with tramadol by pharmacodynamic synergism
It may enhance the effect when combined with pharmacodynamic synergism
It may enhance the effects when combined with tasimelteon by pharmacodynamic synergism
it enhances the serotonergic effect of MAO inhibitors
it enhances the serotonergic effect of MAO inhibitors
it enhances the serotonergic effect of MAO inhibitors
it enhances the serotonergic effect of MAO inhibitors
it enhances the serotonergic effect of MAO inhibitors
the effect of fentanyl is decreased by lorlatinib, by altering intestinal or hepatic CYP3A4 enzyme metabolism
fentanyl increases the effect of lapatinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
CYP3A strong enhancers of the small intestine may reduce the bioavailability of fentanyl
metronidazole enhances the effect of fentanyl by altering the intestinal or hepatic CYP3A4 enzyme metabolism
it increases the effect of CNS depressants
CNS depressants increase the effect of paraldehyde
CNS depressants increase the CNS depressing effect of thalidomide
CNS depressants increase the effect of flunarizine
it decreases by affecting the hepatic enzyme CYP3A4 metabolism
it increases the effect of CNS depressants
may increase the serotonergic effect of Monoamine Oxidase Inhibitors
acetaminophen/dextromethorphan/pseudoephedrine/guaifenesin
may diminish the serum concentration
brompheniramine, dextromethorphan and phenylephrine
may diminish the serum concentration
may diminish the serum concentration
May have an increased serotonergic effect when combined with Serotonin/Norepinephrine Reuptake Inhibitors
May have an increased serotonergic effect when combined with Serotonin/Norepinephrine Reuptake Inhibitors
May have an increased serotonergic effect when combined with Serotonin/Norepinephrine Reuptake Inhibitors
May have an increased serotonergic effect when combined with Serotonin/Norepinephrine Reuptake Inhibitors
May have an increased serotonergic effect when combined with Serotonin/Norepinephrine Reuptake Inhibitors
fentanyl: they may diminish the serum concentration of CYP3A4 Inducers
fentanyl: they may diminish the serum concentration of CYP3A4 Inducers
fentanyl: they may diminish the serum concentration of CYP3A4 Inducers
fentanyl: they may diminish the serum concentration of CYP3A4 Inducers
fentanyl: they may diminish the serum concentration of CYP3A4 Inducers
When fentanyl is used together with bromisoval, the risk or seriousness of CNS depression is enhanced
The potential for CNS depression may enhanced when fentanyl is used together with fencamfamin
When fentanyl is used together with niaprazine, the risk or seriousness of CNS depression is enhanced
fedratinib increases the effect of fentanyl by altering the intestinal/ hepatic CYP3A4 enzyme metabolism
lofexidine may enhance the CNS depressant effect of CNS depressants
may increase the CNS depressant effect
may enhance the activity
may increase the CNS depressant effect
may increase the CNS depressant effect
may increase the CNS depressant effect
may increase the sedative effect of CNS depressants
may diminish the serum concentration of decongestants
may diminish the serum concentration of decongestants
may increase the CNS depressant effect
it increases the effect of CNS depressants
Actions and Spectrum:
fentanyl is a synthetic opioid that is generally used medically for pain relief and anesthesia. It works by binding to specific opioid receptors in brain and spinal cord, which decrease the perception of pain and produces a sense of euphoria.
The spectrum of fentanyl’s effects can range from pain relief to sedation, respiratory depression, and ultimately, death. The onset of action of fentanyl is rapid, with peak effects occurring within minutes of administration, making it useful for acute pain management.
Frequency not defined
Dyspepsia
Visual disturbances
Angina pectoris
Sedation
Hemoptysis
Faintness
Dry mouth
Agitation
Confusion
Respiratory/circulatory depression
Sweating
Amnesia
Upper respiratory tract infection
Application-site reaction
Anxiety
Fever
Rhinitis
Hiccups
Syncope
Severe cardiac arrhythmias
Dyspnea
Back pain
Paranoid reaction
Urinary retention
Diarrhea
Myocardial infarction (MI)
Bronchitis
Seizures
Pruritus
Constipation
Euphoria
Speech disorder
Coma
Nausea
Sweating
Accidental injury
Tremor
Dysphoria
Paresthesia
Depression
Bradycardia
Pharyngitis
Respiratory arrest
Weakness
Vomiting
Influenzalike symptoms
ST-segment elevation
Hallucinations
Oliguria
QT-interval prolongation
Sweating
Cardiac arrest
Sinusitis
Dizziness
Abdominal pain
Ventricular tachycardia
Mental clouding
Black Box Warning:
The black box warning highlights the following potential risks associated with fentanyl:
Contraindication/Caution:
Contraindication
Caution
Pregnancy consideration:
AU TGA pregnancy category: C
US FDA pregnancy category: C
Lactation:
Excreted into human milk: Yes
Pregnancy category:
Pharmacology:
fentanyl is a potent synthetic opioid used for pain management and anesthesia. It acts by binding to opioid receptors in the brain and spinal cord, decreasing the perception of pain.
fentanyl is a mu-opioid receptor agonist, meaning it activates the mu-opioid receptors in the brain and spinal cord. This activation leads to the reduction of pain perception and the production of analgesia.
Pharmacodynamics:
Mechanism of action: This drug is a narcotic agonist-analgesic that targets opiate receptors. It works by inhibiting ascending pain pathways, which alters the body’s response to pain and increases the pain threshold. The drug’s main effects include analgesia, respiratory depression, and sedation.
Pharmacokinetics:
Absorption
The bioavailability is 50%, and the onset of the drug is immediate when administered intravenously and takes 7-15 minutes when administered intramuscularly. The duration of the drug is 0.5-1 hour when given intravenously and 1-2 hours when given intramuscularly. The peak plasma time for intravenous administration (≤100 mcg) is 30-60 minutes, while it is 1-2 hours for intramuscular administration. Adverse effects occur when the concentration of the drug exceeds 2 ng/mL, and the concentration of the drug is typically 0.2-2 ng/mL.
Distribution
fentanyl is protein-bound to a range of 80-85%, which means that most of the drug in the body is bound to proteins. The volume of distribution (Vd) of the drug is 4-6 liters per kilogram
Metabolism
fentanyl is metabolized in the liver by the enzyme CYP3A4, which is responsible for breaking down many drugs in the body.
Elimination and Excretion
The half-life of the drug is between 2 to 4 hours. The total plasma clearance of the drug is 8.3 mL/min/kg, indicating the rate at which the drug is removed from the bloodstream. The drug is primarily excreted from the body through urine (75%) and feces (9%).
Administration:
IV or IM Administration
fentanyl is a synthetic opioid medication used for the treatment of severe pain, such as pain related to cancer or surgery. fentanyl is a prescription medication that is available in various forms, including injectable solutions, transdermal patches, lozenges, and nasal sprays.
The administration of fentanyl should always be done under the supervision of a healthcare professional who is experienced in the use of opioids. fentanyl should be prescribed at the lowest effective dose and for the shortest duration possible to minimize the risk of addiction, dependence, and overdose.
Patient information leaflet
Generic Name: fentanyl
Why do we use fentanyl?
fentanyl is synthetic opioid medication used for the treatment of severe pain, such as pain related to cancer, surgery, or trauma. It is one of the most potent opioid medications available and is generally used when other pain medications have not provided sufficient pain relief.
Common uses of fentanyl:
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