OPIOID | Basic Flashcards
How long does it take for a fentanyl patch to reach maximum plasma concentration?
30 hours
Receptors responsible for RESPIRATORY DEPRESSION
mu-2 receptors
O2 dissociation curve in Opioid Administration:
curve shift to THE RIGHT
The RESPIRATORY DEPRESSION induced by OPIOID is caused by:
INCREASING the CO2 apneic threshold in the MEDULLA
TRUE or FALSE
The context-sensitive halftime for REMIFENTANIL is independent of the duration of infusion.
The context-sensitive halftime of REMIFENTANIL is 4 MINUTES
TRUE
One of the clinical effect of Opioid is EPILEPTOGENIC due to Leu-enkephalin and B-endorphin agonism. What receptor is involved in this process?
delta receptors
Mu 1 receptors associated side effect?
EUPHORIA
Urinary Retention
Mu 2 receptors associated side effects?
Hypoventilation
Constipation
Physical Dependence
Kappa receptors associated side effects
Dysphoria
Hallucinations
Opioid effect that do not show tolerance
MIOSIS
CONSTIPATION
Remifentanil metabolism in infants is faster compared with that of Adults
TRUE
Equianalgesic of IV Morphine to PO
10mg IV = 30mg PO
Which narcotic has a local anesthetic activity?
MEPERIDINE
Narcotic effects that are not REVERSED by NALOXONE
Nausea/Vomiting
Constipation
MUSCLE RIGIDITY
PAIN receptor sites in the brain
AMYGDALA
PERI-AQUEDUCTAL GRAY
SOMATOSENSORY CORTEX (Locus Ceruleus & Rostral Ventral Medulla)
Dull “Burning” Pain
UNmyelinated C Fibers
Sharp “Pin prick” Pain
MYelinated Au FIBERS
Depression of Ventilation is due to what receptor involvement?
Mu-2
This is due to the BRAINSTEM involvement at the Mu-2 receptors
True of HYDROMORPHONE except:
A. The active metabolite hydromorphone-3-glucuronide has no analgesic properties but may cause neuroexcitation.
B. Peak effect is 15 mins
C. Equianalgesic of IV to PO is 1.5mg to 7.5mg
D. Used as a post-operative pain management due to its very short duration
D. Used as a post-operative pain management due to its very short duration
It has a long duration.
PURE OPIOID ANTAGNONISTS
Naloxone
Naltrexone
Nalmefene
These are ALL pure Mu opioid receptor antagonists with no agonist activity!
Stoelting | 5th Edit
True of NALOXONE except:
A. Is a nonselective antagonist at all three opioid receptors
B. Facilitate treatment of deliberate opioid overdose, and detect suspected physical dependence
C. Duration of action of naloxone (30 to 45 minutes) is presumed to be due to its rapid removal from the brain
D. Naloxone cannot easily cross the placenta
E. Administration of naloxone to an opioid-dependent parturient may produce acute withdrawal in the neonate
D. Naloxone cannot easily cross the placenta
Receives inputs from Ag and C primary afferent fibers
LAMINA - I
receives input primarily from LARGE diameters AB fibers from skin
Lamina IV - V
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AGONIST-ANTAGONIST Opioid
Pentazocine
Bremazocine
Dezocine
Maptazinol
Butorphanol
Buprenorphine
Nalorphine
NALBUPHINE
OPIOID Full ANTAGONIST
Naloxone
Naltrexone
Nalmefene
In the brain, opioid receptors are primarily found in:
Periaqeuductal gray
Locus Ceruleus
Rostral ventral medulla
The effect-site equilibration time(its time to PEAK analgesia) of fentanyl is:
A. 6.8 minutes
B. 3.5 minutes
C. 2.5 minutes
D. 5 minutes
The onset of CNS effects of Sulfentanil(effect-site equilibration time of 6.2 minutes is similar to that of 6.8 minutes for fentanyl)
Which of the following opioids has the longest context-sensitive halftime?
A. Fentanyl
B. Remifentanil
C. Sulfentanil
D. Alfentanil
Fentanyl
FROM LONGEST TO SHORTEST
F>A>S>R
Fentanyl > Alfentanil > Sulfentanil > Remifentanil
The effect-site equilibration time(its time to PEAK analgesia) of Alfentanil is:
A. 10 minutes
B. 2.5 minutes
C. 1.4 minutes
D. 5 minutes
C. 1.4 minutes
A unique advantage of alfentanil compared
with fentanyl and sufentanil is the more rapid onset of action (rapid effectsite equilibration) after the IV administration of alfentanil.
For example, the effect-site equilibration time for alfentanil is 1.4 minutes compared with 6.8
and 6.2 minutes for fentanyl and sufentanil, respectively.
Activation of opioid receptors leads to activation of
which intracellular transduction mechanism?
(A) G proteins
(B) adenylate cyclase
(C) voltage gated calcium channels
(D) voltage gated sodium channels
(E) outward recti ying potassium channels
(A) G proteins
G proteins (Gi and/or Go) are activated, as are inward rectifying potassium channels. Adenylate cyclase and voltage-gated calcium channels are inhibited by activation of the opioid receptor.
Voltage-gated sodium channels ARE NOT involved in opioid receptor-activated intracellular transduction mechanisms.
Which of the following opioids is the most hydrophilic?
(A) morphine
(B) fentanyl
(C) codeine
(D) methadone
(E) heroin
(A) morphine
Morphine has a relatively low lipid solubility.
Fentanyl, codeine, methadone, and heroin are all more lipophilic than morphine.
An adult is administered a single dose o entanyl
(100 micrograms intravenously). The clinical effects
of fentanyl are terminated mainly by:
(A) redistribution
(B) hydroxylation
(C) N-dealkylation
(D) conjugation
(E) demethylation
(A) redistribution
After a small bolus of fentanyl the plasma and CSF
levels of fentanyl rapidly diminish due to redistribution to muscle and at. Fentanyl undergoes N-dealkylation and hydroxylation in the liver.
Which opioid has the longest duration of action
after epidural injection?
(A) alfentanil
(B) fentanyl
(C) hydromorphone
(D) methadone
(E) morphine
(E) morphine
Morphine is relatively hydrophilic compared to the
other listed opioids.
This means morphine will remain in the CSF or a longer period of time—up to 24 hours after a single bolus.
