Fentanyl

Introduction:
• Classification: Synthetic opoid

• Fentanyl is the most common used opioid in anesthesia.

• Fentanyl along with bupivacaine or ropivacaine is used as continuous

infusion for painless labor and postoperative analgesia.

• It is 100 times more potent than morphine.

• 1ml vial contains 50 mcg

 OPOID RECEPTORS:
Opioids act through specific receptors which have been classified into 4
types: µ (mu), K (kappa), delta (Delta) and nociceptin.

Although opioid receptors are mainly present in brain (where they are
called as supraspinal receptors) and spinal cord (substantia gelatinosa of
dorsal horn cells) however their presence at extra CNS sites like GIT is
well documented.
• µ (mu) Receptors:These are the most important receptors for the action of
opioids. These are further divided into µ1 and µ2.
 µ1: Mediates analgesia (mainly supraspinal but spinal also), sedation,
bradycardia, miosis, urinary retention , prolactin and growth hormone
release and muscle rigidity.
µ 2: Mediates respiratory depression, constipation and physical
dependence.
• K (kappa) Receptors: Mediates analgesia (mainly spinal but supraspinal
also), sedation, constipation, hallucinations, dependence and diuresis (contrary
to µ which causes urinary retention)
• (Delta) Receptors: Mediates analgesia (mainly spinal but supraspinal also).
• Nociceptin: Endogenous opioids mediate their action through nociceptin.
 Mechanism of Action of Opioids
• Supraspinal level: Opioids bind with receptors in rostroventral region
of medulla and cause stimulation of off cells present there, thereby
blocking nociceptive stimuli transmission.
• Spinal level: They act with their receptors present in substantia
gelatinosa of dorsal horn cells and inhibit the release of excitatory
transmitters.
• Cellular level: Opioids bind to receptors to stimulate G protein
synthesis and cAMP which causes K+ increase producing
hyperpolarization of membrane and decreases Ca++ decreasing
excitability.
• At high concentrations they can directly inhibit NMDA receptors.
 Pharmacokinetics:
• Dose: 2-5 mcg/kg

• Onset: 2-5 mins (rapid)

• Recovery: 1-2 hours (rapid)

• Route: iv, im, mucosal, transdermal, intrathecal

 Uses:
•Potent analgesic agent
•Premedication
•Inducing agent
•Blunt cardiovascular response in
intubation
•Painless labor using epidural analgesia
•Sedation in ICU
 Advantages of Fentanyl
• Due to high lipid solubility it has rapid onset (2 to 5 min.) and
rapid recovery (1-2 hours).

• It can be given by IM, IV, transmucosal, (fentanyl lollipop),

transdermal, (fentanyl patch), intrathecal and epidural route.

• Fentanyl patch provides analgesia for 72 hours.

• It is most cardiac stabile opioid.

 Adverse effects:
• Nausea, vomiting
• Respiratory depression
• Cardiac dysfunction
• Constipation
• Urine retension
• Dependence (physical, psychological)
• Tolerance
 References:
• Short textbook of Anethesia by Dr. Ajay Yadav

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