Fentanyl - IV Flashcards
What is the brand/trade name for fentanyl?
What is the pharmacologic category/class of fentanyl?
- Opioid Analgesic — Synthetic
- Phenylpiperidine
Apex Unit 5: Pharmacology 2; Opioid & Non-Opioid Analgesics; Lesson 4. Classification, Relative Potency & Opioid Abuse
What is the mechanism of action of fentanyl?
Opioid rececptor agonism, especially mu
- Presynaptic: decreases cAMP-dependent influx of calcium ions → inhibition of neurotransmitter release
- Post synaptic: increased outward K+ conductance → hyperpolarization of nerve cell
resultant increase in pain threshold, altered pain perception, and inhibition of ascending pain pathways
Note that these are similar to those of other opioids
Apex Unit 5: Pharmacology 2; Opioid & Non-Opioid Analgesics; Lesson 2. Opioid Receptors
DrugBank Online - Fentanyl
Nagelhout (7th ed.), pp. 141 - Fig. 11.2, 142, 1295-1296, 1298
Stoelting’s Pharmacology (5th ed.), pp. 218-219
The experience of pain can be divided into four steps: transduction, transmission, modulation, and perception. Which of these does fentanyl have an effect on?
Along with other opioids, fentanyl effects
- transduction (peripheral nerves)
- modulation (spinal cord)
- perception (brain/brainstem)
Apex Unit 5: Pharmacology 2; Opioid & Non-Opioid Analgesics; Lessons 1 & 2
When used as an adjunct during induction and intubation what dose of fentanyl is used?
- 1-3 mcg/kg IV
This helps to blunt the SNS response to laryngoscopy
Dosing is similar for pediatrics
Stoelting’s Pharmacology (5th ed.), p. 232
UpToDate - Fentanyl: Drug Information
What is the typical dose of fentanyl for procedural sedation and analgesia?
Emphasis because ranges may vary depending on patient/procedure
- 0.5-1 mcg/kg IV (or just like 25-100 mcg at a time)
repeated as often as every 2-15 minutes to achieve desired level of sedation/analgesia — continuous infusion is also an option
Dosing is similar for pediatrics
Stoelting’s Pharmacology (5th ed.), p. 232
UpToDate - Fentanyl: Drug Information
What is the onset of action for fentanyl?
- “Rapid/immediate” with maximal effects in 2-5 minutes
Nagelhout (7th ed.), p. 1298
Stoelting’s Pharmacology (5th ed.), p. 231
What is the duration of action for fentanyl?
- 30-60 minutes
Duration related to rapid redistribution to inactive tissue sites
What organ(s) are responsible for fentanyl’s clearance (metabolism/elimination)?
- Metabolism: Liver (P450)
- Elimination: Kidneys
Half-life: ~3-6 hrs — due to sequestration in tissues
As an analgesic, fentanyl is __________ times more potent than morphine
- ~100
This number varies slightly between texts
Anesthesia Guidebook - Episode 17: Anesthesia Top Drawer Run Down - Part 1
Apex Unit 5: Pharmacology 2; Opioid & Non-Opioid Analgesics; Lesson 4. Classification, Relative Potency & Opioid Abuse
Cardiovascular effects of fentanyl include:
- Bradycardia
- Stable SVR/MAP
no histamine release
Apex Unit 5: Pharmacology 2; Opioid & Non-Opioid Analgesics; Lessons 2 & 3
Stoelting’s Pharmacology (5th ed.), p. 233
What are the respiratory effects of fentanyl?
- Dose dependent depression of ventilation — RR affected before Vt
(shifting of the CO2 response curve) - Inhibits hypoxic ventilatory drive
- Apnea at large doses
Note that these are similar to those of other opioids
Apex Unit 5: Pharmacology 2; Opioid & Non-Opioid Analgesics; Lessons 2 & 3
Nagelhout (7th ed.), p. 142
Stoelting’s Pharmacology (5th ed.), p. 222
What are the effects of fentanyl on the CNS?
- Sedation
- Miosis/pinpoint pupils
- Mild hypothermia
resets hypothalamic temperature setpoint - N/V
Partial dopamine agonists at CTZ
Note that these are similar to those of other opioids
Apex Unit 5: Pharmacology 2; Opioid & Non-Opioid Analgesics; Lessons 2 & 3
Nagelhout (7th ed.), p. 142
Stoelting’s Pharmacology (5th ed.), p. 222
What are the GI/GU effects of fentanyl?
- Slowed peristalsis → CONSTIPATION
- N/V
- Contraction of sphincter of Oddi → biliary colic (meh)
evidence is kind meh on this - Delayed gastric emptying
- Urinary retention (IDGAF)
detrusor relaxation, urinary sphincter constriction
Note that these are similar to those of other opioids
Apex Unit 5: Pharmacology 2; Opioid & Non-Opioid Analgesics; Lessons 2 & 3
Nagelhout (7th ed.), pp. 143-144
Stoelting’s Pharmacology (5th ed.), pp. 223-224
Rapid IV administration of large doses of opioids, particularly fentanyl and its derivatives, can lead to generalized ______________; the greatest impact is on the ability to ______________
- Skeletal muscle rigidity
- Ventilate
some decrease in chest wall compliance, but this is mostly related to constriction of laryngeal musculature
Apex Unit 5: Pharmacology 2; Opioid & Non-Opioid Analgesics; Lesson 10. Skeletal Muscle Rigidity
Nagelhout (7th ed.), pp. 143-144
Stoelting’s Pharmacology (5th ed.), p. 223
BONUS
True or false:
- Fentanyl is more hydrophilic than morphine
- False
Fentanyl is more lipophilic, as evidenced by some of it’s pharmacokinetic and pharmacodynamic characteristics
Nagelhout (7th ed.), p. 147
Stoelting’s Pharmacology (5th ed.), p. 231
Why is fentanyl preferred over morphine in patients with renal failure?
- It’s metabolites are inactive
Apex Unit 5: Pharmacology 2; Opioid & Non-Opioid Analgesics; Lesson 5. Metabolism
Nagelhout (7th ed.), p. 147
What is the concentration (mcg/mL) of fentanyl vials?