FANTANYL a potent, synthetic opioid analgesic with a rapid onset and short

duration of action. It is a strong agonist at the -opioid receptors.

MECHANISM OF ACTION: Fentanyl provides some of the effects typical of other
opioids through its agonism of the opioid receptors. Its strong potency in relation
to that of morphine is largely due to its highlipophilicity.
Binds with stereospecific receptors at many sites within the CNS, increases pain
threshold, alters pain reception, inhibits ascending pain pathways

USES:
IntravenouS
Intravenous fentanyl is often used for anesthesia and analgesia.
local anesthetic for neuraxial administration (epidural or intrathecal/spinal)
procedural sedationfor endoscopy, cardiac catheterization, oral surgery, etc.,
management of chronic pain including cancer pain
Patches

ADVERSE EFFECTS
diarrhea, nausea, constipation, dry mouth, somnolence,
confusion, asthenia (weakness), and sweating and, less frequently (3 to 10% of
patients), abdominal pain, headache, fatigue, anorexia and weight loss,
dizziness, nervousness, hallucinations, anxiety, depression, flu-like
symptoms, dyspepsia (indigestion), dyspnea (shortness of
breath), hypoventilation, apnea, and urinary retention. Fentanyl use has also
been associated with aphasia.
Fentanyl has a therapeutic index of 270.[41]

Pharmacodynamics and Pharmacokinetics

Onset of action: Analgesic:

IM: 7 to 8 minutes;
IV: Almost immediate
Transdermal (initial placement): 6 hours;
Transmucosal: 5 to 15 minutes
Duration:
IM: 1 to 2 hours;
IV: 0.5 to 1 hour;
Transdermal 72 to 96 hours

Distribution:
4 to 6 L/kg; Highly lipophilic, redistributes into muscle and fat
Protein binding:
79% to 87%
Metabolism:
Hepatic, primarily via CYP3A4
Bioavailability:
Buccal film: 71% (mucositis did not have a clinically significant effect on
Cmax and AUC; however, bioavailability is expected to decrease if film is
inappropriately chewed and swallowed)
Buccal tablet: 65%
Lozenge: ~50%
Sublingual spray: 76%
Sublingual tablet: 54%

Half-life elimination:
IV: 2 to 4 hours; when administered as a continuous infusion, the half-life
due to the large volume of distribution
Transdermal device: Terminal: ~16 hours
Transdermal patch:
20 to 27 hours
Transmucosal products:
3 to 14 hours
Time to peak:

Buccal film: 0.75 to 4 hours (median: 1 hour)

Buccal tablet: 20 to 240 minutes (median: 47 minutes)
Lozenge: 20 to 480 minutes (median: 20 to 40 minutes)
Nasal spray: Median: 15 to 21 minutes
Sublingual spray: 10 to 120 minutes (median: 90 minutes)
Sublingual tablet: 15 to 240 minutes (median: 30 to 60 minutes)
Transdermal patch: 20 to 72 hours; steady state serum concentrations are
reached after two sequential 72-hour applications
Excretion: Urine 75% (primarily as metabolites, <7% to 10% as unchanged
drug); feces ~9%

CONTRAINDICATIONS
Hypersensitivity to fentanyl or any component of the formulation

DOSAGE:
STAT : 1-2MCG/KG/DOSE
INFUSION : 1-6MCG/KG/HR